"Warren Center for Neuroscience Drug Discovery" - Search Results

Year	Number of Results
2020	9
2021	28
2022	23
2023	21
2024	28
2025	10

1

Total Synthesis and Pharmacological Evaluation of Phochrodines A-C.

Bouchard JL, Chang S, Krishnan S, Presley CC, Boutaud O, Schley ND, Engers DW, Engers JL, Lindsley CW, Bender AM. Bouchard JL, et al. J Nat Prod. 2025 Apr 1. doi: 10.1021/acs.jnatprod.5c00104. Online ahead of print. J Nat Prod. 2025. PMID: 40169259

2

Application of Deuterium in an M₁ Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422.

Engers JL, Li J, Han C, Long MF, Gregro AR, Presley CC, Dickerson JW, Peng W, Cho HP, Rodriguez AL, Xiang Z, Boutaud O, O'Carroll C, Dey PM, Burstein ES, Niswender CM, Rook JM, Conn PJ, Engers DW, Lindsley CW. Engers JL, et al. ACS Chem Neurosci. 2025 Apr 16;16(8):1582-1591. doi: 10.1021/acschemneuro.5c00119. Epub 2025 Mar 25. ACS Chem Neurosci. 2025. PMID: 40132023 Free PMC article.

3

Shank3 modulates Rpl3 expression and protein synthesis via mGlu5: implications for Phelan McDermid syndrome.

Giona F, Beretta S, Zippo A, Stefanoni A, Tomasoni Z, Vicidomini C, Ponzoni L, Sala M, Jones CK, Conn PJ, Boeckers TM, Sala C, Verpelli C. Giona F, et al. Mol Psychiatry. 2025 Mar 15. doi: 10.1038/s41380-025-02947-9. Online ahead of print. Mol Psychiatry. 2025. PMID: 40089604

4

M₄ Positive Allosteric Modulator VU0467154 Impacts Amphetamine Sensitization and Spontaneous Locomotion in Male Mice.

Berezovskaia A, Lindsley C, Fink-Jensen A, Wörtwein G. Berezovskaia A, et al. ACS Chem Neurosci. 2025 Mar 5;16(5):868-879. doi: 10.1021/acschemneuro.4c00795. Epub 2025 Feb 21. ACS Chem Neurosci. 2025. PMID: 39982140

5

Discovery of ONO-2920632 (VU6011887): A Highly Selective and CNS Penetrant TREK-2 (TWIK-Related K+ Channel 2) Preferring Activator In Vivo Tool Compound.

Yashiro K, Iwaki Y, Urata H, Kokubo M, Mori T, Sekioka Y, Isami K, Kato J, Wieting J, McGowan KM, Bridges TM, Boutaud O, Engers DW, Denton JS, Kurata H, Lindsley CW. Yashiro K, et al. ACS Chem Neurosci. 2025 Mar 5;16(5):960-967. doi: 10.1021/acschemneuro.5c00032. Epub 2025 Feb 21. ACS Chem Neurosci. 2025. PMID: 39981749 Free PMC article.

6

Cryo-EM reveals a new allosteric binding site at the M₅ mAChR.

Burger WAC, Mobbs JI, Rana B, Wang J, Joshi K, Gentry PR, Yeasmin M, Venugopal H, Bender AM, Lindsley CW, Miao Y, Christopoulos A, Valant C, Thal DM. Burger WAC, et al. bioRxiv [Preprint]. 2025 Feb 8:2025.02.05.636602. doi: 10.1101/2025.02.05.636602. bioRxiv. 2025. PMID: 39975287 Free PMC article. Preprint.

7

Synthesis of a Hydroxy-15-Azasterol.

Jones CAH, Melancon BJ, Lindsley CW. Jones CAH, et al. ACS Omega. 2025 Jan 31;10(5):4784-4791. doi: 10.1021/acsomega.4c09907. eCollection 2025 Feb 11. ACS Omega. 2025. PMID: 39959107 Free PMC article.

8

Further Optimization of the mGlu₁ PAM VU6024578/BI02982816: Discovery and Characterization of VU6033685.

Reed CW, Kalbfleisch JF, Turkett JA, Trombley TA, Spearing PK, Haymer DH, Quitalig M, Dickerson JW, Foster DJ, Blobaum AL, Boutaud O, Cho HP, Niswender CM, Rook JM, Priepke H, Sommer H, Scheuerer S, Ursu D, Conn PJ, Melancon BJ, Lindsley CW. Reed CW, et al. ACS Chem Neurosci. 2025 Feb 19;16(4):745-752. doi: 10.1021/acschemneuro.5c00014. Epub 2025 Feb 5. ACS Chem Neurosci. 2025. PMID: 39907715 Free PMC article.

9

Discovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.

Childress ES, Capstick RA, Crocker KE, Ledyard ML, Bender AM, Maurer MA, Billard NB, Cho HP, Rodriguez AL, Niswender CM, Peng W, Rook JM, Chang S, Blobaum AL, Boutaud O, Thompson Gray A, Jones CK, Conn PJ, Felts AS, Lindsley CW, Temple KJ. Childress ES, et al. ACS Med Chem Lett. 2024 Nov 18;15(12):2210-2219. doi: 10.1021/acsmedchemlett.4c00481. eCollection 2024 Dec 12. ACS Med Chem Lett. 2024. PMID: 39691522 Free PMC article.

10

Discovery of VU6024578/BI02982816: An mGlu₁ Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models.

Reed CW, Kalbfleisch JF, Turkett JA, Trombley TA, Nastase AF, Spearing PK, Haymer DH, Sarwar MM, Quitalig M, Dickerson JW, Blobaum AL, Boutaud O, Voehringer P, Schuelert N, Cho HP, Niswender CM, Rook JM, Priepke H, Ursu D, Conn PJ, Melancon BJ, Lindsley CW. Reed CW, et al. J Med Chem. 2024 Dec 26;67(24):22291-22312. doi: 10.1021/acs.jmedchem.4c02554. Epub 2024 Dec 12. J Med Chem. 2024. PMID: 39665415 Free PMC article.

11

Discovery of VU0467319: an M₁ Positive Allosteric Modulator Candidate That Advanced into Clinical Trials.

Poslunsey MS, Wood MR, Han C, Stauffer SR, Panarese JD, Melancon BJ, Engers JL, Dickerson JW, Peng W, Noetzel MJ, Cho HP, Rodriguez AL, Hopkins CR, Morrison R, Crouch RD, Bridges TM, Blobaum AL, Boutaud O, Daniels JS, Kates MJ, Castelhano A, Rook JM, Niswender CM, Jones CK, Conn PJ, Lindsley CW. Poslunsey MS, et al. ACS Chem Neurosci. 2025 Jan 1;16(1):95-107. doi: 10.1021/acschemneuro.4c00769. Epub 2024 Dec 11. ACS Chem Neurosci. 2025. PMID: 39660766 Free PMC article. Clinical Trial.

12

Move over COVID, Tuberculosis Is Once again the Leading Cause of Death from a Single Infectious Disease.

Berida T, Lindsley CW. Berida T, et al. J Med Chem. 2024 Dec 26;67(24):21633-21640. doi: 10.1021/acs.jmedchem.4c02876. Epub 2024 Dec 9. J Med Chem. 2024. PMID: 39652566 No abstract available.

13

What Is Pink Cocaine? The Dark Reality behind a Colorful Name.

Barbaro L, Bouchard JL. Barbaro L, et al. J Med Chem. 2024 Dec 12;67(23):20733-20736. doi: 10.1021/acs.jmedchem.4c02821. Epub 2024 Dec 3. J Med Chem. 2024. PMID: 39624978 No abstract available.

14

The cannabinoid CB₂ receptor positive allosteric modulator EC21a exhibits complicated pharmacology in vitro.

Qi A, Han X, Quitalig M, Wu J, Christov PP, Jeon K, Jana S, Kim K, Engers DW, Lindsley CW, Rodriguez AL, Niswender CM. Qi A, et al. J Recept Signal Transduct Res. 2024 Aug;44(4):151-159. doi: 10.1080/10799893.2024.2431986. Epub 2024 Nov 22. J Recept Signal Transduct Res. 2024. PMID: 39575892 Free article.

15

Spermine oxidase promotes Helicobacter pylori-mediated gastric carcinogenesis through acrolein production.

McNamara KM, Sierra JC, Latour YL, Hawkins CV, Asim M, Williams KJ, Barry DP, Allaman MM, Zagol-Ikapitte I, Luis PB, Schneider C, Delgado AG, Piazuelo MB, Tyree RN, Carson KS, Choksi YA, Coburn LA, Gobert AP, Wilson KT. McNamara KM, et al. Oncogene. 2025 Feb;44(5):296-306. doi: 10.1038/s41388-024-03218-7. Epub 2024 Nov 10. Oncogene. 2025. PMID: 39523394 Free PMC article.

16

Classics in Chemical Neuroscience: Medetomidine.

de Andrade Horn P, Berida TI, Parr LC, Bouchard JL, Jayakodiarachchi N, Schultz DC, Lindsley CW, Crowley ML. de Andrade Horn P, et al. ACS Chem Neurosci. 2024 Nov 6;15(21):3874-3883. doi: 10.1021/acschemneuro.4c00583. Epub 2024 Oct 15. ACS Chem Neurosci. 2024. PMID: 39405508 Free PMC article. Review.

17

Synthesis of the Dimeric Diarylheptanoids Alpinidinoid C and Officinine B Enabled by Blue-Light-Mediated Triple-Minisci-Type Alkylation.

Schultz DC, Rathnayake U, Duncan RA, Richardson AE, Bender AM. Schultz DC, et al. Org Lett. 2024 Oct 25;26(42):9028-9033. doi: 10.1021/acs.orglett.4c03227. Epub 2024 Oct 10. Org Lett. 2024. PMID: 39388634 Free PMC article.

18

Elucidating the molecular logic of a metabotropic glutamate receptor heterodimer.

Lin X, Provasi D, Niswender CM, Asher WB, Javitch JA. Lin X, et al. Nat Commun. 2024 Oct 3;15(1):8552. doi: 10.1038/s41467-024-52822-4. Nat Commun. 2024. PMID: 39362861 Free PMC article.

19

Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M₄ Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM).

Engers JL, Baker LA, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Cho HP, Bubser M, Gray AT, Jones CK, Peng W, Rook JM, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ. Engers JL, et al. ACS Chem Neurosci. 2024 Sep 24;15(20):3744-54. doi: 10.1021/acschemneuro.4c00465. Online ahead of print. ACS Chem Neurosci. 2024. PMID: 39316465 Free PMC article.

20

Characterization of four structurally diverse inhibitors of SUR2-containing K_ATP channels.

Li K, Satpute Janve V, Denton J. Li K, et al. Channels (Austin). 2024 Dec;18(1):2398565. doi: 10.1080/19336950.2024.2398565. Epub 2024 Sep 20. Channels (Austin). 2024. PMID: 39303216 Free PMC article.

21

Discovery of VU6007496: Challenges in the Development of an M₁ Positive Allosteric Modulator Backup Candidate.

Engers JL, Bollinger KA, Capstick RA, Long MF, Bender AM, Dickerson JW, Peng W, Presley CC, Cho HP, Rodriguez AL, Niswender CM, Moran SP, Xiang Z, Blobaum AL, Boutaud O, Rook JM, Engers DW, Conn PJ, Lindsley CW. Engers JL, et al. ACS Chem Neurosci. 2024 Sep 18;15(18):3421-3433. doi: 10.1021/acschemneuro.4c00508. Epub 2024 Aug 28. ACS Chem Neurosci. 2024. PMID: 39197083 Free PMC article.

22

It's Not "Just Weed" Anymore.

Gilliland K. Gilliland K. J Med Chem. 2024 Sep 12;67(17):14697-14699. doi: 10.1021/acs.jmedchem.4c01854. Epub 2024 Aug 15. J Med Chem. 2024. PMID: 39145761 No abstract available.

23

Discovery of VU6008677: A Structurally Distinct Tricyclic M₄ Positive Allosteric Modulator with Improved CYP450 Profile.

Capstick RA, Bollinger SR, Engers JL, Long MF, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ. Capstick RA, et al. ACS Med Chem Lett. 2024 Jul 3;15(8):1358-1366. doi: 10.1021/acsmedchemlett.4c00249. eCollection 2024 Aug 8. ACS Med Chem Lett. 2024. PMID: 39140069 Free PMC article.

24

Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M₅ Muscarinic Acetylcholine Receptor.

Li J, Orsi DL, Engers JL, Long MF, Capstick RA, Maurer MA, Presley CC, Vinson PN, Rodriguez AL, Han A, Cho HP, Chang S, Jackson M, Bubser M, Blobaum AL, Boutaud O, Nader MA, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Li J, et al. J Med Chem. 2024 Aug 22;67(16):14394-14413. doi: 10.1021/acs.jmedchem.4c01193. Epub 2024 Aug 6. J Med Chem. 2024. PMID: 39105778 Free PMC article.

25

Structural basis of positive allosteric modulation of metabotropic glutamate receptor activation and internalization.

Strauss A, Gonzalez-Hernandez AJ, Lee J, Abreu N, Selvakumar P, Salas-Estrada L, Kristt M, Arefin A, Huynh K, Marx DC, Gilliland K, Melancon BJ, Filizola M, Meyerson J, Levitz J. Strauss A, et al. Nat Commun. 2024 Aug 1;15(1):6498. doi: 10.1038/s41467-024-50548-x. Nat Commun. 2024. PMID: 39090128 Free PMC article.

26

Co-stimulation of muscarinic M1 and M4 acetylcholine receptors prevents later cocaine reinforcement in male and female mice, but not place-conditioning.

Balakrishnan AS, Johansen LBE, Lindsley CW, Conn PJ, Thomsen M. Balakrishnan AS, et al. Prog Neuropsychopharmacol Biol Psychiatry. 2024 Aug 30;134:111079. doi: 10.1016/j.pnpbp.2024.111079. Epub 2024 Jun 29. Prog Neuropsychopharmacol Biol Psychiatry. 2024. PMID: 38950842 Free article.

27

Potentiation of the muscarinic acetylcholine receptor 1 modulates neurophysiological features in a mouse model of Rett syndrome.

Dong HW, Weiss K, Baugh K, Meadows MJ, Niswender CM, Neul JL. Dong HW, et al. Neurotherapeutics. 2024 Jul;21(4):e00384. doi: 10.1016/j.neurot.2024.e00384. Epub 2024 Jun 15. Neurotherapeutics. 2024. PMID: 38880672 Free PMC article.

28

MeCP2 gene therapy ameliorates disease phenotype in mouse model for Pitt Hopkins syndrome.

Dennys CN, Vermudez SAD, Deacon RJM, Sierra-Delgado JA, Rich K, Zhang X, Buch A, Weiss K, Moxley Y, Rajpal H, Espinoza FD, Powers S, Ávila AS, Gogliotti RG, Cogram P, Niswender CM, Meyer KC. Dennys CN, et al. Neurotherapeutics. 2024 Sep;21(5):e00376. doi: 10.1016/j.neurot.2024.e00376. Epub 2024 Jun 14. Neurotherapeutics. 2024. PMID: 38876822 Free PMC article.

29

Computer-Aided Design and Biological Evaluation of Diazaspirocyclic D₄R Antagonists.

Jones CAH, Brown BP, Schultz DC, Engers J, Kramlinger VM, Meiler J, Lindsley CW. Jones CAH, et al. ACS Chem Neurosci. 2024 Jun 19;15(12):2396-2407. doi: 10.1021/acschemneuro.4c00086. Epub 2024 Jun 7. ACS Chem Neurosci. 2024. PMID: 38847395 Free PMC article.

30

Discovery of Protease-Activated Receptor 4 (PAR4)-Tethered Ligand Antagonists Using Ultralarge Virtual Screening.

Smith ST, Cassada JB, Von Bredow L, Erreger K, Webb EM, Trombley TA, Kalbfleisch JJ, Bender BJ, Zagol-Ikapitte I, Kramlinger VM, Bouchard JL, Mitchell SG, Tretbar M, Shoichet BK, Lindsley CW, Meiler J, Hamm HE. Smith ST, et al. ACS Pharmacol Transl Sci. 2024 Mar 21;7(4):1086-1100. doi: 10.1021/acsptsci.3c00378. eCollection 2024 Apr 12. ACS Pharmacol Transl Sci. 2024. PMID: 38633591 Free PMC article.

31

Novel pharmacological targets for GABAergic dysfunction in ADHD.

Ferranti AS, Luessen DJ, Niswender CM. Ferranti AS, et al. Neuropharmacology. 2024 May 15;249:109897. doi: 10.1016/j.neuropharm.2024.109897. Epub 2024 Mar 8. Neuropharmacology. 2024. PMID: 38462041 Free article. Review.

32

Therapeutic Potential for Metabotropic Glutamate Receptor 7 Modulators in Cognitive Disorders.

Parent HH, Niswender CM. Parent HH, et al. Mol Pharmacol. 2024 Apr 17;105(5):348-358. doi: 10.1124/molpharm.124.000874. Mol Pharmacol. 2024. PMID: 38423750 Review.

33

Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.

Jayakodiarachchi N, Maurer MA, Schultz DC, Dodd CJ, Thompson Gray A, Cho HP, Boutaud O, Jones CK, Lindsley CW, Bender AM. Jayakodiarachchi N, et al. ACS Med Chem Lett. 2024 Jan 19;15(2):302-309. doi: 10.1021/acsmedchemlett.3c00566. eCollection 2024 Feb 8. ACS Med Chem Lett. 2024. PMID: 38352850 Free PMC article.

34

Rapid sp³-Enriched Scaffold Generation via a Selective Aziridine Amide Ring-Opening Reaction.

Abe M, Coleman JS, Presley CC, Schley ND, Lindsley CW. Abe M, et al. J Org Chem. 2024 Mar 1;89(5):3500-3508. doi: 10.1021/acs.joc.3c02952. Epub 2024 Feb 10. J Org Chem. 2024. PMID: 38340064 Free PMC article.

35

Development of a Peripherally Restricted 5-HT_2B Partial Agonist for Treatment of Pulmonary Arterial Hypertension.

Valentine MS, Bender AM, Shay S, Paffenroth KC, Gladson S, Dickerson JW, Watson KJ, Kapolka NJ, Boutaud O, Rook JM, Blackwell TS, Roth BL, Harrison FE, Austin ED, West JD, Lindsley CW, Merryman WD. Valentine MS, et al. JACC Basic Transl Sci. 2023 Sep 13;8(10):1379-1388. doi: 10.1016/j.jacbts.2023.06.014. eCollection 2023 Oct. JACC Basic Transl Sci. 2023. PMID: 38094686 Free PMC article.

36

Activation of Metabotropic Glutamate Receptor 3 Modulates Thalamo-accumbal Transmission and Rescues Schizophrenia-Like Physiological and Behavioral Deficits.

Dogra S, Aguayo C, Xiang Z, Putnam J, Smith J, Johnston C, Foster DJ, Lindsley CW, Niswender CM, Conn PJ. Dogra S, et al. Biol Psychiatry. 2024 Aug 1;96(3):230-242. doi: 10.1016/j.biopsych.2023.11.023. Epub 2023 Dec 5. Biol Psychiatry. 2024. PMID: 38061467

37

Development of a Selective and High Affinity Radioligand, [³H]VU6013720, for the M₄ Muscarinic Receptor.

Qi A, Kling HE, Billard N, Rodriguez AL, Peng L, Dickerson JW, Engers JL, Bender AM, Moehle MS, Lindsley CW, Rook JM, Niswender CM. Qi A, et al. Mol Pharmacol. 2023 Nov;104(5):195-202. doi: 10.1124/molpharm.122.000643. Epub 2023 Aug 18. Mol Pharmacol. 2023. PMID: 37595966 Free PMC article.

38

2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery.

Bender AM, Parr LC, Livingston WB, Lindsley CW, Merryman WD. Bender AM, et al. J Med Chem. 2023 Aug 24;66(16):11027-11039. doi: 10.1021/acs.jmedchem.3c01178. Epub 2023 Aug 16. J Med Chem. 2023. PMID: 37584406 Free PMC article. Review.

39

Targeting the Actions of Muscarinic Receptors on Dopamine Systems: New Strategies for Treating Neuropsychiatric Disorders.

Nunes EJ, Addy NA, Conn PJ, Foster DJ. Nunes EJ, et al. Annu Rev Pharmacol Toxicol. 2024 Jan 23;64:277-289. doi: 10.1146/annurev-pharmtox-051921-023858. Epub 2023 Aug 9. Annu Rev Pharmacol Toxicol. 2024. PMID: 37552895 Free PMC article. Review.

40

Trofinetide: a pioneering treatment for Rett syndrome.

Parent H, Ferranti A, Niswender C. Parent H, et al. Trends Pharmacol Sci. 2023 Oct;44(10):740-741. doi: 10.1016/j.tips.2023.06.008. Epub 2023 Jul 16. Trends Pharmacol Sci. 2023. PMID: 37460385 Free PMC article.

41

Alkylation of NH-sulfoximines under Mitsunobu-type conditions.

Dodd CJ, Schultz DC, Li J, Lindsley CW, Bender AM. Dodd CJ, et al. Org Biomol Chem. 2023 Jun 28;21(25):5181-5184. doi: 10.1039/d3ob00810j. Org Biomol Chem. 2023. PMID: 37293894

42

Hypusination Maintains Intestinal Homeostasis and Prevents Colitis and Carcinogenesis by Enhancing Aldehyde Detoxification.

Gobert AP, Smith TM, Latour YL, Asim M, Barry DP, Allaman MM, Williams KJ, McNamara KM, Delgado AG, Short SP, Mirmira RG, Rose KL, Schey KL, Zagol-Ikapitte I, Coleman JS, Boutaud O, Zhao S, Piazuelo MB, Washington MK, Coburn LA, Wilson KT. Gobert AP, et al. Gastroenterology. 2023 Sep;165(3):656-669.e8. doi: 10.1053/j.gastro.2023.05.041. Epub 2023 Jun 2. Gastroenterology. 2023. PMID: 37271289 Free PMC article.

43

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics.

Vuckovic Z, Wang J, Pham V, Mobbs JI, Belousoff MJ, Bhattarai A, Burger WAC, Thompson G, Yeasmin M, Nawaratne V, Leach K, van der Westhuizen ET, Khajehali E, Liang YL, Glukhova A, Wootten D, Lindsley CW, Tobin A, Sexton P, Danev R, Valant C, Miao Y, Christopoulos A, Thal DM. Vuckovic Z, et al. Elife. 2023 May 30;12:e83477. doi: 10.7554/eLife.83477. Elife. 2023. PMID: 37248726 Free PMC article.

44

GPCR interactions involving metabotropic glutamate receptors and their relevance to the pathophysiology and treatment of CNS disorders.

Nicoletti F, Di Menna L, Iacovelli L, Orlando R, Zuena AR, Conn PJ, Dogra S, Joffe ME. Nicoletti F, et al. Neuropharmacology. 2023 Sep 1;235:109569. doi: 10.1016/j.neuropharm.2023.109569. Epub 2023 May 2. Neuropharmacology. 2023. PMID: 37142158 Review.

45

Differential Activity of Orthosteric Agonists and Allosteric Modulators at Metabotropic Glutamate Receptor 7.

Lei X, Hofmann CS, Rodriguez AL, Niswender CM. Lei X, et al. Mol Pharmacol. 2023 Jul;104(1):17-27. doi: 10.1124/molpharm.123.000678. Epub 2023 Apr 27. Mol Pharmacol. 2023. PMID: 37105671 Free PMC article.

46

M₁-selective muscarinic allosteric modulation enhances cognitive flexibility and effective salience in nonhuman primates.

Hassani SA, Neumann A, Russell J, Jones CK, Womelsdorf T. Hassani SA, et al. Proc Natl Acad Sci U S A. 2023 May 2;120(18):e2216792120. doi: 10.1073/pnas.2216792120. Epub 2023 Apr 27. Proc Natl Acad Sci U S A. 2023. PMID: 37104474 Free PMC article.

47

GRM7 gene mutations and consequences for neurodevelopment.

Freitas GA, Niswender CM. Freitas GA, et al. Pharmacol Biochem Behav. 2023 Apr;225:173546. doi: 10.1016/j.pbb.2023.173546. Epub 2023 Mar 30. Pharmacol Biochem Behav. 2023. PMID: 37003303 Free PMC article. Review.

48

Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.

Dodd CJ, Chronister KS, Rathnayake U, Parr LC, Li K, Chang S, Mi D, Days EL, Bauer JA, Cho HP, Boutaud O, Denton JS, Lindsley CW, Han C. Dodd CJ, et al. Bioorg Med Chem Lett. 2023 May 1;87:129256. doi: 10.1016/j.bmcl.2023.129256. Epub 2023 Mar 24. Bioorg Med Chem Lett. 2023. PMID: 36966977 Free PMC article.

49

Identification of Potent, Selective, and Peripherally Restricted Serotonin Receptor 2B Antagonists from a High-Throughput Screen.

Bender AM, Valentine MS, Bauer JA, Days E, Lindsley CW, Merryman WD. Bender AM, et al. Assay Drug Dev Technol. 2023 Apr;21(3):89-96. doi: 10.1089/adt.2022.116. Epub 2023 Mar 17. Assay Drug Dev Technol. 2023. PMID: 36930852 Free PMC article.

50

The Evolving Role of Animal Models in the Discovery and Development of Novel Treatments for Psychiatric Disorders.

Teal LB, Ingram SM, Bubser M, McClure E, Jones CK. Teal LB, et al. Adv Neurobiol. 2023;30:37-99. doi: 10.1007/978-3-031-21054-9_3. Adv Neurobiol. 2023. PMID: 36928846

51

Selective M₅ muscarinic acetylcholine receptor negative allosteric modulator VU6008667 blocks acquisition of opioid self-administration.

Teal LB, Bubser M, Duncan E, Gould RW, Lindsley CW, Jones CK. Teal LB, et al. Neuropharmacology. 2023 Apr 1;227:109424. doi: 10.1016/j.neuropharm.2023.109424. Epub 2023 Jan 28. Neuropharmacology. 2023. PMID: 36720403 Free article.

52

M₁/M₄-Preferring Muscarinic Cholinergic Receptor Agonist Xanomeline Reverses Wake and Arousal Deficits in Nonpathologically Aged Mice.

Russell JK, Ingram SM, Teal LB, Lindsley CW, Jones CK. Russell JK, et al. ACS Chem Neurosci. 2023 Feb 1;14(3):435-457. doi: 10.1021/acschemneuro.2c00592. Epub 2023 Jan 19. ACS Chem Neurosci. 2023. PMID: 36655909 Free PMC article.

53

DARK Classics in Chemical Neuroscience: Methaqualone.

Inger JA, Mihan ER, Kolli JU, Lindsley CW, Bender AM. Inger JA, et al. ACS Chem Neurosci. 2023 Feb 1;14(3):340-350. doi: 10.1021/acschemneuro.2c00697. Epub 2023 Jan 18. ACS Chem Neurosci. 2023. PMID: 36651763 Review.

54

On the Recent Changes to Animal Protection Measures in United States Food and Drug Administration Policy.

Melancon BJ. Melancon BJ. Assay Drug Dev Technol. 2023 Jan;21(1):1-2. doi: 10.1089/adt.2023.29103.bjm. Assay Drug Dev Technol. 2023. PMID: 36649598 No abstract available.

55

Persistent challenges in the development of an mGlu₇ PAM in vivo tool compound: The discovery of VU6046980.

Kalbfleisch JJ, Rodriguez AL, Lei X, Weiss K, Blobaum AL, Boutaud O, Niswender CM, Lindsley CW. Kalbfleisch JJ, et al. Bioorg Med Chem Lett. 2023 Jan 15;80:129106. doi: 10.1016/j.bmcl.2022.129106. Epub 2022 Dec 15. Bioorg Med Chem Lett. 2023. PMID: 36528230 Free PMC article.

56

Metabotropic glutamate receptor 3 as a potential therapeutic target for psychiatric and neurological disorders.

Dogra S, Putnam J, Conn PJ. Dogra S, et al. Pharmacol Biochem Behav. 2022 Nov;221:173493. doi: 10.1016/j.pbb.2022.173493. Epub 2022 Nov 17. Pharmacol Biochem Behav. 2022. PMID: 36402243 Free PMC article. Review.

57

Editor's Response to a Letter on "3D Printing Has an Imperative Role in Colitis Management" by Sahoo and Singh.

Melancon BJ. Melancon BJ. Assay Drug Dev Technol. 2022 Oct;20(7):298-299. doi: 10.1089/adt.2022.29101.bjm. Epub 2022 Oct 11. Assay Drug Dev Technol. 2022. PMID: 36269232 No abstract available.

58

Discovery of a potent M₅ antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists.

Orsi DL, Felts AS, Rodriguez AL, Vinson PN, Cho HP, Chang S, Blobaum AL, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Orsi DL, et al. Bioorg Med Chem Lett. 2022 Dec 15;78:129021. doi: 10.1016/j.bmcl.2022.129021. Epub 2022 Oct 10. Bioorg Med Chem Lett. 2022. PMID: 36228968 Free PMC article.

59

Discovery of a potent M₅ antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists.

Capstick RA, Whomble D, Orsi DL, Felts AS, Rodriguez AL, Vinson PN, Chang S, Blobaum AL, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C. Capstick RA, et al. Bioorg Med Chem Lett. 2022 Nov 15;76:128988. doi: 10.1016/j.bmcl.2022.128988. Epub 2022 Sep 14. Bioorg Med Chem Lett. 2022. PMID: 36113671 Free PMC article.

60

Differential activity of mGlu₇ allosteric modulators provides evidence for mGlu_7/8 heterodimers at hippocampal Schaffer collateral-CA1 synapses.

Lin X, Fisher NM, Dogra S, Senter RK, Reed CW, Kalbfleisch JJ, Lindsley CW, Asher WB, Xiang Z, Niswender CM, Javitch JA. Lin X, et al. J Biol Chem. 2022 Oct;298(10):102458. doi: 10.1016/j.jbc.2022.102458. Epub 2022 Sep 5. J Biol Chem. 2022. PMID: 36063995 Free PMC article.

61

Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits.

Ferranti AS, Foster DJ. Ferranti AS, et al. Front Neurosci. 2022 Aug 11;16:925792. doi: 10.3389/fnins.2022.925792. eCollection 2022. Front Neurosci. 2022. PMID: 36033626 Free PMC article. Review.

62

Development and profiling of mGlu₇ NAMs with a range of saturable inhibition of agonist responses in vitro.

Reed CW, Rodriguez AL, Kalbfleisch JJ, Seto M, Jenkins MT, Blobaum AL, Chang S, Lindsley CW, Niswender CM. Reed CW, et al. Bioorg Med Chem Lett. 2022 Oct 15;74:128923. doi: 10.1016/j.bmcl.2022.128923. Epub 2022 Aug 6. Bioorg Med Chem Lett. 2022. PMID: 35944850 Free PMC article.

63

Optimized Administration of the M₄ PAM VU0467154 Demonstrates Broad Efficacy, but Limited Effective Concentrations in Mecp2^+/- Mice.

Cikowski J, Holt C, Arthur B, Smith M, Gonzalez S, Lindsley CW, Niswender CM, Gogliotti RG. Cikowski J, et al. ACS Chem Neurosci. 2022 Jul 6;13(13):1891-1901. doi: 10.1021/acschemneuro.2c00113. Epub 2022 Jun 7. ACS Chem Neurosci. 2022. PMID: 35671352 Free PMC article.

64

Clinical and Preclinical Evidence for M₁ Muscarinic Acetylcholine Receptor Potentiation as a Therapeutic Approach for Rett Syndrome.

Smith M, Arthur B, Cikowski J, Holt C, Gonzalez S, Fisher NM, Vermudez SAD, Lindsley CW, Niswender CM, Gogliotti RG. Smith M, et al. Neurotherapeutics. 2022 Jul;19(4):1340-1352. doi: 10.1007/s13311-022-01254-3. Epub 2022 Jun 7. Neurotherapeutics. 2022. PMID: 35670902 Free PMC article.

65

mGlu₁-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice.

Luessen DJ, Gallinger IM, Ferranti AS, Foster DJ, Melancon BJ, Lindsley CW, Niswender CM, Conn PJ. Luessen DJ, et al. Neuropsychopharmacology. 2022 Sep;47(10):1826-1835. doi: 10.1038/s41386-022-01350-0. Epub 2022 May 28. Neuropsychopharmacology. 2022. PMID: 35643819 Free PMC article.

66

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M₅ Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Garrison AT, Orsi DL, Capstick RA, Whomble D, Li J, Carter TR, Felts AS, Vinson PN, Rodriguez AL, Han A, Hajari K, Cho HP, Teal LB, Ragland MG, Ghamari-Langroudi M, Bubser M, Chang S, Schnetz-Boutaud NC, Boutaud O, Blobaum AL, Foster DJ, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Han C. Garrison AT, et al. J Med Chem. 2022 Apr 28;65(8):6273-6286. doi: 10.1021/acs.jmedchem.2c00192. Epub 2022 Apr 13. J Med Chem. 2022. PMID: 35417155

67

Sulforaphane reduces obesity by reversing leptin resistance.

Çakır I, Lining Pan P, Hadley CK, El-Gamal A, Fadel A, Elsayegh D, Mohamed O, Rizk NM, Ghamari-Langroudi M. Çakır I, et al. Elife. 2022 Mar 24;11:e67368. doi: 10.7554/eLife.67368. Elife. 2022. PMID: 35323110 Free PMC article.

68

Exploration of group II metabotropic glutamate receptor modulation in mouse models of Rett syndrome and MECP2 Duplication syndrome.

Vermudez SAD, Buch A, Weiss K, Gogliotti RG, Niswender CM. Vermudez SAD, et al. Neuropharmacology. 2022 May 15;209:109022. doi: 10.1016/j.neuropharm.2022.109022. Epub 2022 Mar 3. Neuropharmacology. 2022. PMID: 35248529 Free PMC article.

69

Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia.

Dogra S, Conn PJ. Dogra S, et al. Mol Pharmacol. 2022 May;101(5):275-285. doi: 10.1124/molpharm.121.000460. Epub 2022 Mar 3. Mol Pharmacol. 2022. PMID: 35246479 Free PMC article. Review.

70

Prefrontal cortex parvalbumin interneurons exhibit decreased excitability and potentiated synaptic strength after ethanol reward learning.

Ferranti AS, Johnson KA, Winder DG, Conn PJ, Joffe ME. Ferranti AS, et al. Alcohol. 2022 Jun;101:17-26. doi: 10.1016/j.alcohol.2022.02.003. Epub 2022 Feb 26. Alcohol. 2022. PMID: 35227826 Free PMC article.

71

Muscarinic receptors: from clinic to bench to clinic.

Foster DJ. Foster DJ. Trends Pharmacol Sci. 2022 Jun;43(6):461-463. doi: 10.1016/j.tips.2022.01.006. Epub 2022 Jan 31. Trends Pharmacol Sci. 2022. PMID: 35101279 Free PMC article.

72

Acute restraint stress redirects prefrontal cortex circuit function through mGlu₅ receptor plasticity on somatostatin-expressing interneurons.

Joffe ME, Maksymetz J, Luschinger JR, Dogra S, Ferranti AS, Luessen DJ, Gallinger IM, Xiang Z, Branthwaite H, Melugin PR, Williford KM, Centanni SW, Shields BC, Lindsley CW, Calipari ES, Siciliano CA, Niswender CM, Tadross MR, Winder DG, Conn PJ. Joffe ME, et al. Neuron. 2022 Mar 16;110(6):1068-1083.e5. doi: 10.1016/j.neuron.2021.12.027. Epub 2022 Jan 18. Neuron. 2022. PMID: 35045338 Free PMC article.

73

Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity.

Çakır I, Hadley CK, Pan PL, Bagchi RA, Ghamari-Langroudi M, Porter DT, Wang Q, Litt MJ, Jana S, Hagen S, Lee P, White A, Lin JD, McKinsey TA, Cone RD. Çakır I, et al. Nat Metab. 2022 Jan;4(1):44-59. doi: 10.1038/s42255-021-00515-3. Epub 2022 Jan 17. Nat Metab. 2022. PMID: 35039672 Free PMC article.

74

The effects of predator odor (TMT) exposure and mGlu₃ NAM pretreatment on behavioral and NMDA receptor adaptations in the brain.

Tyler RE, Bluitt MN, Engers JL, Lindsley CW, Besheer J. Tyler RE, et al. Neuropharmacology. 2022 Apr 1;207:108943. doi: 10.1016/j.neuropharm.2022.108943. Epub 2022 Jan 7. Neuropharmacology. 2022. PMID: 35007623 Free PMC article.

75

Discovery and Optimization of a Novel Series of Competitive and Central Nervous System-Penetrant Protease-Activated Receptor 4 (PAR4) Inhibitors.

Bertron JL, Duvernay MT, Mitchell SG, Smith ST, Maeng JG, Blobaum AL, Davis DC, Meiler J, Hamm HE, Lindsley CW. Bertron JL, et al. ACS Chem Neurosci. 2021 Dec 15;12(24):4524-4534. doi: 10.1021/acschemneuro.1c00557. Epub 2021 Dec 2. ACS Chem Neurosci. 2021. PMID: 34855359 Free PMC article.

76

Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M₄ muscarinic acetylcholine receptor.

Bender AM, Carter TR, Spock M, Rodriguez AL, Dickerson JW, Rook JM, Chang S, Qi A, Presley CC, Engers DW, Harp JM, Bridges TM, Niswender CM, Conn PJ, Lindsley CW. Bender AM, et al. Bioorg Med Chem Lett. 2022 Jan 15;56:128479. doi: 10.1016/j.bmcl.2021.128479. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838649

77

Intravitreal HDAC Inhibitor Belinostat Effectively Eradicates Vitreous Seeds Without Retinal Toxicity In Vivo in a Rabbit Retinoblastoma Model.

Kaczmarek JV, Bogan CM, Pierce JM, Tao YK, Chen SC, Liu Q, Liu X, Boyd KL, Calcutt MW, Bridges TM, Lindsley CW, Friedman DL, Richmond A, Daniels AB. Kaczmarek JV, et al. Invest Ophthalmol Vis Sci. 2021 Nov 1;62(14):8. doi: 10.1167/iovs.62.14.8. Invest Ophthalmol Vis Sci. 2021. PMID: 34757417 Free PMC article.

78

mGlu₁ potentiation enhances prelimbic somatostatin interneuron activity to rescue schizophrenia-like physiological and cognitive deficits.

Maksymetz J, Byun NE, Luessen DJ, Li B, Barry RL, Gore JC, Niswender CM, Lindsley CW, Joffe ME, Conn PJ. Maksymetz J, et al. Cell Rep. 2021 Nov 2;37(5):109950. doi: 10.1016/j.celrep.2021.109950. Cell Rep. 2021. PMID: 34731619 Free PMC article.

79

Discovery of structurally distinct tricyclic M₄ positive allosteric modulator (PAM) chemotypes - Part 2.

Long MF, Capstick RA, Spearing PK, Engers JL, Gregro AR, Bollinger SR, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Lindsley CW, Engers DW, Temple KJ. Long MF, et al. Bioorg Med Chem Lett. 2021 Dec 1;53:128416. doi: 10.1016/j.bmcl.2021.128416. Epub 2021 Oct 26. Bioorg Med Chem Lett. 2021. PMID: 34710625 Free PMC article.

80

Endogenous cannabinoids are required for MC4R-mediated control of energy homeostasis.

Yong Y, Cakir I, Lining Pan P, Biddinger JE, Bluett RJ, Mackie K, Bingham N, Patel S, Ghamari-Langroudi M. Yong Y, et al. Proc Natl Acad Sci U S A. 2021 Oct 19;118(42):e2015990118. doi: 10.1073/pnas.2015990118. Proc Natl Acad Sci U S A. 2021. PMID: 34654741 Free PMC article.

81

Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.

Yamada Y, Gilliland K, Xiang Z, Haymer D, Crocker KE, Loch MT, Schulte ML, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Melancon BJ. Yamada Y, et al. Bioorg Med Chem Lett. 2021 Oct 15;50:128342. doi: 10.1016/j.bmcl.2021.128342. Epub 2021 Aug 27. Bioorg Med Chem Lett. 2021. PMID: 34461178

82

Discovery of the First Selective M₄ Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

Moehle MS, Bender AM, Dickerson JW, Foster DJ, Qi A, Cho HP, Donsante Y, Peng W, Bryant Z, Stillwell KJ, Bridges TM, Chang S, Watson KJ, O'Neill JC, Engers JL, Peng L, Rodriguez AL, Niswender CM, Lindsley CW, Hess EJ, Conn PJ, Rook JM. Moehle MS, et al. ACS Pharmacol Transl Sci. 2021 Aug 2;4(4):1306-1321. doi: 10.1021/acsptsci.0c00162. eCollection 2021 Aug 13. ACS Pharmacol Transl Sci. 2021. PMID: 34423268 Free PMC article.

83

Modeling intrahippocampal effects of anterior hippocampal hyperactivity relevant to schizophrenia using chemogenetic excitation of long axis-projecting mossy cells in the mouse dentate gyrus.

Bauer JP, Rader SL, Joffe ME, Kwon W, Quay J, Seanez L, Zhou C, Conn PJ, Lewis AS. Bauer JP, et al. Biol Psychiatry Glob Open Sci. 2021 Aug;1(2):101-111. doi: 10.1016/j.bpsgos.2021.04.005. Epub 2021 May 4. Biol Psychiatry Glob Open Sci. 2021. PMID: 34414387 Free PMC article.

84

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M₄ Muscarinic Acetylcholine Receptor Antagonist.

Spock M, Carter TR, Bollinger KA, Han C, Baker LA, Rodriguez AL, Peng L, Dickerson JW, Qi A, Rook JM, O'Neill JC, Watson KJ, Chang S, Bridges TM, Engers JL, Engers DW, Niswender CM, Conn PJ, Lindsley CW, Bender AM. Spock M, et al. ACS Med Chem Lett. 2021 Aug 2;12(8):1342-1349. doi: 10.1021/acsmedchemlett.1c00363. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413964 Free PMC article.

85

Discovery of "Molecular Switches" within a Series of mGlu₅ Allosteric Ligands Driven by a "Magic Methyl" Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M₁ PAM Chemotype.

Barbaro L, Rodriguez AL, Blevins AN, Dickerson JW, Billard N, Boutaud O, Rook JL, Niswender CM, Conn PJ, Engers DW, Lindsley CW. Barbaro L, et al. ACS Bio Med Chem Au. 2021 Aug 20;1(1):21-30. doi: 10.1021/acsbiomedchemau.1c00024. eCollection 2021 Dec 15. ACS Bio Med Chem Au. 2021. PMID: 37101980 Free PMC article.

86

Identification of a Novel Allosteric Site at the M₅ Muscarinic Acetylcholine Receptor.

Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ, Tobin AB, Christopoulos A, Valant C, Thal DM. Burger WAC, et al. ACS Chem Neurosci. 2021 Aug 18;12(16):3112-3123. doi: 10.1021/acschemneuro.1c00383. Epub 2021 Aug 5. ACS Chem Neurosci. 2021. PMID: 34351123 Free PMC article.

87

DARK Classics in Chemical Neuroscience: Loperamide.

Malinky CA, Lindsley CW, Han C. Malinky CA, et al. ACS Chem Neurosci. 2021 Aug 18;12(16):2964-2973. doi: 10.1021/acschemneuro.1c00382. Epub 2021 Aug 4. ACS Chem Neurosci. 2021. PMID: 34346690 Review.

88

Developing breakthrough psychiatric treatments by modulating G protein-coupled receptors on prefrontal cortex somatostatin interneurons.

Crowley NA, Joffe ME. Crowley NA, et al. Neuropsychopharmacology. 2022 Jan;47(1):389-390. doi: 10.1038/s41386-021-01119-x. Neuropsychopharmacology. 2022. PMID: 34341496 Free PMC article. No abstract available.

89

Partial mGlu₅ Negative Allosteric Modulator M-5MPEP Demonstrates Antidepressant-Like Effects on Sleep Without Affecting Cognition or Quantitative EEG.

Holter KM, Lekander AD, LaValley CM, Bedingham EG, Pierce BE, Sands LP 3rd, Lindsley CW, Jones CK, Gould RW. Holter KM, et al. Front Neurosci. 2021 Jul 2;15:700822. doi: 10.3389/fnins.2021.700822. eCollection 2021. Front Neurosci. 2021. PMID: 34276300 Free PMC article.

90

Regulation and functional consequences of mGlu₄ RNA editing.

Hofmann CS, Carrington S, Keller AN, Gregory KJ, Niswender CM. Hofmann CS, et al. RNA. 2021 Oct;27(10):1220-1240. doi: 10.1261/rna.078729.121. Epub 2021 Jul 8. RNA. 2021. PMID: 34244459 Free PMC article.

91

Targeting metabotropic glutamate receptors for the treatment of depression and other stress-related disorders.

Dogra S, Conn PJ. Dogra S, et al. Neuropharmacology. 2021 Sep 15;196:108687. doi: 10.1016/j.neuropharm.2021.108687. Epub 2021 Jun 25. Neuropharmacology. 2021. PMID: 34175327 Free PMC article. Review.

92

Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M₁.

Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Spearing PK, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128193. doi: 10.1016/j.bmcl.2021.128193. Epub 2021 Jun 9. Bioorg Med Chem Lett. 2021. PMID: 34118412 Free PMC article.

93

Frontal cortex genetic ablation of metabotropic glutamate receptor subtype 3 (mGlu₃) impairs postsynaptic plasticity and modulates affective behaviors.

Joffe ME, Santiago CI, Vermudez SAD, Fisher NM, Dogra S, Niswender CM, Jeffrey Conn P. Joffe ME, et al. Neuropsychopharmacology. 2021 Nov;46(12):2148-2157. doi: 10.1038/s41386-021-01041-2. Epub 2021 May 25. Neuropsychopharmacology. 2021. PMID: 34035469 Free PMC article.

94

Profiling beneficial and potential adverse effects of MeCP2 overexpression in a hypomorphic Rett syndrome mouse model.

Vermudez SAD, Gogliotti RG, Arthur B, Buch A, Morales C, Moxley Y, Rajpal H, Conn PJ, Niswender CM. Vermudez SAD, et al. Genes Brain Behav. 2022 Jan;21(1):e12752. doi: 10.1111/gbb.12752. Epub 2021 May 28. Genes Brain Behav. 2022. PMID: 34002468 Free PMC article.

95

Activating mGlu₃ Metabotropic Glutamate Receptors Rescues Schizophrenia-like Cognitive Deficits Through Metaplastic Adaptations Within the Hippocampus.

Dogra S, Stansley BJ, Xiang Z, Qian W, Gogliotti RG, Nicoletti F, Lindsley CW, Niswender CM, Joffe ME, Conn PJ. Dogra S, et al. Biol Psychiatry. 2021 Sep 15;90(6):385-398. doi: 10.1016/j.biopsych.2021.02.970. Epub 2021 Mar 6. Biol Psychiatry. 2021. PMID: 33965197 Free PMC article.

96

Muscarinic M₄ and M₅ receptors in the ventral subiculum differentially modulate alcohol seeking versus consumption in male alcohol-preferring rats.

Walker LC, Huckstep KL, Chen NA, Hand LJ, Lindsley CW, Langmead CJ, Lawrence AJ. Walker LC, et al. Br J Pharmacol. 2021 Sep;178(18):3730-3746. doi: 10.1111/bph.15513. Epub 2021 Jun 3. Br J Pharmacol. 2021. PMID: 33942300 Free article.

97

Ten-Year Retrospective of the Vanderbilt Institute of Chemical Biology Chemical Synthesis Core.

Kim K, Christov PP, Romaine I, Tian J, Jana S, Lamers AP, Dutter BF, Scaggs T, Jeon K, Guttentag B, Weaver CD, Lindsley CW, Waterson AG, Sulikowski GA. Kim K, et al. ACS Chem Biol. 2021 May 21;16(5):787-793. doi: 10.1021/acschembio.0c00818. Epub 2021 Apr 20. ACS Chem Biol. 2021. PMID: 33877812 Review.

98

Input-specific regulation of glutamatergic synaptic transmission in the medial prefrontal cortex by mGlu₂/mGlu₄ receptor heterodimers.

Xiang Z, Lv X, Lin X, O'Brien DE, Altman MK, Lindsley CW, Javitch JA, Niswender CM, Conn PJ. Xiang Z, et al. Sci Signal. 2021 Apr 6;14(677):eabd2319. doi: 10.1126/scisignal.abd2319. Sci Signal. 2021. PMID: 33824180 Free PMC article.

99

Targeting muscarinic receptors to treat schizophrenia.

Foster DJ, Bryant ZK, Conn PJ. Foster DJ, et al. Behav Brain Res. 2021 May 7;405:113201. doi: 10.1016/j.bbr.2021.113201. Epub 2021 Feb 26. Behav Brain Res. 2021. PMID: 33647377 Free PMC article. Review.

100

Discovery and optimization of a novel CNS penetrant series of mGlu₄ PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model.

Kent CN, Fulton MG, Stillwell KJ, Dickerson JW, Loch MT, Rodriguez AL, Blobaum AL, Boutaud O, Rook JL, Niswender CM, Conn PJ, Lindsley CW. Kent CN, et al. Bioorg Med Chem Lett. 2021 Apr 1;37:127838. doi: 10.1016/j.bmcl.2021.127838. Epub 2021 Feb 5. Bioorg Med Chem Lett. 2021. PMID: 33556572

101

A GRM7 mutation associated with developmental delay reduces mGlu7 expression and produces neurological phenotypes.

Fisher NM, AlHashim A, Buch AB, Badivuku H, Samman MM, Weiss KM, Cestero GI, Does MD, Rook JM, Lindsley CW, Conn PJ, Gogliotti RG, Niswender CM. Fisher NM, et al. JCI Insight. 2021 Feb 22;6(4):e143324. doi: 10.1172/jci.insight.143324. JCI Insight. 2021. PMID: 33476302 Free PMC article.

102

Increased Synaptic Strength and mGlu_2/3 Receptor Plasticity on Mouse Prefrontal Cortex Intratelencephalic Pyramidal Cells Following Intermittent Access to Ethanol.

Joffe ME, Winder DG, Conn PJ. Joffe ME, et al. Alcohol Clin Exp Res. 2021 Mar;45(3):518-529. doi: 10.1111/acer.14546. Epub 2021 Feb 9. Alcohol Clin Exp Res. 2021. PMID: 33434325 Free PMC article.

103

Lead optimization of the VU0486321 series of mGlu₁ PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.

Davis DC, Bungard JD, Chang S, Rodriguez AL, Blobaum AL, Boutaud O, Melancon BJ, Niswender CM, Jeffrey Conn P, Lindsley CW. Davis DC, et al. Bioorg Med Chem Lett. 2021 Jan 15;32:127724. doi: 10.1016/j.bmcl.2020.127724. Epub 2020 Nov 27. Bioorg Med Chem Lett. 2021. PMID: 33253881

104

Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu₇ Positive Allosteric Modulator Tool Compound.

Reed CW, Kalbfleisch JJ, Wong MJ, Washecheck JP, Hunter A, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Reed CW, et al. ACS Med Chem Lett. 2020 Aug 20;11(9):1773-1779. doi: 10.1021/acsmedchemlett.0c00432. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944146 Free PMC article.

105

Synthesis and SAR of a series of mGlu₇ NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.

Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Kalbfleisch JJ, et al. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127529. doi: 10.1016/j.bmcl.2020.127529. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890686 Free PMC article.

106

Modulation of arousal and sleep/wake architecture by M₁ PAM VU0453595 across young and aged rodents and nonhuman primates.

Gould RW, Russell JK, Nedelcovych MT, Bubser M, Blobaum AL, Bridges TM, Newhouse PA, Lindsley CW, Conn PJ, Nader MA, Jones CK. Gould RW, et al. Neuropsychopharmacology. 2020 Dec;45(13):2219-2228. doi: 10.1038/s41386-020-00812-7. Epub 2020 Aug 31. Neuropsychopharmacology. 2020. PMID: 32868847 Free PMC article.

107

DARK Classics in Chemical Neuroscience: Carfentanil.

Ringuette AE, Spock M, Lindsley CW, Bender AM. Ringuette AE, et al. ACS Chem Neurosci. 2020 Dec 2;11(23):3955-3967. doi: 10.1021/acschemneuro.0c00441. Epub 2020 Aug 25. ACS Chem Neurosci. 2020. PMID: 32786301 Review.

108

Contrasting sex-dependent adaptations to synaptic physiology and membrane properties of prefrontal cortex interneuron subtypes in a mouse model of binge drinking.

Joffe ME, Winder DG, Conn PJ. Joffe ME, et al. Neuropharmacology. 2020 Nov 1;178:108126. doi: 10.1016/j.neuropharm.2020.108126. Epub 2020 Aug 8. Neuropharmacology. 2020. PMID: 32781000 Free PMC article.

109

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.

Engers DW, Bollinger SR, Felts AS, Vadukoot AK, Williams CH, Blobaum AL, Lindsley CW, Hong CC, Hopkins CR. Engers DW, et al. Bioorg Med Chem Lett. 2020 Sep 15;30(18):127418. doi: 10.1016/j.bmcl.2020.127418. Epub 2020 Jul 17. Bioorg Med Chem Lett. 2020. PMID: 32750526 Free PMC article.

110

DARK Classics in Chemical Neuroscience: U-47700.

Kyei-Baffour K, Lindsley CW. Kyei-Baffour K, et al. ACS Chem Neurosci. 2020 Dec 2;11(23):3928-3936. doi: 10.1021/acschemneuro.0c00330. Epub 2020 Jul 22. ACS Chem Neurosci. 2020. PMID: 32639714 Review.

111

Classics in Chemical Neuroscience: Baclofen.

Kent CN, Park C, Lindsley CW. Kent CN, et al. ACS Chem Neurosci. 2020 Jun 17;11(12):1740-1755. doi: 10.1021/acschemneuro.0c00254. Epub 2020 Jun 3. ACS Chem Neurosci. 2020. PMID: 32436697 Review.

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