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Page 1
Molecular determinants of ASIC1 modulation by divalent cations.
Liu Y, Ma J, DesJarlais RL, Hagan R, Rech J, Liu C, Miller R, Schoellerman J, Luo J, Letavic M, Grasberger B, Maher MP. Liu Y, et al. Among authors: letavic m. Sci Rep. 2024 Jan 28;14(1):2320. doi: 10.1038/s41598-024-52845-3. Sci Rep. 2024. PMID: 38282035 Free PMC article.
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A. Letavic MA, et al. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. doi: 10.1021/ml400040v. eCollection 2013 Apr 11. ACS Med Chem Lett. 2013. PMID: 24900687 Free PMC article.
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.
Rudolph DA, Alcazar J, Ameriks MK, Anton AB, Ao H, Bonaventure P, Carruthers NI, Chrovian CC, De Angelis M, Lord B, Rech JC, Wang Q, Bhattacharya A, Andres JI, Letavic MA. Rudolph DA, et al. Among authors: letavic ma. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3157-63. doi: 10.1016/j.bmcl.2015.06.004. Epub 2015 Jun 9. Bioorg Med Chem Lett. 2015. PMID: 26099534
The evolution of P2X7 antagonists with a focus on CNS indications.
Rech JC, Bhattacharya A, Letavic MA, Savall BM. Rech JC, et al. Among authors: letavic ma. Bioorg Med Chem Lett. 2016 Aug 15;26(16):3838-45. doi: 10.1016/j.bmcl.2016.06.048. Epub 2016 Jun 30. Bioorg Med Chem Lett. 2016. PMID: 27426304 Review.
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA. Swanson DM, et al. Among authors: letavic ma. J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8. J Med Chem. 2016. PMID: 27548392
1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.
Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: letavic ma. ACS Med Chem Lett. 2019 Jan 10;10(3):261-266. doi: 10.1021/acsmedchemlett.8b00542. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891123 Free PMC article.
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders.
Chrovian CC, Soyode-Johnson A, Stenne B, Pippel DJ, Schoellerman J, Lord B, Needham AS, Xia C, Coe KJ, Sepassi K, Schoetens F, Scott B, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA. Chrovian CC, et al. Among authors: letavic ma. J Med Chem. 2020 Sep 10;63(17):9181-9196. doi: 10.1021/acs.jmedchem.9b02113. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32787105
63 results