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Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: gaskin p. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.
Demont EH, Andrews BI, Bit RA, Campbell CA, Cooke JW, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Haynes A, Holmes DS, Kumar U, Morse MA, Osborne GJ, Panchal T, Patel B, Perboni A, Taylor S, Watson R, Witherington J, Willis R. Demont EH, et al. Among authors: gaskin p. ACS Med Chem Lett. 2011 Mar 24;2(6):444-9. doi: 10.1021/ml2000214. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900328 Free PMC article.
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: gaskin p. J Med Chem. 2016 Feb 11;59(3):1003-20. doi: 10.1021/acs.jmedchem.5b01512. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751273
Correction to: Luvadaxistat: A Novel Potent and Selective D-Amino Acid Oxidase Inhibitor Improves Cognitive and Social Deficits in Rodent Models for Schizophrenia.
Fradley R, Goetghebeur P, Miller D, Burley R, Almond S, Gruart I Massó A, Delgado García JM, Zhu B, Howley E, Neill JC, Grayson B, Gaskin P, Carlton M, Gray I, Serrats J, Davies CH. Fradley R, et al. Among authors: gaskin p. Neurochem Res. 2023 Nov;48(11):3472. doi: 10.1007/s11064-023-03987-9. Neurochem Res. 2023. PMID: 37440119 Free PMC article. No abstract available.
Luvadaxistat: A Novel Potent and Selective D-Amino Acid Oxidase Inhibitor Improves Cognitive and Social Deficits in Rodent Models for Schizophrenia.
Fradley R, Goetghebeur P, Miller D, Burley R, Almond S, Gruart I Massó A, Delgado García JM, Zhu B, Howley E, Neill JC, Grayson B, Gaskin P, Carlton M, Gray I, Serrats J, Davies CH. Fradley R, et al. Among authors: gaskin p. Neurochem Res. 2023 Oct;48(10):3027-3041. doi: 10.1007/s11064-023-03956-2. Epub 2023 Jun 8. Neurochem Res. 2023. PMID: 37289348 Free PMC article.
Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia.
Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, Collia DR, Ray WJ, Serrats J, Bliesath J, Kaushal N, Lam BP, Amador-Arjona A, Rahbaek L, McConn DJ, Mulligan VJ, Brice N, Gaskin PLR, Cilia J, Hitchcock S. Reichard HA, et al. Among authors: gaskin plr. J Med Chem. 2021 Aug 12;64(15):11527-11542. doi: 10.1021/acs.jmedchem.1c00820. Epub 2021 Jul 14. J Med Chem. 2021. PMID: 34260228
121 results