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Page 1
Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators.
Burley R, Hewer RC, Teall M, Dickson L, Ossola B, Russell S, Bender C, Cheung T, Powell JAC, Xu X, Brice NL, Otter L, Arimont M, Kidd SL, Vidal D, Dale JW, Mervin L, Sore HF, Mateu N, Lakshminarayana N, Dawson LA, Carlton M, Bürli RW. Burley R, et al. Among authors: brice nl. Bioorg Med Chem Lett. 2022 Apr 1;61:128607. doi: 10.1016/j.bmcl.2022.128607. Epub 2022 Feb 3. Bioorg Med Chem Lett. 2022. PMID: 35123006
Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease.
Brice NL, Schiffer HH, Monenschein H, Mulligan VJ, Page K, Powell J, Xu X, Cheung T, Burley JR, Sun H, Dickson L, Murphy ST, Kaushal N, Sheardown S, Lawrence J, Chen Y, Bartkowski D, Kanta A, Russo J, Hosea N, Dawson LA, Hitchcock SH, Carlton MB. Brice NL, et al. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. doi: 10.1124/jpet.120.000438. Epub 2021 Apr 1. J Pharmacol Exp Ther. 2021. PMID: 33795395
First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.
Sun H, Monenschein H, Schiffer HH, Reichard HA, Kikuchi S, Hopkins M, Macklin TK, Hitchcock S, Adams M, Green J, Brown J, Murphy ST, Kaushal N, Collia DR, Moore S, Ray WJ, English NM, Carlton MBL, Brice NL. Sun H, et al. Among authors: brice nl. J Med Chem. 2021 Jul 22;64(14):9875-9890. doi: 10.1021/acs.jmedchem.0c02081. Epub 2021 Apr 16. J Med Chem. 2021. PMID: 33861086
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. 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
A Phase I, First-in-Human, Healthy Volunteer Study to Investigate the Safety, Tolerability, and Pharmacokinetics of CVN424, a Novel G Protein-Coupled Receptor 6 Inverse Agonist for Parkinson's Disease.
Margolin DH, Brice NL, Davidson AM, Matthews KL, Carlton MBL. Margolin DH, et al. Among authors: brice nl. J Pharmacol Exp Ther. 2022 Apr;381(1):33-41. doi: 10.1124/jpet.121.000842. Epub 2022 Feb 2. J Pharmacol Exp Ther. 2022. PMID: 35110393 Clinical Trial.
Characterisation of C101248: A novel selective THIK-1 channel inhibitor for the modulation of microglial NLRP3-inflammasome.
Ossola B, Rifat A, Rowland A, Hunter H, Drinkall S, Bender C, Hamlischer M, Teall M, Burley R, Barker DF, Cadwalladr D, Dickson L, Lawrence JMK, Harvey JRM, Lizio M, Xu X, Kavanagh E, Cheung T, Sheardown S, Lawrence CB, Harte M, Brough D, Madry C, Matthews K, Doyle K, Page K, Powell J, Brice NL, Bürli RW, Carlton MB, Dawson LA. Ossola B, et al. Among authors: brice nl. Neuropharmacology. 2023 Feb 15;224:109330. doi: 10.1016/j.neuropharm.2022.109330. Epub 2022 Nov 12. Neuropharmacology. 2023. PMID: 36375694 Free PMC article.
Mismatch negativity as an index of target engagement for excitation/inhibition-based treatment development: a double-blind, placebo-controlled, randomized, single-dose cross-over study of the serotonin type-3 receptor antagonist CVN058.
Sehatpour P, Javitt DC, De Baun HM, Carlson M, Beloborodova A, Margolin DH, Carlton MBL, Brice NL, Kantrowitz JT. Sehatpour P, et al. Among authors: brice nl. Neuropsychopharmacology. 2022 Feb;47(3):711-718. doi: 10.1038/s41386-021-01170-8. Epub 2021 Oct 20. Neuropsychopharmacology. 2022. PMID: 34667294 Free PMC article. Clinical Trial.
SIPA1L2 controls trafficking and local signaling of TrkB-containing amphisomes at presynaptic terminals.
Andres-Alonso M, Ammar MR, Butnaru I, Gomes GM, Acuña Sanhueza G, Raman R, Yuanxiang P, Borgmeyer M, Lopez-Rojas J, Raza SA, Brice N, Hausrat TJ, Macharadze T, Diaz-Gonzalez S, Carlton M, Failla AV, Stork O, Schweizer M, Gundelfinger ED, Kneussel M, Spilker C, Karpova A, Kreutz MR. Andres-Alonso M, et al. Nat Commun. 2019 Nov 29;10(1):5448. doi: 10.1038/s41467-019-13224-z. Nat Commun. 2019. PMID: 31784514 Free PMC article.
29 results