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The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD. Gaster LM, et al. Among authors: wyman pa. J Med Chem. 1998 Apr 9;41(8):1218-35. doi: 10.1021/jm970457s. J Med Chem. 1998. PMID: 9548813
Identification of a potent and selective 5-HT1B receptor antagonist.
Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA. Wyman PA, et al. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4708-12. doi: 10.1016/j.bmcl.2005.07.085. Bioorg Med Chem Lett. 2005. PMID: 16153839
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Bromidge SM, Brown AM, Clarke SE, Dodgson K, Gager T, Grassam HL, Jeffrey PM, Joiner GF, King FD, Middlemiss DN, Moss SF, Newman H, Riley G, Routledge C, Wyman P. Bromidge SM, et al. J Med Chem. 1999 Jan 28;42(2):202-5. doi: 10.1021/jm980532e. J Med Chem. 1999. PMID: 9925723 No abstract available.
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Bromidge SM, Dabbs S, Davies DT, Duckworth DM, Forbes IT, Ham P, Jones GE, King FD, Saunders DV, Starr S, Thewlis KM, Wyman PA, Blaney FE, Naylor CB, Bailey F, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: wyman pa. J Med Chem. 1998 May 7;41(10):1598-612. doi: 10.1021/jm970741j. J Med Chem. 1998. PMID: 9572885
81 results