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Page 1
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: ham p. J Med Chem. 1998 May 7;41(10):1598-612. doi: 10.1021/jm970741j. J Med Chem. 1998. PMID: 9572885
Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists.
Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gadre A, Ham P, Jones GE, King FD, Saunders DV, Thewlis KM, Vyas D, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: ham p. Bioorg Med Chem. 1999 Dec;7(12):2767-73. doi: 10.1016/s0968-0896(99)00228-x. Bioorg Med Chem. 1999. PMID: 10658582
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.
Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gaster LM, Ham P, Jones GE, King FD, Mulholland KR, Saunders DV, Wyman PA, Blaney FE, Clarke SE, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Trail B, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: ham p. J Med Chem. 2000 Mar 23;43(6):1123-34. doi: 10.1021/jm990388c. J Med Chem. 2000. PMID: 10737744
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: ham p. J Med Chem. 1998 Apr 9;41(8):1218-35. doi: 10.1021/jm970457s. J Med Chem. 1998. PMID: 9548813
The selective 5-HT1B receptor inverse agonist SB-224289, potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Gaster LM, Ham P, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Price GW, Roberts C, Routledge C, Selkirk J, Slade PD, Middlemiss DN. Gaster LM, et al. Among authors: ham p. Ann N Y Acad Sci. 1998 Dec 15;861:270-1. doi: 10.1111/j.1749-6632.1998.tb10219.x. Ann N Y Acad Sci. 1998. PMID: 9928285 No abstract available.
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