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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: middlemiss dn. J Med Chem. 1998 Apr 9;41(8):1218-35. doi: 10.1021/jm970457s. J Med Chem. 1998. PMID: 9548813
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Atkinson PJ, Bromidge SM, Duxon MS, Gaster LM, Hadley MS, Hammond B, Johnson CN, Middlemiss DN, North SE, Price GW, Rami HK, Riley GJ, Scott CM, Shaw TE, Starr KR, Stemp G, Thewlis KM, Thomas DR, Thompson M, Vong AK, Watson JM. Atkinson PJ, et al. Among authors: middlemiss dn. Bioorg Med Chem Lett. 2005 Feb 1;15(3):737-41. doi: 10.1016/j.bmcl.2004.11.030. Bioorg Med Chem Lett. 2005. PMID: 15664848
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.
Heightman TD, Gaster LM, Pardoe SL, Pilleux JP, Hadley MS, Middlemiss DN, Price GW, Roberts C, Scott CM, Watson JM, Gordon LJ, Holland VA, Powles J, Riley GJ, Stean TO, Trail BK, Upton N, Austin NE, Ayrton AD, Coleman T, Cutler L. Heightman TD, et al. Among authors: middlemiss dn. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4370-4. doi: 10.1016/j.bmcl.2005.06.042. Bioorg Med Chem Lett. 2005. PMID: 16039851
Species differences in 5-HT autoreceptors.
Price GW, Roberts C, Watson J, Burton M, Mulholland K, Middlemiss DN, Jones BJ. Price GW, et al. Among authors: middlemiss dn. Behav Brain Res. 1996;73(1-2):79-82. doi: 10.1016/0166-4328(96)00074-5. Behav Brain Res. 1996. PMID: 8788481
139 results