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Spiropiperidines as high-affinity, selective sigma ligands.
Chambers MS, Baker R, Billington DC, Knight AK, Middlemiss DN, Wong EH. Chambers MS, et al. J Med Chem. 1992 May 29;35(11):2033-9. doi: 10.1021/jm00089a013. J Med Chem. 1992. PMID: 1317923
Bromobenzofuran-based non-peptide antagonists of angiotensin II: GR138950, a potent antihypertensive agent with high oral bioavailability.
Judd DB, Dowle MD, Middlemiss D, Scopes DI, Ross BC, Jack TI, Pass M, Tranquillini E, Hobson JE, Panchal TA, et al. Judd DB, et al. J Med Chem. 1994 Sep 16;37(19):3108-20. doi: 10.1021/jm00045a016. J Med Chem. 1994. PMID: 7932534
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
Macdonald GJ, Branch CL, Hadley MS, Johnson CN, Nash DJ, Smith AB, Stemp G, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Winborn KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Watson JM, Wood M, Parker SG, Ashby CR Jr. Macdonald GJ, et al. Among authors: middlemiss dn. J Med Chem. 2003 Nov 6;46(23):4952-64. doi: 10.1021/jm030817d. J Med Chem. 2003. PMID: 14584946
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
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
The discovery and development of 5-HT-terminal autoreceptor antagonists.
Clitherow JW, King FD, Middlemiss DN, Wyman PA. Clitherow JW, et al. Among authors: middlemiss dn. Prog Med Chem. 2003;41:129-65. doi: 10.1016/s0079-6468(02)41004-1. Prog Med Chem. 2003. PMID: 12774693 Review. No abstract available.
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. J Med Chem. 1998 Apr 9;41(8):1218-35. doi: 10.1021/jm970457s. J Med Chem. 1998. PMID: 9548813
Design and synthesis of 2-naphthoate esters as selective dopamine D4 antagonists.
Boyfield I, Brown TH, Coldwell MC, Cooper DG, Hadley MS, Hagan JJ, Healy MA, Johns A, King RJ, Middlemiss DN, Nash DJ, Riley GJ, Scott EE, Smith SA, Stemp G. Boyfield I, et al. J Med Chem. 1996 May 10;39(10):1946-8. doi: 10.1021/jm960017l. J Med Chem. 1996. PMID: 8642552 No abstract available.
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.
Hibert MF, Gittos MW, Middlemiss DN, Mir AK, Fozard JR. Hibert MF, et al. J Med Chem. 1988 Jun;31(6):1087-93. doi: 10.1021/jm00401a007. J Med Chem. 1988. PMID: 3373482
Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino)ethyl]thio]-3-phenylquinoline and its analogues.
Blackburn TP, Cox B, Guildford AJ, Le Count DJ, Middlemiss DN, Pearce RJ, Thornber CW. Blackburn TP, et al. J Med Chem. 1987 Dec;30(12):2252-9. doi: 10.1021/jm00395a013. J Med Chem. 1987. PMID: 3681895
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