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Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.
Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, Nash DJ, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Avenell KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Routledge C, Wood M. Stemp G, et al. Among authors: middlemiss dn. J Med Chem. 2000 May 4;43(9):1878-85. doi: 10.1021/jm000090i. J Med Chem. 2000. PMID: 10794704
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
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
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. Among authors: middlemiss dn. J Med Chem. 1996 May 10;39(10):1946-8. doi: 10.1021/jm960017l. J Med Chem. 1996. PMID: 8642552 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. Among authors: middlemiss dn. J Med Chem. 1998 Apr 9;41(8):1218-35. doi: 10.1021/jm970457s. J Med Chem. 1998. PMID: 9548813
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. Among authors: middlemiss dn. J Med Chem. 1999 Jan 28;42(2):202-5. doi: 10.1021/jm980532e. J Med Chem. 1999. PMID: 9925723 No abstract available.
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, King FD, Middlemiss DN, Rahman SK, Saunders DV, Collin LL, Hagan JJ, Riley GJ, Thomas DR. Lovell PJ, et al. Among authors: middlemiss dn. J Med Chem. 2000 Feb 10;43(3):342-5. doi: 10.1021/jm991151j. J Med Chem. 2000. PMID: 10669560 No abstract available.
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: middlemiss dn. J Med Chem. 2000 Mar 23;43(6):1123-34. doi: 10.1021/jm990388c. J Med Chem. 2000. PMID: 10737744
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC, Hadley MS, Hunter AJ, Jeffrey P, Jewitt F, Johnson CN, Jones DN, Medhurst AD, Middlemiss DN, Nash DJ, Riley GJ, Routledge C, Stemp G, Thewlis KM, Trail B, Vong AK, Hagan JJ. Reavill C, et al. Among authors: middlemiss dn. J Pharmacol Exp Ther. 2000 Sep;294(3):1154-65. J Pharmacol Exp Ther. 2000. PMID: 10945872
SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.
Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, Deeks NJ, Eddershaw PJ, Fenwick SH, Riley G, Stean T, Scott CM, Hill MJ, Middlemiss DN, Hagan JJ, Price GW, Forbes IT. Thomas DR, et al. Among authors: middlemiss dn. Br J Pharmacol. 2003 Jun;139(4):705-14. doi: 10.1038/sj.bjp.0705290. Br J Pharmacol. 2003. PMID: 12812993 Free PMC article.
139 results