5-chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046):: A potent, selective, and orally bioavailable 5-HT6 receptor antagonist

被引:174
作者
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
机构
[1] SmithKline Beecham Pharmaceut, Dept Med Chem, Discovery Res, Harlow CM19 5AW, Essex, England
[2] SmithKline Beecham Pharmaceut, Dept Neurosci Res, Discovery Res, Harlow CM19 5AW, Essex, England
[3] SmithKline Beecham Pharmaceut, Dept Drug Metab & Pharmacokinet, Discovery Res, Harlow CM19 5AW, Essex, England
关键词
D O I
10.1021/jm980532e
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
引用
收藏
页码:202 / 205
页数:4
相关论文
共 17 条
[1]   KETOCONAZOLE AND SULFAPHENAZOLE AS THE RESPECTIVE SELECTIVE INHIBITORS OF P4503A AND 2C9 [J].
BALDWIN, SJ ;
BLOOMER, JC ;
SMITH, GJ ;
AYRTON, AD ;
CLARKE, SE ;
CHENERY, RJ .
XENOBIOTICA, 1995, 25 (03) :261-270
[2]  
BOURSON A, 1995, J PHARMACOL EXP THER, V274, P173
[3]  
BROMIDGE SM, 1998, Patent No. 27081
[4]  
Gerard C, 1996, SYNAPSE, V23, P164, DOI 10.1002/(SICI)1098-2396(199607)23:3<164::AID-SYN5>3.3.CO
[5]  
2-C
[6]   5-HT receptor classification and nomenclature: Towards a harmonization with the human genome [J].
Hoyer, D ;
Martin, G .
NEUROPHARMACOLOGY, 1997, 36 (4-5) :419-428
[7]  
HOYER D, 1994, PHARMACOL REV, V46, P157
[8]  
KOHEN R, 1994, SOC NEUR ABSTR, V20
[9]  
Lewis DF., 1996, CYTOCHROMES P450 STR
[10]  
MONSMA FJ, 1993, MOL PHARMACOL, V43, P320