Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor

被引：13

作者：

Kozlowski, JA ^{[1
]}

Lowe, DB ^{[1
]}

Guzik, HS ^{[1
]}

Zhou, GW ^{[1
]}

Ruperto, VB ^{[1
]}

Duffy, RA ^{[1
]}

McQuade, R ^{[1
]}

Crosby, G ^{[1
]}

Taylor, LA ^{[1
]}

Billard, W ^{[1
]}

Binch, H ^{[1
]}

Lachowicz, JE ^{[1
]}

机构：

[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(00)00438-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity studies on [14-(phenylsulfonyl)phenyl] methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4- methoxyphenyl](S)-sulfinyl]phenyl]-1-piperazineacetonitrile, 1, an M-2 selective muscarinic antagonist. Affinity at the cloned human M-2 receptor was 2.7 nM; the M-1/M-2 selectivity is 40-fold. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：2255 / 2257

页数：3

相关论文

共 17 条

[1] CONFIGURATIONAL RELATIONSHIPS AMONG SOME SULFOXIDES [J].

ANDERSEN, KK .

JOURNAL OF ORGANIC CHEMISTRY, 1964, 29 (07) :1953-&

[2]

BARTUS RT, 1987, PSYCHOPHARMACOLOGY 3, P219

[3]

BILLARD W, 1995, J PHARMACOL EXP THER, V273, P273

[4] Effects of xanomeline, a selective muscarinic receptor agonist, on cognitive function and behavioral symptoms in Alzheimer disease [J].

Bodick, NC ;

Offen, WW ;

Levey, AI ;

Cutler, NR ;

Gauthier, SG ;

Satlin, A ;

Shannon, HE ;

Tollefson, GD ;

Rasmussen, K ;

Bymaster, FP ;

Hurley, DJ ;

Potter, WZ ;

Paul, SM .

ARCHIVES OF NEUROLOGY, 1997, 54 (04) :465-473

[5] CHARACTERIZATION OF BIBN-99 - A LIPOPHILIC AND SELECTIVE MUSCARINIC M(2)-RECEPTOR ANTAGONIST [J].

DOODS, H ;

ENTZEROTH, M ;

ZIEGLER, H ;

SCHIAVI, G ;

ENGEL, W ;

MIHM, G ;

RUDOLF, K ;

EBERLEIN, W .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1993, 242 (01) :23-30

[6]

FRASER CM, 1989, MOL PHARMACOL, V36, P840

[7] The reaction between organomagnesium halides and the esters of some sulfur acids [J].

Gilman, H ;

Robinson, J ;

Beaber, NJ .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1926, 48 :2715-2718

[8]

GRAY JA, 1989, TRENDS PHARMACOL SCI, P85

[9] BIOCHEMICAL AND BEHAVIORAL EVIDENCE FOR MUSCARINIC AUTORECEPTORS IN THE CNS [J].

HOSS, W ;

MESSER, WS ;

MONSMA, FJ ;

MILLER, MD ;

ELLERBROCK, BR ;

SCRANTON, T ;

GHODSIHOVSEPIAN, S ;

PRICE, MA ;

BALAN, S ;

MAZLOUM, Z ;

BOHNETT, M .

BRAIN RESEARCH, 1990, 517 (1-2) :195-201

[10]

KOZLOWSKI JA, 1998, SOC NEUR LOS ANG CA