PREPARATION AND EVALUATION OF SOME HYDROPHILIC PHENYLACETYLPIPERAZINES AS PERIPHERALLY SELECTIVE KAPPA-OPIOID RECEPTOR AGONISTS

被引:6
作者
BIRCH, PJ
HAYES, AG
JOHNSON, MR
LEA, TA
MURRAY, PJ
ROGERS, H
SCOPES, DIC
机构
[1] GLAXO GRP RES LTD,DEPT MED CHEM,WARE SG12 0DP,HERTS,ENGLAND
[2] GLAXO GRP RES LTD,DEPT NEUROPHARMACOL,WARE SG12 0DP,HERTS,ENGLAND
关键词
D O I
10.1016/S0960-894X(00)80229-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of hydrophilic phenylacetylpiperazines as potential peripherally selective kappa-opioid receptor agonists is described. Several compounds were potent kappa-agonists in vitro and one, the sulphone (18), showed significant peripheral selectivity in vivo.
引用
收藏
页码:1275 / 1278
页数:4
相关论文
共 10 条
[1]   NEIGHBORING SULFONIUM GROUP IN ESTER HYDROLYSIS [J].
CASANOVA, J ;
WERNER, ND ;
KIEFER, HR .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1967, 89 (10) :2411-&
[2]   INVIVO STUDIES ON KAPPA-OPIOID RECEPTORS [J].
COWAN, A ;
GMEREK, DE .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1986, 7 (02) :69-72
[3]   A SERIES OF NOVEL, HIGHLY POTENT AND SELECTIVE AGONISTS FOR THE KAPPA-OPIOID RECEPTOR [J].
HAYES, AG ;
BIRCH, PJ ;
HAYWARD, NJ ;
SHEEHAN, MJ ;
ROGERS, H ;
TYERS, MB ;
JUDD, DB ;
SCOPES, DIC ;
NAYLOR, A .
BRITISH JOURNAL OF PHARMACOLOGY, 1990, 101 (04) :944-948
[4]   DIFFERENTIAL SENSITIVITY OF MODELS OF ANTINOCICEPTION IN THE RAT, MOUSE AND GUINEA-PIG TO MU-OPIOID AND KAPPA-OPIOID RECEPTOR AGONISTS [J].
HAYES, AG ;
SHEEHAN, MJ ;
TYERS, MB .
BRITISH JOURNAL OF PHARMACOLOGY, 1987, 91 (04) :823-832
[5]   ENDOGENOUS OPIOID PEPTIDES - MULTIPLE AGONISTS AND RECEPTORS [J].
LORD, JAH ;
WATERFIELD, AA ;
HUGHES, J ;
KOSTERLITZ, HW .
NATURE, 1977, 267 (5611) :495-499
[6]  
MARTIN WR, 1976, J PHARMACOL EXP THER, V197, P517
[7]   KAPPA-OPIOID RECEPTORS AND ANALGESIA [J].
MILLAN, MJ .
TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (02) :70-76
[8]   RABBIT VAS-DEFERENS - A SPECIFIC BIOASSAY FOR OPIOID KAPPA-RECEPTOR AGONISTS [J].
OKA, T ;
NEGISHI, K ;
SUDA, M ;
MATSUMIYA, T ;
INAZU, T ;
UEKI, M .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1981, 73 (2-3) :235-236
[9]   ICI-204448 - A KAPPA-OPIOID AGONIST WITH LIMITED ACCESS TO THE CNS [J].
SHAW, JS ;
CARROLL, JA ;
ALCOCK, P ;
MAIN, BG .
BRITISH JOURNAL OF PHARMACOLOGY, 1989, 96 (04) :986-992
[10]  
STEIN C, 1989, J PHARMACOL EXP THER, V248, P1269