SELECTIVE AND ENANTIOSPECIFIC ACYLATION OF KAPPA-OPIOID RECEPTORS BY (1S,2S)-TRANS-2-ISOTHIOCYANATO-N-METHYL-N-[2-(1-PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE - DEMONSTRATION OF KAPPA-RECEPTOR HETEROGENEITY

被引:40
作者
DECOSTA, BR
ROTHMAN, RB
BYKOV, V
JACOBSON, AE
RICE, KC
机构
[1] NIDDKD,NEUROSCI LAB,DRUG DESIGN & SYNTH SECT,BETHESDA,MD 20892
[2] NIMH,CLIN STUDIES LAB,RECEPTOR STUDIES UNIT,BETHESDA,MD 20892
关键词
D O I
10.1021/jm00122a001
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
引用
收藏
页码:281 / 283
页数:3
相关论文
共 30 条
[1]   SYNTHESIS AND CHARACTERIZATION OF AN AFFINITY LABEL FOR BRAIN RECEPTORS TO PSYCHOTOMIMETIC BENZOMORPHANS - DIFFERENTIATION OF SIGMA-TYPE AND PHENCYCLIDINE RECEPTORS [J].
ADAMS, JT ;
TEAL, PM ;
SONDERS, MS ;
TESTER, B ;
ESHERICK, JS ;
SCHERZ, MW ;
KEANA, JFW ;
WEBER, E .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1987, 142 (01) :61-71
[2]   STEREOCHEMISTRY - A SOURCE OF PROBLEMS IN MEDICINAL CHEMISTRY [J].
ARIENS, EJ .
MEDICINAL RESEARCH REVIEWS, 1986, 6 (04) :451-466
[3]   PROBES FOR NARCOTIC RECEPTOR MEDIATED PHENOMENA .12. CIS-(+)-3-METHYLFENTANYL ISOTHIOCYANATE, A POTENT SITE-DIRECTED ACYLATING AGENT FOR SIGMA-OPIOID RECEPTORS - SYNTHESIS, ABSOLUTE-CONFIGURATION, AND RECEPTOR ENANTIOSELECTIVITY [J].
BURKE, TR ;
JACOBSON, AE ;
RICE, KC ;
SILVERTON, JV ;
SIMONDS, WF ;
STREATY, RA ;
KLEE, WA .
JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (06) :1087-1093
[4]   PURIFICATION TO APPARENT HOMOGENEITY OF A MU-TYPE OPIOID RECEPTOR FROM RAT-BRAIN [J].
CHO, TM ;
HASEGAWA, JI ;
GE, BL ;
LOH, HH .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (12) :4138-4142
[5]   HIGHLY SELECTIVE KAPPA-OPIOID ANALGESICS - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL N-[(2-AMINOCYCLOHEXYL)ARYL]ACETAMIDE AND N-[(2-AMINOCYCLOHEXYL)ARYLOXY]ACETAMIDE DERIVATIVES [J].
CLARK, CR ;
HALFPENNY, PR ;
HILL, RG ;
HORWELL, DC ;
HUGHES, J ;
JARVIS, TC ;
REES, DC ;
SCHOFIELD, D .
JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (04) :831-836
[6]   SYNTHESIS AND ABSOLUTE-CONFIGURATION OF OPTICALLY PURE ENANTIOMERS OF A KAPPA-OPIOID RECEPTOR SELECTIVE AGONIST [J].
DECOSTA, B ;
GEORGE, C ;
ROTHMAN, RB ;
JACOBSON, AE ;
RICE, KC .
FEBS LETTERS, 1987, 223 (02) :335-339
[7]   [H-3]U-69593 A HIGHLY SELECTIVE LIGAND FOR THE OPIOID K-RECEPTOR [J].
LAHTI, RA ;
MICKELSON, MM ;
MCCALL, JM ;
VONVOIGTLANDER, PF .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1985, 109 (02) :281-284
[8]   PHARMACOLOGICAL PROFILE OF PD-117302, A SELECTIVE KAPPA-OPIOID AGONIST [J].
LEIGHTON, GE ;
JOHNSON, MA ;
MEECHAM, KG ;
HILL, RG ;
HUGHES, J .
BRITISH JOURNAL OF PHARMACOLOGY, 1987, 92 (04) :915-922
[9]  
MARTIN WR, 1983, PHARMACOL REV, V35, P283
[10]  
MUNSON PJ, 1980, ANAL BIOCHEM, V107, P735