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
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1989年 / 32卷 / 02期
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
[11]   6-BETA [N,N-BIS(2-CHLOROETHYL)AMINO]-17-(CYCLOPROPYLMETHYL)-4,5-ALPHA-EPOXY-3,14-DIHYDROXYMORPHINAN (CHLORANALTREXAMINE) - POTENT OPIOID RECEPTOR ALKYLATING AGENT WITH ULTRALONG NARCOTIC-ANTAGONIST ACTIVITY [J].
PORTOGHESE, PS ;
LARSON, DL ;
JIANG, JB ;
TAKEMORI, AE ;
CARUSO, TP .
JOURNAL OF MEDICINAL CHEMISTRY, 1978, 21 (07) :598-599
[12]   NOVEL OPIOID RECEPTOR-SITE DIRECTED ALKYLATING AGENT WITH IRREVERSIBLE NARCOTIC ANTAGONISTIC AND REVERSIBLE AGONISTIC ACTIVITIES [J].
PORTOGHESE, PS ;
LARSON, DL ;
SAYRE, LM ;
FRIES, DS ;
TAKEMORI, AE .
JOURNAL OF MEDICINAL CHEMISTRY, 1980, 23 (03) :233-234
[13]   BINALTORPHIMINE-RELATED BIVALENT LIGANDS AND THEIR KAPPA-OPIOID RECEPTOR ANTAGONIST SELECTIVITY [J].
PORTOGHESE, PS ;
NAGASE, H ;
LIPKOWSKI, AW ;
LARSON, DL ;
TAKEMORI, AE .
JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (04) :836-841
[14]   IRREVERSIBLE LIGANDS WITH HIGH SELECTIVITY TOWARD DELTA-OPIATE OR MU-OPIATE RECEPTORS [J].
RICE, KC ;
JACOBSON, AE ;
BURKE, TR ;
BAJWA, BS .
SCIENCE, 1983, 220 (4594) :314-316
[15]   TRITIATED-6-BETA-FLUORO-6-DESOXY-OXYMORPHONE ([H-3] FOXY) - A NEW LIGAND AND PHOTOAFFINITY PROBE FOR THE MU OPIOID RECEPTORS [J].
ROTHMAN, RB ;
BYKOV, V ;
RICE, KC ;
JACOBSON, AE ;
KOOPER, GN ;
BOWEN, WD .
NEUROPEPTIDES, 1988, 11 (01) :1-6
[16]   PREPARATION OF RAT-BRAIN MEMBRANES GREATLY ENRICHED WITH EITHER TYPE-I-DELTA OR TYPE-II-DELTA OPIATE BINDING-SITES USING SITE DIRECTED ALKYLATING-AGENTS - EVIDENCE FOR A 2-SITE ALLOSTERIC MODEL [J].
ROTHMAN, RB ;
BOWEN, WD ;
BYKOV, V ;
SCHUMACHER, UK ;
PERT, CB ;
JACOBSON, AE ;
BURKE, TR ;
RICE, KC .
NEUROPEPTIDES, 1984, 4 (03) :201-215
[17]   PREPARATION OF RAT-BRAIN MEMBRANES HIGHLY ENRICHED WITH OPIATE KAPPA BINDING-SITES USING SITE-DIRECTED ACYLATING AGENTS - OPTIMIZATION OF ASSAY CONDITIONS [J].
ROTHMAN, RB ;
BYKOV, V ;
DANKS, JA ;
JACOBSON, AE ;
BURKE, TR ;
RICE, KC ;
HERKENHAM, M .
NEUROPEPTIDES, 1985, 6 (06) :503-516
[18]   A BRIEF STUDY OF THE SELECTIVITY OF NORBINALTORPHIMINE, (-)-CYCLOFOXY, AND (+)-CYCLOFOXY AMONG OPIOID RECEPTOR SUBTYPES INVITRO [J].
ROTHMAN, RB ;
BYKOV, V ;
REID, A ;
DECOSTA, BR ;
NEWMAN, AH ;
JACOBSON, AE ;
RICE, KC .
NEUROPEPTIDES, 1988, 12 (03) :181-187
[19]   LY164929 - A HIGHLY SELECTIVE LIGAND FOR THE LOWER AFFINITY [H-3]D-ALA2-D-LEU-5-ENKEPHALIN BINDING-SITE [J].
ROTHMAN, RB ;
BYKOV, V ;
OFRI, D ;
RICE, KC .
NEUROPEPTIDES, 1988, 11 (01) :13-16
[20]  
ROTHMAN RB, 1988, J PHARMACOL EXP THER, V247, P405
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