2-(3,4-DICHLOROPHENYL)-N-METHYL-N-[(1S)1-(3-ISOTHIOCYANATOPHENYL)-2-(1-PYRROLIDINYL)ETHYL]ACETAMIDE - AN OPIOID RECEPTOR AFFINITY LABEL THAT PRODUCES SELECTIVE AND LONG-LASTING KAPPA ANTAGONISM IN MICE

被引:21
作者
CHANG, AC
TAKEMORI, AE
PORTOGHESE, PS
机构
[1] UNIV MINNESOTA,COLL PHARM,DEPT MED CHEM,MINNEAPOLIS,MN 55455
[2] UNIV MINNESOTA,SCH MED,DEPT PHARMACOL,MINNEAPOLIS,MN 55455
关键词
D O I
10.1021/jm00037a001
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
[No abstract available]
引用
收藏
页码:1547 / 1549
页数:3
相关论文
共 34 条
[1]  
BARLOW J J, 1991, Journal of Medicinal Chemistry, V34, P3149, DOI 10.1021/jm00115a001
[2]   A SINGLE AMINO-ACID OF THE CHOLECYSTOKININ-B GASTRIN RECEPTOR DETERMINES SPECIFICITY FOR NONPEPTIDE ANTAGONISTS [J].
BEINBORN, M ;
LEE, YM ;
MCBRIDE, EW ;
QUINN, SM ;
KOPIN, AS .
NATURE, 1993, 362 (6418) :348-350
[3]   [D-ALA2,LEU5,CYS6]ENKEPHALIN - SHORT-TERM AGONIST EFFECTS AND LONG-TERM ANTAGONISM AT DELTA OPIOID RECEPTORS [J].
CALCAGNETTI, DJ ;
FANSELOW, MS ;
HELMSTETTER, FJ ;
BOWEN, WD .
PEPTIDES, 1989, 10 (02) :319-326
[4]   SELECTIVE REVERSIBLE AND IRREVERSIBLE LIGANDS FOR THE KAPPA-OPIOID RECEPTOR [J].
CHENG, CY ;
WU, SC ;
HSIN, LW ;
TAM, SW .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (12) :2243-2247
[5]   2-(3,4-DICHLOROPHENYL)-N-METHYL-N-[2-(1-PYRROLIDINYL)-1-SUBSTITUTED-ETHYL]-ACETAMIDES - THE USE OF CONFORMATIONAL-ANALYSIS IN THE DEVELOPMENT OF A NOVEL SERIES OF POTENT OPIOID KAPPA-AGONISTS [J].
COSTELLO, GF ;
JAMES, R ;
SHAW, JS ;
SLATER, AM ;
STUTCHBURY, NCJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) :181-189
[6]  
D'amour FE, 1941, J PHARMACOL EXP THER, V72, P74
[7]   SYNTHESIS OF HIGH SPECIFIC ACTIVITY TRITIUM LABELED 1S,2S-(-)-TRANS-2-ISOTHIOCYANATO-N-METHYL-N-[2-(1-PYRROLIDINYL)-CYCLOHEXYL]BENZENEACETAMIDE, A SPECIFIC IRREVERSIBLE LIGAND FOR KAPPA-OPIOID RECEPTORS [J].
DECOSTA, BR ;
THURKAUF, A ;
ROTHMAN, RR ;
JACOBSON, AE ;
RICE, KC .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1990, 28 (11) :1257-1264
[8]   SYNTHESIS OF AN AFFINITY LIGAND (UPHIT) FOR INVIVO ACYLATION OF THE KAPPA-OPIOID RECEPTOR [J].
DECOSTA, BR ;
BAND, L ;
ROTHMAN, RB ;
JACOBSON, AE ;
BYKOV, V ;
PERT, A ;
RICE, KC .
FEBS LETTERS, 1989, 249 (02) :178-182
[9]   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 [J].
DECOSTA, BR ;
ROTHMAN, RB ;
BYKOV, V ;
JACOBSON, AE ;
RICE, KC .
JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (02) :281-283
[10]   PROBES FOR NARCOTIC RECEPTOR MEDIATED PHENOMENA .17. SYNTHESIS AND EVALUATION OF A SERIES OF TRANS-3,4-DICHLORO-N-METHYL-N-[2-(1-PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE (U50,488) RELATED ISOTHIOCYANATE DERIVATIVES AS OPIOID RECEPTOR AFFINITY LIGANDS [J].
DECOSTA, BR ;
ROTHMAN, RB ;
BYKOV, V ;
BAND, L ;
PERT, A ;
JACOBSON, AE ;
RICE, KC .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (04) :1171-1176