N-MODIFIED FLUOROPHENYLTROPANE ANALOGS OF COCAINE WITH HIGH-AFFINITY FOR COCAINE RECEPTORS

被引：36

作者：

MADRAS, BK ^{[1
]}

KAMIEN, JB ^{[1
]}

FAHEY, MA ^{[1
]}

CANFIELD, DR ^{[1
]}

MILIUS, RA ^{[1
]}

SAHA, JK ^{[1
]}

NEUMEYER, JL ^{[1
]}

SPEALMAN, RD ^{[1
]}

机构：

[1] RES BIOCHEM INC,NATICK,MA 01760

来源：

PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR | 1990年 / 35卷 / 04期

关键词：

Cocaine; Cocaine analogs; Drug discrimination; Monkeys; [!sup]3[!/sup]H]Cocaine binding;

D O I：

10.1016/0091-3057(90)90384-T

中图分类号：

B84 [心理学]; C [社会科学总论]; Q98 [人类学];

学科分类号：

03 ; 0303 ; 030303 ; 04 ; 0402 ;

摘要：

The binding properties of three N-modified fluorophenyltropane analogs of cocaine were compared in competition experiments with [3H]cocaine. All three analogs displaced specifically bound [3H]cocaine from caudateputamen membranes of cynomolgus monkeys with affinities exceeding that of cocaine. The compound with the highest affinity, 2β-carbomethoxy-3β-(4-fluorophenyl)-N-allyl-nortropane, (N-allyl-CFNT) was about three times more potent than cocaine. N-Allyl-CFNT also had cocaine-like interoceptive effects and was about three times more potent than cocaine in squirrel monkeys trained to discriminate cocaine from vehicle in an operant drug discrimination procedure. The results suggest that N-modified fluorophenyltropane derivatives may be useful precursors for development of pharmacological probes for cocaine receptors. © 1990.

引用

页码：949 / 953

页数：5

共 26 条

[1] BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERIZATION OF [H-3] GBR-12935 BINDING INVITRO TO RAT STRIATAL MEMBRANES - LABELING OF THE DOPAMINE UPTAKE COMPLEX [J].