PREPARATION AND STUDY OF DERIVATIVES AND ANALOGS OF THE PHENCYCLIDINE MOLECULE POSSESSING IMMUNOSUPPRESSIVE PROPERTIES INVITRO

被引:12
作者
ILAGOUMA, AT
DORNAND, J
LIU, CF
ZENONE, F
MANI, JC
KAMENKA, JM
机构
[1] ECOLE NATL SUPER CHIM,CNRS,UPR 8402,INSERM,U249,8 RUE ECOLE NORMALE,F-34053 MONTPELLIER 1,FRANCE
[2] CNRS,INSERM,CTR PHARMACOL ENDOCRINOL,F-34094 MONTPELLIER,FRANCE
[3] UNIV MONTPELLIER 2,INSERM,U65,F-34060 MONTPELLIER,FRANCE
关键词
conformation; immuno suppression; PCP; phencyclidine;
D O I
10.1016/0223-5234(90)90186-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Derivatives and analogues of the phencyclidine molecule (1-phenyl 1-(1-piperidino) cyclohexane or PCP) were prepared to investigate their immunosuppressive potency and to define the physicochemical parameters which may influence this activity recently demonstrated for PCP. Most of the tested molecules are more effective than PCP itself. In spite of lack of quantitative data, the biological activity appears to be dependent upon 3 parameters: conforamation, lipophilicity, and the empirical Hammett's parameters. The homogeneous conformations with a high lipophilicity were the most immunosuppressive. Interestingly, such structures appeared to be of weak potency on the PCP receptor in the CNS. © 1990.
引用
收藏
页码:609 / 615
页数:7
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