Enantiomers of 11‐hydroxy‐10‐methylaporphine having opposing pharmacological effects at 5‐HT1Areceptors
作者:
Joseph G. Cannon,
Scott T. Moe,
John Paul Long,
期刊:
Chirality
(WILEY Available online 1991)
卷期:
Volume 3,
issue 1
页码: 19-23
ISSN:0899-0042
年代: 1991
DOI:10.1002/chir.530030105
出版商: Wiley‐Liss, Inc.
关键词: aporphine enantiomers;serotonin 5‐HT1Areceptors
数据来源: WILEY
摘要:
AbstractThe two enantiomers of the title compound have been prepared by different synthetic routes. Both bind strongly to 5‐HT1Areceptors from rat forebrain membrane tissue. However, in a guinea pig ileum preparation, the (R)‐enantiomer exhibits properties consistent with its being an agonist, whereas the (S)‐enantiomer shows no agonist effect, but it blocks the actions of the (R)‐enantiomer and of 8‐hydroxy‐2‐di‐n‐propylaminotetralin (8‐OH‐DPAT), a 5‐HT1Aagonist. These data are presented as a rare example of enantiomers which demonstrate opposite pharmacological effec
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