氟哌啶醇在体外可增加催乳素释放及环磷酸腺苷的生成：对多巴胺D2受体的反向激动作用？
Haloperidol increases prolactin release and cyclic AMP formation in vitro: inverse agonism at dopamine D2 receptors?
作者信息
Nilsson C L, Eriksson E
机构信息
Department of Pharmacology, University of Göteborg, Sweden.
出版信息
J Neural Transm Gen Sect. 1993;92(2-3):213-20. doi: 10.1007/BF01244880.
PMID:7690232
Abstract
Haloperidol (30 nM, 3 microM) was found to increase prolactin release from GH4C 1 cells transfected with the D2 receptor cDNA (GH4ZR 7) and from wild-type (untransfected) GH 3 cells, but not from wild-type GH4C 1 cells. In addition, haloperidol (3 microM) stimulated cAMP formation in GH 3 cells. It is suggested that haloperidol may act as an inverse agonist rather than as a neutral antagonist at dopaminergic D2 receptors.
摘要
已发现氟哌啶醇（30 nM，3 microM）可增加转染了D2受体cDNA的GH4C1细胞（GH4ZR 7）以及野生型（未转染）GH3细胞中催乳素的释放，但对野生型GH4C1细胞无此作用。此外，氟哌啶醇（3 microM）可刺激GH3细胞中cAMP的生成。提示氟哌啶醇在多巴胺能D2受体上可能作为反向激动剂而非中性拮抗剂起作用。
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