牛松果体中的苯二氮䓬受体位点。

Benzodiazepine receptor sites in bovine pineal.

作者信息

Lowenstein P R, Cardinali D P

出版信息

Eur J Pharmacol. 1982 Dec 24;86(2):287-9. doi: 10.1016/0014-2999(82)90329-6.

Abstract

[3H]Flunitrazepam (FNZP) binds to a single class of high affinity binding sites in bovine pineal membranes (KD 2.8 nM). FNZP binding increased by 25% after exposure to gamma-aminobutyric acid and exhibits a high degree of specificity for drugs acting on the central type of benzodiazepine receptor. High affinity binding of [3H]ethyl-3-carboline ester to pineal membranes has a KD 0.8 nM and about 60% of the maximal number of FNZP binding sites.

摘要

[3H]氟硝西泮（FNZP）与牛松果体膜中的一类高亲和力结合位点结合（解离常数KD为2.8纳摩尔）。暴露于γ-氨基丁酸后，FNZP结合增加了25%，并且对作用于中枢型苯二氮䓬受体的药物表现出高度特异性。[3H]乙基-3-咔啉酯与松果体膜的高亲和力结合的解离常数KD为0.8纳摩尔，约为FNZP结合位点最大数量的60%。