[3H]β-咔啉-3-羧酸乙酯的非苯二氮䓬类、银依赖性、脑特异性结合位点。

Non-benzodiazepine, Ag-dependent, brain-specific binding sites for [3H]beta-carboline-3-carboxylic acid ethyl ester.

作者信息

Meliksetyan M B

机构信息

Institute of Pharmacology, Acad. Med. Sci. U.S.S.R., Moscow.

出版信息

Eur J Pharmacol. 1989 Dec 7;173(2-3):201-5. doi: 10.1016/0014-2999(89)90521-9.

DOI:10.1016/0014-2999(89)90521-9

PMID:2560435

Abstract

Specific, saturable and reversible binding of [3H]beta + CCE ([3H]beta-carboline-3-carboxylic acid ethyl ester) in buffer containing 20 microM AgNO3 and 10 microM diazepam was detected in rat brain membranes. The binding of [3H]beta CCE to non-benzodiazepine binding sites is Ag+ (Cu)-dependent, stimulated by NaCl and ascorbic acid and inhibited by dithiothreitol. The concentration of non-benzodiazepine [3H]beta CCE binding sites (Bmax) determined in the brain membranes was 1180 +/- 320 pmol/g tissue, and Kd = 77 +/- 19 nM. [3H]beta CCE bound to benzodiazepine receptors in the same membranes with Bmax = 81 +/- 9 pmol/g tissue and Kd = 3.2 +/- 0.4 nM.

摘要

在含有20微摩尔硝酸银和10微摩尔地西泮的缓冲液中，在大鼠脑膜中检测到了[3H]β + CCE（[3H]β-咔啉-3-羧酸乙酯）的特异性、可饱和性和可逆性结合。[3H]β CCE与非苯二氮䓬结合位点的结合是银离子（铜离子）依赖性的，受氯化钠和抗坏血酸刺激，并被二硫苏糖醇抑制。在脑膜中测定的非苯二氮䓬[3H]β CCE结合位点的浓度（Bmax）为1180±320皮摩尔/克组织，解离常数（Kd）= 77±19纳摩尔。[3H]β CCE与同一膜中的苯二氮䓬受体结合，Bmax = 81±9皮摩尔/克组织，Kd = 3.2±0.4纳摩尔。