beta-Carbolines enhance shock-induced suppression of drinking in rats.
beta-Carbolines enhance shock-induced suppression of drinking in rats.
复制标题
β-咔啉增强大鼠休克诱导的饮酒抑制。
DOI：
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发表时间：
1983
影响因子：
11.1
通讯作者：
E. Costa
中科院分区：
文献类型：
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作者：
M. Corda;W. D. Blaker;W. Mendelson;A. Guidotti;E. Costa
通过使用Vogel的方法来测试苯二氮卓类药物的抗焦虑作用，并降低输送到饮水管的电流强度，可以区分苯二氮卓类识别位点的三种配体的药理活性。抗焦虑苯二氮卓类的典型抗冲突作用，许多β-咔啉类（包括FG 7142）的典型促冲突作用（β-咔啉-3-羧酸乙酯甲基酰胺），以及RO 15-1788典型的促冲突和反冲突作用的拮抗作用（乙基-8-氟-5，6-二氢-5-甲基-6-氧代-4H-咪唑[1，5-α]-[1，4]-苯并二氮杂-3-羧酸酯）和CGS 8216（2-苯基吡唑并[4，3-c]喹啉-3-（5 H）-酮）。戊四唑通过与不同于苯二氮卓类识别位点的γ-氨基丁酸受体亚基相互作用而引起惊厥，也诱导前冲突作用，该作用可被抗焦虑苯二氮卓类拮抗，但不被RO 15-1788拮抗。
By using Vogel's method to test the anxiolytic action of benzodiazepines and reducing the intensity of the current delivered to the drinking tube, it is possible to distinguish the pharmacological activity of three types of ligands for the benzodiazepine recognition site. An anticonflict action typical of anxiolytic benzodiazepines, a proconflict action typical of many beta-carbolines, including FG 7142 (beta-carboline-3-carboxylic acid ethyl ester methyl amide), and an antagonistic action of the proconflict and anticonflict actions typical of RO 15-1788 (ethyl-8-fluoro-5, 6-dihydro-5-methyl-6-oxo-4H-imidazol[1,5-alpha]-[1, 4]-benzodiazepine-3-carboxylate) and CGS 8216 (2-phenylpyrazolo[4,3-c]quinolin-3-(5H)-one). Pentylenetetrazole, which causes convulsions by interacting with a subunit of the gamma-aminobutyric acid receptor that is different from the benzodiazepine recognition site, also induces a proconflict action that is antagonized by anxiolytic benzodiazepines but not by RO 15-1788.