β-咔啉增强大鼠休克诱导的饮水抑制。
beta-Carbolines enhance shock-induced suppression of drinking in rats.
作者信息
Corda M G, Blaker W D, Mendelson W B, Guidotti A, Costa E
出版信息
Proc Natl Acad Sci U S A. 1983 Apr;80(7):2072-6. doi: 10.1073/pnas.80.7.2072.
Abstract
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.
摘要
通过使用沃格尔方法测试苯二氮䓬类药物的抗焦虑作用，并降低输送到饮水管的电流强度，可以区分三种类型的苯二氮䓬识别位点配体的药理活性。抗焦虑苯二氮䓬类药物典型的抗冲突作用、许多β-咔啉（包括FG 7142，即β-咔啉-3-羧酸乙酯甲酰胺）典型的促冲突作用，以及RO 15-1788（8-氟-5,6-二氢-5-甲基-6-氧代-4H-咪唑并[1,5-α][1,4]苯二氮䓬-3-羧酸乙酯）和CGS 8216（2-苯基吡唑并[4,3-c]喹啉-3-(5H)-酮）典型的对促冲突和抗冲突作用的拮抗作用。戊四氮通过与不同于苯二氮䓬识别位点的γ-氨基丁酸受体亚基相互作用引起惊厥，也诱导一种促冲突作用，该作用可被抗焦虑苯二氮䓬类药物拮抗，但不能被RO 15-1788拮抗。
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本文引用的文献
1
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Proc Natl Acad Sci U S A. 1982 Oct;79(19):6084-8. doi: 10.1073/pnas.79.19.6084.
2
Does the reversal of the anticonflict effect of phenobarbital by beta-CCE and FG 7142 indicate benzodiazepine receptor-mediated anxiogenic properties?
Eur J Pharmacol. 1982 Aug 27;82(3-4):217-21. doi: 10.1016/0014-2999(82)90517-9.
3
beta-Carboline inhibition of benzodiazepine receptor binding in vivo.
Brain Res. 1982 Apr 22;238(1):286-91. doi: 10.1016/0006-8993(82)90799-5.
4
Interaction of convulsive ligands with benzodiazepine receptors.惊厥性配体与苯二氮䓬受体的相互作用。
Science. 1982 Jun 11;216(4551):1241-3. doi: 10.1126/science.6281892.
5
Unusual interactions of benzodiazepine receptor antagonists.苯二氮䓬受体拮抗剂的异常相互作用。
Nature. 1982 Feb 4;295(5848):436-8. doi: 10.1038/295436a0.
6
Agonist and antagonist benzodiazepine receptor interaction in vitro.体外激动剂与拮抗剂对苯二氮䓬受体的相互作用
Nature. 1981 Dec 24;294(5843):763-5. doi: 10.1038/294763a0.
7
Proconvulsant effects in baboons of beta-carboline, a putative endogenous ligand for benzodiazepine receptors.
Neurosci Lett. 1981 Jun 12;24(1):53-7. doi: 10.1016/0304-3940(81)90358-x.
8
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9
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10
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Nature. 1981 Mar 5;290(5801):54-5. doi: 10.1038/290054a0.
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