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5-羟色胺2B受体激动剂BW 723C86对三种大鼠焦虑模型的影响。

Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.

作者信息

Kennett G A, Bright F, Trail B, Baxter G S, Blackburn T P

机构信息

Psychiatry Department, SmithKline Beecham Pharmaceuticals, Harlow, Essex.

出版信息

Br J Pharmacol. 1996 Apr;117(7):1443-8. doi: 10.1111/j.1476-5381.1996.tb15304.x.

DOI:10.1111/j.1476-5381.1996.tb15304.x
PMID:8730737
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1909458/
Abstract
  1. BW 723C86 (3 and 10 mg kg-1, s.c. 30 min pretest), a 5-HT2B receptor agonist, increased total interaction, but not locomotion in a rat social interaction test, a profile consistent with anxiolysis. 2. The effect of BW 723C86 in the social interaction test is likely to be 5-HT2B receptor-mediated as it was prevented by pretreatment with the 5-HT2C/2B receptor antagonist, SB 200646A, (1 and 2 mg kg-1, p.o., 1 h pretest) which did not affect basal levels of social interaction at the doses used. 3. An anxiolytic-like action was also observed in the rat Geller-Seifter conflict test, where BW 723C86 (0.5-50 mg kg-1, s.c. 30 min pretest) modestly, but significantly increased punished, but not unpublished responding. 4. In a rat 5 min elevated x-maze test, BW 723C86 (1-10 mg kg-1, s.c.) had no significant effect. 5. The maximal anxiolytic-like effect of BW 723C86 approached that of the benzodiazepine anxiolytic, chloradiazepoxide (5 mg kg-1, s.c. 30 min pretest) in the social interaction test, but was markedly less in the Geller-Siefter test. The effect of BW 723C86 was also clearly less than chlordiazepoxide in the elevated x-maze procedure where it had no significant effect. 6. In conclusion, BW 723C86 exerted an appreciable anxiolytic-like profile in a rat social interaction test, but had a weaker effect in the Geller-Siefter and was ineffective in the elevated x-maze test used. These effects are likely to be 5-HT2B receptor-mediated.
摘要
  1. BW 723C86(3和10毫克/千克,皮下注射,测试前30分钟),一种5-羟色胺2B受体激动剂,在大鼠社交互动测试中增加了总互动,但未增加运动,这一表现与抗焦虑作用一致。2. BW 723C86在社交互动测试中的作用可能是由5-羟色胺2B受体介导的,因为用5-羟色胺2C/2B受体拮抗剂SB 200646A(1和2毫克/千克,口服,测试前1小时)预处理可阻止该作用,而所用剂量的SB 200646A不影响社交互动的基础水平。3. 在大鼠盖勒-西弗冲突测试中也观察到了类似抗焦虑的作用,其中BW 723C86(0.5 - 50毫克/千克,皮下注射,测试前30分钟)适度但显著增加了受惩罚的反应,但未增加未受惩罚的反应。4. 在大鼠5分钟高架十字迷宫测试中,BW 723C86(1 - 10毫克/千克,皮下注射)没有显著影响。5. 在社交互动测试中,BW 723C86的最大类似抗焦虑作用接近苯二氮䓬类抗焦虑药氯氮卓(5毫克/千克,皮下注射,测试前30分钟),但在盖勒-西弗测试中明显较小。在高架十字迷宫实验中,BW 723C86的作用也明显小于氯氮卓,且无显著影响。6. 总之,BW 723C86在大鼠社交互动测试中表现出明显的类似抗焦虑作用,但在盖勒-西弗测试中作用较弱,在所用的高架十字迷宫测试中无效。这些作用可能是由5-羟色胺2B受体介导的。

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