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FG 5893(一种具有5-HT1A受体激动和5-HT2受体拮抗特性的新型化合物)对雄性大鼠性行为的影响。

Effects of FG 5893, a new compound with 5-HT1A receptor agonistic and 5-HT2 receptor antagonistic properties, on male rat sexual behavior.

作者信息

Andersson G, Larsson K

机构信息

Kabi-Pharmacia Therapeutics AB, Malmö, Sweden.

出版信息

Eur J Pharmacol. 1994 Apr 1;255(1-3):131-7. doi: 10.1016/0014-2999(94)90091-4.

DOI:10.1016/0014-2999(94)90091-4
PMID:8026539
Abstract

In the present study male rat sexual behavior was used to explore the functional properties of FG 5893, a newly developed diphenylbutylpiperazinepyridyl derivative which is a 5-HT1A receptor agonist and a 5-HT2 receptor antagonist. Treatment with FG 5893 (0.1-6.0 mg kg-1) stimulated male rat sexual behavior, as evidenced by a decrease in the number of mounts and intromissions to elicit ejaculation, and a shortening of the ejaculation latency. The stimulatory effects varied in a dose-dependent manner, reaching a maximum at 3.0 mg kg-1. Pretreatment with (+/-)-pindolol (0.5 mg kg-1 -30 min), a selective 5-HT1A receptor antagonist, completely antagonized the stimulatory effects of FG 5893 (1 mg kg-1 -20 min) on male sexual behavior. In addition, the behavioral action of FG 5893 was investigated on various components of the 'serotonin behavior syndrome' including flat body posture, forepaw treading, and lower lip retraction. The effects obtained were compared with those induced by treatment with 8-hydroxy-2(di-n-propyl-amino)tetralin (8-OH-DPAT), the prototype of a 5-HT1A receptor agonist. Compared to 8-OH-DPAT, a 100 times higher dose of FG 5893 (10 mg kg-1) was needed to elicit flat body posture while forepaw treading was never seen. Lower lip retraction was elicited by the lowest doses of FG 5893 (0.1 mg kg-1) and 8-OH-DPAT (0.03 mg kg-1). Treatment with (+/-)-pindolol reduced flat body posture elicited by 8-OH-DPAT and completely eradicated the flat body posture induced by FG 5893.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在本研究中,利用雄性大鼠的性行为来探究FG 5893的功能特性。FG 5893是一种新开发的二苯基丁基哌嗪吡啶衍生物,它是5-羟色胺1A(5-HT1A)受体激动剂和5-羟色胺2(5-HT2)受体拮抗剂。用FG 5893(0.1 - 6.0毫克/千克)处理可刺激雄性大鼠的性行为,这表现为引发射精所需的爬跨和插入次数减少,以及射精潜伏期缩短。刺激作用呈剂量依赖性变化,在3.0毫克/千克时达到最大值。用选择性5-HT1A受体拮抗剂(±)-吲哚洛尔(0.5毫克/千克,提前30分钟给药)预处理,可完全拮抗FG 5893(1毫克/千克,提前20分钟给药)对雄性性行为的刺激作用。此外,还研究了FG 5893对“5-羟色胺行为综合征”各个组成部分的行为作用,包括平身姿势、前爪踩踏和下唇回缩。将所得结果与用5-HT1A受体激动剂原型8-羟基-2(二正丙基氨基)四氢萘(8-OH-DPAT)处理所诱导的结果进行比较。与8-OH-DPAT相比,需要高100倍剂量的FG 5893(10毫克/千克)才能引发平身姿势,而从未观察到前爪踩踏。最低剂量的FG 5893(0.1毫克/千克)和8-OH-DPAT(0.03毫克/千克)可引发下唇回缩。用(±)-吲哚洛尔处理可减少8-OH-DPAT引发的平身姿势,并完全消除FG 5893诱导的平身姿势。(摘要截选至250字)

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