Central action of ipsapirone, a new anxiolytic drug, on serotoninergic, noradrenergic and dopaminergic functions
Central action of ipsapirone, a new anxiolytic drug, on serotoninergic, noradrenergic and dopaminergic functions
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新型抗焦虑药伊沙匹隆对血清素能、去甲肾上腺素能和多巴胺能功能的中枢作用
DOI：
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发表时间：
2005
影响因子：
3.3
通讯作者：
A. Kłodzińska
中科院分区：
文献类型：
--
作者：
J. Maj;E. Chojnacka;E. Tatarczyńska;A. Kłodzińska
研究了新型抗焦虑药Ipsapirone （TVX Q 7821,2 -（4-（4-（2-嘧啶基）-1-哌嗪基）丁基）-1,2-苯并异噻唑-3-(2H) 1- 1,1-二氧基盐酸）对中枢5-羟色胺（5-HT）、去甲肾上腺素和多巴胺功能的影响。发现ipsapirone抑制8-OH-DPAT和5-甲氧基-二甲基色胺（5-HT1A受体激动剂）诱导的正常和利血平化大鼠的行为效应（平身姿势和前爪踩）。伊沙匹龙部分抑制大鼠8- oh - dpat诱导的低温，但对小鼠无抑制作用。大剂量ipsapione可以降低大鼠和小鼠的体温，抑制5-羟色氨酸引起的小鼠头抽搐和色氨酸引起的大鼠惊厥和震颤。在脊髓大鼠后肢屈肌反射制备中，只有高剂量的药物能抑制喹帕嗪、间氯苯哌嗪、8-OH-DPAT和St 587 （α 1-肾上腺素受体激动剂）引起的刺激。在环境温度为28℃时，伊沙匹龙不能阻断芬氟拉明和间氯苯哌嗪诱导的大鼠热疗。该药物不影响可乐定诱导的镇静作用，也不显著减轻可乐定诱导的小鼠体温过低。它减轻了d-安非他明引起的小鼠和大鼠的运动过度活跃，但单独给药会降低运动活动。结果表明，ipsapione具有5-HT1A的拮抗作用，且只有在大剂量时才会对5-HT2和α 1肾上腺素能功能产生抑制作用。
Ipsapirone (TVX Q 7821, 2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1,2-benzisothiazol-3-(2H)one-1,1-dioxidehydrochloride), a new anxiolytic drug in respect of the evaluation of its effect on central 5-hydroxy-tryptamine (5-HT), noradrenaline and dopamine functions was studied. It was found that ipsapirone inhibits induced by 8-OH-DPAT and 5-methoxy-dimethyltryptamine (agonists of 5-HT1A receptors) behavioural effects (flat body posture and forepaw treading) in normal and reserpinized rats. Ipsapirone partly inhibited in rats but not in mice the 8-OH-DPAT-induced hypothermia. Ipsapirone, administered at high doses, decreased the body temperature in rats and mice, inhibited the 5-hydroxytryptophan-induced head twitches in mice and the tryptamine-induced convulsions and tremor in rats. In the hind limb flexor reflex preparation of the spinal rat only high doses of the drug inhibited stimulation induced by quipazine, m-chlorphenylpiperazine, 8-OH-DPAT and St 587 (an agonist ofα 1-adrenoceptors). Ipsapirone did not block the fenfluramine- and m-chlorphenylpiperazine-induced hyperthermia in rats at an ambient temperature of 28‡C. The drug did not affect clonidine-induced sedation and inconsiderably attenuated clonidine-induced hypothermia in mice. It attenuated the d-amphetamine-induced locomotor hyperactivity in mice and rats but, given alone, decreased the locomotor activity. The obtained results indicate that ipsapirone exhibits 5-HT1A antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and theα 1adrenergic function.
血清素拮抗剂对大鼠血清素受体激活的两种行为模型的不同作用。
DOI：
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发表时间：
1984
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Lucki,I;Nobler,MS;Frazer,A
通讯作者：
Frazer,A
(-)-Propranolol 可阻断 5-HT1A 选择性激动剂对血清素能中缝背细胞放电的抑制。
影响因子：
5
作者：
Sprouse,JS;Aghajanian,GK
通讯作者：
Aghajanian,GK