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组胺及H1和H2受体激动剂与拮抗剂经脑室注射后在禽类中的中枢效应。

Central effects of histamine and H1 and H2 receptors agonists and antagonists after intraventricular infusion in fowls.

作者信息

Nisticò G, Rotiroti D, De Sarro A, Naccari F, Stephenson J D

出版信息

Res Commun Chem Pathol Pharmacol. 1980 Mar;27(3):431-50.

PMID:6104348
Abstract

In adult fowls (Gallus deomesticus) the effects of histamine H2 and H2 histamine receptors angonists and antagonists infused into the III cerebral ventricle were studied on behaviour, electrocortical activity and body temperature. Histamine produced biphasic effects, i.e. an initial period of electrocortical synchronization was followed by a longer-lasting behavioural stimulation, electrocortical desynchronization and shivering. Body temperature was increased in a dose-dependent manner. Dimaprit, an agonist at H2 receptors, produced behavioural and electrocortical sleep and decreased body temperature whereas, 2-(2-thiazolyl-)-ethyl-amine, an agonist at H1 receptors, behavioural stimulation, electrocortical desynchronization, vocalization and hyperthermia. Cimetidine, an antagonist at H2 receptors, produced intense behavioural stimulation and electrocortical desynchronization accompanied by vocalization, tachypnoea, occasional escape responses and stereotypies. Body temperature was increased. Mepyramine, an antagonist at H1 receptors, produced behavioural and electrocortical sleep and prevented behavioural excitation elicited by subsequent infusion of histamine and hyperthermia evoked by 2-(2-thiazolyl -ethylamine. Haloperidol, a neuroleptic drug, sharing with mepyramine membrane stabilizing properties, was unable to antagonize histamine-induced behavioural excitation. In conclusion, present experiments provide pharmacological evidence for the existence of H1 and H2 histamine receptors in avian brain and suggest an involvement of histamine H1 and H2 receptors in the control of arousal-sleep and thermoregulatory mechanisms.

摘要

在成年家禽(家鸡)中,研究了向第三脑室注入组胺H1和H2组胺受体激动剂和拮抗剂对行为、皮层电活动和体温的影响。组胺产生双相效应,即最初的皮层电同步期之后是持续时间更长的行为刺激、皮层电去同步化和颤抖。体温以剂量依赖的方式升高。H2受体激动剂二甲双胍产生行为和皮层电睡眠,并降低体温,而H1受体激动剂2-(2-噻唑基)-乙胺则产生行为刺激、皮层电去同步化、鸣叫和体温过高。H2受体拮抗剂西咪替丁产生强烈的行为刺激和皮层电去同步化,伴有鸣叫、呼吸急促、偶尔的逃避反应和刻板行为。体温升高。H1受体拮抗剂美吡拉敏产生行为和皮层电睡眠,并阻止随后注入组胺引起的行为兴奋以及2-(2-噻唑基)-乙胺引起的体温过高。抗精神病药物氟哌啶醇与美吡拉敏具有共同的膜稳定特性,但无法拮抗组胺诱导的行为兴奋。总之,目前的实验为禽类大脑中存在H1和H2组胺受体提供了药理学证据,并表明组胺H1和H2受体参与了觉醒-睡眠和体温调节机制的控制。

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