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γ-氨基丁酸A激动剂以不同方式增强C57BL/6J小鼠中由间接作用多巴胺激动剂诱导的啃咬行为。

gamma-Aminobutyric acidA agonists differentially augment gnawing induced by indirect-acting dopamine agonists in C57BL/6J mice.

作者信息

Tirelli E, Geter-Douglass B, Witkin J M

机构信息

Preclinical Pharmacology Laboratory, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland, USA.

出版信息

J Pharmacol Exp Ther. 1998 Jan;284(1):116-24.

PMID:9435169
Abstract

Evidence from structure-activity, molecular biology, ligand binding and behavioral studies has suggested potential differences in the pharmacological effects of indirect dopamine agonists. Striatal dopaminergic neurotransmission is under the regulatory control of GABAergic inputs. The ability of agonists of gamma-aminobutyric acidA (GABAA) receptors to enhance stereotyped gnawing was used as a method for dissociating the pharmacological effects of indirect-acting dopamine agonists. Gnawing on corrugated cardboard was studied in C57BL/6J mice. The GABAA agonists, gaboxadol HCl (THIP) and muscimol, were not effective in augmenting gnawing in the presence of the direct-acting dopamine agonists, apomorphine, pergolide, RU 24213 or SKF 38393. In addition, THIP did not enhance the gnawing produced by cocaine, bupropion, GBR 12909 or WIN 35428. In contrast, THIP produced marked augmentation of the gnawing induced by methylphenidate, (+)-amphetamine, methamphetamine, amfonelic acid, indatraline, nomifensine, diclofensine, mazindol and GBR 12935. The qualitative differences in potentiation were not caused by differences in the maximal effect of the drugs alone, inadequate dose or routes of administration, or by differences in duration of action. Neither can the absence of potentiation be accounted for by unique effects of THIP; muscimol was only marginally effective in potentiating the effects of WIN 35428 and bupropion but completely inactive in augmenting the effects of cocaine and GBR 12909. Muscimol was efficacious in augmenting the effects of the drugs for which THIP was active. These results add to a small but growing literature that demonstrates differences in the in vitro and in vivo pharmacological effects of indirect dopamine agonists. The methods used here may help in defining the molecular and neural substrates of these differential effects.

摘要

来自构效关系、分子生物学、配体结合及行为学研究的证据表明,间接多巴胺激动剂的药理作用可能存在差异。纹状体多巴胺能神经传递受γ-氨基丁酸能输入的调控。γ-氨基丁酸A(GABAA)受体激动剂增强刻板啃咬的能力被用作区分间接作用多巴胺激动剂药理作用的一种方法。在C57BL/6J小鼠中研究了其对瓦楞纸板的啃咬行为。在直接作用多巴胺激动剂阿扑吗啡、培高利特、RU 24213或SKF 38393存在的情况下,GABAA激动剂盐酸加波沙朵(THIP)和蝇蕈醇在增强啃咬行为方面无效。此外,THIP并未增强可卡因、安非他酮、GBR 12909或WIN 35428所引起的啃咬行为。相比之下,THIP显著增强了哌甲酯、(+)-苯丙胺、甲基苯丙胺、氨苯利酸、茚达立嗪、诺米芬辛、双氯芬辛、马吲哚和GBR 12935所诱导的啃咬行为。增强作用的定性差异并非由药物单独的最大效应差异、剂量不足或给药途径不同,也不是由作用持续时间差异所导致。THIP不存在增强作用也不能用其独特效应来解释;蝇蕈醇在增强WIN 35428和安非他酮的作用方面仅具有微弱效果,但在增强可卡因和GBR 12909的作用方面完全无效。蝇蕈醇在增强THIP有活性的药物作用方面是有效的。这些结果补充了少量但不断增加的文献,这些文献证明了间接多巴胺激动剂在体外和体内药理作用的差异。这里使用的方法可能有助于确定这些差异效应的分子和神经基础。

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