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[肾上腺素能α受体激动剂LE S3341急性和慢性治疗对大鼠各种外周器官和脑结构中儿茶酚胺周转速率的影响]

[Effects of acute and chronic treatment with an adrenergic alpha receptor agonist, LE S3341, on the rate of catecholamine turnover in various peripheral organs and brain structures in the rat].

作者信息

Rochette L, Beley A, Bralet J

出版信息

J Pharmacol. 1986 Oct-Dec;17(4):567-77.

PMID:2882066
Abstract

The turnover of catecholamines (CA) in some peripheral tissues and various areas of the rat brain was estimated by measuring the amine depletion after inhibition of their biosynthesis by alpha-methyl-p-tyrosine (alpha-MPT). Acute or chronic treatment with S3341 (3mg/kg i.p.) reduced NA turnover in submaxillary glands, brain stem and rest of the brain but had no effect on NA turnover in the hypothalamus. The dopamine (DA) levels were unaltered following chronic S3341 treatment but the alpha-MPT induced disappearance of DA was significantly retarded in the striatum and rest of the brain. The results of the present study demonstrate that no tolerance to the effect of S3341 on brain CA turnover develops during chronic drug administration. The central biochemical effects of S3341 appear different from those of other agonists of central alpha 2-adrenoceptors such as clonidine.

摘要

通过测量α-甲基对酪氨酸(α-MPT)抑制儿茶酚胺(CA)生物合成后胺的耗竭情况,估算了大鼠某些外周组织和脑不同区域中CA的周转率。急性或慢性给予S3341(3mg/kg腹腔注射)可降低颌下腺、脑干和脑其他部位的去甲肾上腺素(NA)周转率,但对下丘脑的NA周转率无影响。慢性给予S3341后多巴胺(DA)水平未改变,但α-MPT诱导的DA在纹状体和脑其他部位的消失明显延迟。本研究结果表明,在慢性给药期间,对S3341对脑CA周转率的影响不会产生耐受性。S3341的中枢生化作用似乎与其他中枢α2-肾上腺素能受体激动剂如可乐定不同。

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