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选择性α2-肾上腺素能受体拮抗剂[3H]咪唑克生与大鼠嗅皮质膜的结合特性

Binding characteristics of the selective alpha 2-adrenoceptor antagonist [3H]idazoxan to rat olfactory cortex membranes.

作者信息

McLaughlin N J, Collins G G

出版信息

Eur J Pharmacol. 1986 Feb 11;121(1):91-6. doi: 10.1016/0014-2999(86)90396-1.

Abstract

[3H]Idazoxan binding to membranes prepared from rat olfactory cortex obeyed saturation kinetics and was to a single population of sites. Although the density of sites was dependent on the incubation medium, binding was of high affinity (KD approximately 5.5 nM) with a Hill coefficient close to unity. Competition studies with a range of adrenoceptor agonists and antagonists confirmed that [3H]idazoxan binding was to alpha 2-adrenoceptors. Neither chemical lesions with the neurotoxin kainic acid nor chronic unilateral bulbectomy significantly altered any of the [3H]idazoxan binding parameters. These findings suggest that alpha 2-adrenoceptors are not located on the lateral olfactory tract terminals or pyramidal cells of the olfactory cortex.

摘要

[3H]咪唑克生与大鼠嗅觉皮质制备的膜结合遵循饱和动力学,且针对单一的位点群体。尽管位点密度取决于孵育培养基,但结合具有高亲和力(解离常数KD约为5.5 nM),希尔系数接近1。用一系列肾上腺素能受体激动剂和拮抗剂进行的竞争研究证实,[3H]咪唑克生结合的是α2 - 肾上腺素能受体。用神经毒素 kainic 酸进行化学损伤或慢性单侧嗅球切除均未显著改变任何[3H]咪唑克生结合参数。这些发现表明,α2 - 肾上腺素能受体不在嗅觉皮质的外侧嗅束终末或锥体细胞上。

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