Wikberg J E, Uhlén S, Chhajlani V
Department of Pharmacology, Umeå University, Sweden.
Eur J Pharmacol. 1991 Feb 14;193(3):335-40. doi: 10.1016/0014-2999(91)90148-j.
A number of imidazoline, imidazole and guanidinium compounds and other drugs were compared for their ability to bind to non-adrenergic idazoxan (imidazoline) I-receptors in particulate guinea pig cerebral cortex and ileum smooth muscle fractions. Radioligand binding with [3H]idazoxan was used for the experiments. Computer modelling of the binding data gave dissociation constants for drug binding to both I-receptors and alpha 2-adrenoceptors. Most drugs showed similar affinities for I-receptors in cortex and ileum. However, medetomidine stereoisomers as well as a few other drugs clearly delineated the I-receptors in cortex and ileum as different.
比较了多种咪唑啉、咪唑和胍化合物及其他药物与豚鼠大脑皮层微粒体和回肠平滑肌组分中非肾上腺素能的咪唑克生（咪唑啉）I受体的结合能力。实验采用[³H]咪唑克生进行放射性配体结合研究。对结合数据进行计算机建模得出了药物与I受体及α₂肾上腺素能受体结合的解离常数。大多数药物对皮层和回肠中的I受体显示出相似的亲和力。然而，美托咪定立体异构体以及其他一些药物清楚地表明皮层和回肠中的I受体是不同的。
