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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >A series of novel imidazoline I2-receptor selective Schiff bases of 1-(benzylidenamino)-3,3-dimethylguanidine.
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A series of novel imidazoline I2-receptor selective Schiff bases of 1-(benzylidenamino)-3,3-dimethylguanidine.

机译：一系列新颖的1-（苄亚氨基）-3,3-二甲基胍的咪唑啉I2-受体选择性席夫碱。

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摘要

A series of 12 Schiff bases of 1-(benyzylidenamino)-3,3-dimethylguanidine were evaluated for their affinities at imidazoline I2-receptors and alpha 2-adrenoceptors in the guinea pig cerebral cortex by using a 2-curve assay with [3H]idazoxan as ligand and the simultaneous computer analysis of (-)adrenaline masked and non-masked competition curves. All of the dimethylguanidines were selective for I2-receptors with the selectivity ranging 6-110-fold, and the most selective being WAP8 (2-bromobenzylidenamino-3,3-dimethylguanidine) closely followed by FLA151 (2-chlorobenzylidenamino-3, 3-dimethylguanidine). Some of the dimethylguanidines were also tested for affinity at bovine kidney cortex I2-receptors and guinea pig alpha 1-adrenoceptors. These substances were found to have similar affinities for bovine kidney I2-receptors as for guinea pig cerebral cortex I2-receptors, but their affinities for the alpha 1-adrenoceptors were considerably lower.
机译：使用[3H]的2曲线分析法评估了一系列12种1-（苯甲酰亚氨基）-3,3-二甲基胍的席夫碱对豚鼠大脑皮层中咪唑啉I2-受体和α2-肾上腺素受体的亲和力。以伊达唑烷为配体，同时对（-）肾上腺素掩蔽和非掩蔽竞争曲线进行计算机分析。所有二甲基胍对I2-受体具有选择性，选择性范围为6-110倍，选择性最高的是WAP8（2-溴苄亚氨基-3,3-二甲基胍），其次是FLA151（2-氯苄亚氨基-3，3-二甲基胍）。还测试了一些二甲基胍对牛肾皮质I2-受体和豚鼠α1-肾上腺素受体的亲和力。发现这些物质对牛肾I2受体的亲和力与对豚鼠脑皮质I2受体的亲和力相似，但它们对α1肾上腺素能受体的亲和力要低得多。

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