Add time:08/16/2019         Source:sciencedirect.com

A series of variously substituted 2-(4,5-dihydro-1H-imidazol-2-yl)indazoles 3a–j and 2-(4,5-dihydro-1H-imidazol-2-yl)-4,5,6,7-tetrahydroindazole 6 were prepared by the regiospecific heteroalkylation of corresponding indazoles 1a–k with 2-chloro-4,5-dihydroimidazole (2). Their affinity to imidazoline I2 receptors and α2-adrenergic receptors was determined by radioligand binding assay carried out on P2 membrane preparations obtained from rat whole brains. 4-Chloro-2-(4,5-dihydro-1H-imidazol-2-yl)indazole (3f, 4-Cl-indazim) showed a 3076-fold difference in affinity for the [3H]2BFI-labeled imidazoline I2 receptors relative to the [3H]RX821001-labeled α2-adrenergic receptors. This highly selective compound should prove to be useful tool in further understanding the functions of the imidazoline I2 receptors.

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