PMID: 9550309Apr 29, 1998Paper

Isothiocyanatobenzyl imidazoline is an alkylating agent for I2-imidazoline binding sites in rat and rabbit tissues

Naunyn-Schmiedeberg's Archives of Pharmacology
M A BoronatJ A García-Sevilla

Abstract

Isothiocyanatobenzyl imidazoline (IBI), the 4'-NCS analogue of tolazoline, has been used to alkylate several receptor sites in rabbit iris muscles. Because of the high affinity of tolazoline for the I2-imidazoline binding sites (Ki = 16-130 nM), this study was designed to assess whether IBI is also an alkylating agent for these sites. In competition studies, IBI displayed moderate affinity (Ki approximately 2-3 microM) against I2A-imidazoline sites in the rabbit cerebral cortex and I2B-imidazoline sites in the rat cerebral cortex labelled by [3H]2-(2-benzofuranyl)-2-imidazoline ([3H]2-BFI). However, preincubation (30 min at 25 degrees C) of rat cortical and liver membranes with IBI (10(-7) M to 10(-3) M), followed by extensive washing, markedly decreased (17% to 96%) the specific binding of [3H]2-BFI to I2B-imidazoline sites. IBI (10(-5) M to 10(-3) M) also bound irreversibly to I2A-imidazoline sites in rabbit cerebral cortex but with a lesser efficacy (27% to 83% reduction of [3H]2-BFI binding). Saturation curves of [3H]2-BFI binding in the rat cerebral cortex indicated that preincubation with 10(-6) M IBI reduced the total density (Bmax) without affecting the affinity (Kd) of I2B-imidazoline sites for IBI. Acute treatments (6...Continue Reading

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