PMID: 8971730Dec 1, 1996Paper

Pharmacological and molecular discrimination of brain I2-imidazoline receptor subtypes

Naunyn-Schmiedeberg's Archives of Pharmacology
G OlmosJ A García-Sevilla

Abstract

I2-imidazoline receptors labelled with [3H]-idazoxan in the rabbit and rat brains displayed high and low affinity, respectively, for the guanidide amiloride; reinforcing the previous definition of I2A-imidazoline receptors expressed in the rabbit brain and I2B-imidazoline receptors expressed in the rat brain. Other drugs tested displayed biphasic curves in competition experiments, indicating the existence of high and low affinity sites for both subtypes of I2-imidazoline receptors. Among the drugs studied, bromoxidine, moxonidine, (+)- and (-)-medetomidine and clorgyline were more potent on the high and/or low affinity sites of I2B-than on their corresponding of I2A-imidazoline receptors (KiH ratios 20 to 65). No correlation was found for the potencies of the drugs tested at the low affinity sites of both I2-imidazoline receptor subtypes. Preincubation (30 min at 25 degrees C) with 10(-6) M clorgyline reduced by 60% the Bmax of [3H]-idazoxan binding to I2B-imidazoline receptors in the rat brain, but it did not affect the binding parameters of the radioligand saturation curves to I2A-imidazoline receptors in the rabbit brain. These results indicated that I2A- and I2B-imidazoline receptor subtypes differ in the pharmacological pr...Continue Reading

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Citations

Apr 5, 2000·European Journal of Pharmacology·C PolidoriM Massi
Oct 11, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·F SaczewskiJ Saczewski
Jul 15, 1998·British Journal of Clinical Pharmacology·P BitsiosC M Bradshaw
Jul 23, 1999·Annals of the New York Academy of Sciences·G OlmosJ A García-Sevilla

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