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Binding of [125I]iodocyanopindolol by rat harderian gland crude membranes: kinetic characteristics and day-night variations.

作者信息

Harmouch A, Osuna C, Rafii-el-Idrissi M, Calvo J R, Guerrero J M

机构信息

Department of Medical Biochemistry and Molecular Biology, The University of Seville School of Medicine, Spain.

出版信息

Biosci Rep. 1996 Oct;16(5):369-77. doi: 10.1007/BF01207262.

DOI:10.1007/BF01207262
PMID:8913527
Abstract

The Harderian glands are innervated by sympathetic fibers originating in the superior cervical ganglia. The aim of this study is to characterize the beta-adrenergic receptors in the rat Harderian gland. The characteristics of beta-adrenergic receptors were determined in crude membrane preparations from rat Harderian gland, using [125I]iodocyanopindolol ([125I]CYP) as radioligand. The binding of the ligand to the receptor is rapid, reversible, saturable, specific and dependent on time, temperature and membrane concentration. At 30 degrees C, stoichiometric data suggest the presence of one binding site with a Kd value of 0.29 nM and Bmax of 32 pmol/L. The interaction shows a high degree of specificity for beta-adrenergic agonists and blockers, as suggested by competitive displacement experiment with isoproterenol (IC50 = 19.1 nM), propranolol (IC50 = 28.1 nM), and norepinephrine (IC50 = 96.3 nM). Clonidine, yohimbine, methoxamine, and prazosin are ineffective at concentrations up to 1 microM. In the other hand, binding of [125I]CYP by Harderian gland membranes exhibits day-night variations. Binding values are low during the daytime and increase progressively late in the evening to reach a maximum at 2200 h (2 h after the onset of dark period), but decreased to the end of the dark period (0600 h). In conclusion, the results presented in this paper show the functional and pharmacological characterization of beta-adrenergic receptors in the rat Harderian gland. This neurotransmitter may play a physiological role at this level regulating, at least, processes such as a thyroid hormone metabolism.

摘要

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