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Constitutively active melatonin MT(1) receptors in male rat caudal arteries
Cağatay Erşahin1, Monica I Masana, Margarita L Dubocovich
1Department of Molecular Pharmacology and Biological Chemistry (S215), Northwestern University Medical School, 303 East Chicago Avenue, Chicago, IL 60611, USA.
Abstract:
This study assessed the state of melatonin MT(1) receptor coupling in sections of male rat caudal arteries by [35S]GTPgammaS binding autoradiography. The melatonin MT(1) receptor inverse agonist 4-phenyl-2-propionamidotetraline (4P-PDOT) (0.1-1 microM) significantly decreased [35S]GTPgammaS binding compared to basal, strongly suggesting the presence of constitutively active receptors. Formation of constitutively active receptors during subjective day, when the levels of melatonin are low, may be a physiological mechanism by which the organism maintains vascular tone.