Constitutively active melatonin MT1 receptors in male rat caudal arteries

Çaǧatay Erşahin; Monica I. Masana; Margarita L. Dubocovich

doi:10.1016/S0014-2999(02)01407-3

Constitutively active melatonin MT₁ receptors in male rat caudal arteries

Çaǧatay Erşahin
, Monica I. Masana
, Margarita L. Dubocovich

Pharmacology and Toxicology

Northwestern University

Research output: Contribution to journal › Article › peer-review

29 Scopus citations

Abstract

This study assessed the state of melatonin MT₁ receptor coupling in sections of male rat caudal arteries by [³⁵S]GTPγS binding autoradiography. The melatonin MT₁ receptor inverse agonist 4-phenyl-2-propionamidotetraline (4P-PDOT) (0.1-1 μM) significantly decreased [³⁵S]GTPγS 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.

Original language	English
Pages (from-to)	171-172
Number of pages	2
Journal	European Journal of Pharmacology
Volume	439
Issue number	1-3
DOIs	https://doi.org/10.1016/S0014-2999(02)01407-3
State	Published - Mar 29 2002

Keywords

4P-PDOT (4-phenyl-2-propionamidotetraline)
Constitutive activity
Melatonin MT receptor

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10.1016/S0014-2999(02)01407-3

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title = "Constitutively active melatonin MT1 receptors in male rat caudal arteries",

abstract = "This study assessed the state of melatonin MT1 receptor coupling in sections of male rat caudal arteries by [35S]GTPγS binding autoradiography. The melatonin MT1 receptor inverse agonist 4-phenyl-2-propionamidotetraline (4P-PDOT) (0.1-1 μM) significantly decreased [35S]GTPγS 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.",

keywords = "4P-PDOT (4-phenyl-2-propionamidotetraline), Constitutive activity, Melatonin MT receptor",

author = "{\c C}aǧatay Er{\c s}ahin and Masana, \{Monica I.\} and Dubocovich, \{Margarita L.\}",

year = "2002",

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doi = "10.1016/S0014-2999(02)01407-3",

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T1 - Constitutively active melatonin MT1 receptors in male rat caudal arteries

AU - Erşahin, Çaǧatay

AU - Masana, Monica I.

AU - Dubocovich, Margarita L.

PY - 2002/3/29

Y1 - 2002/3/29

N2 - This study assessed the state of melatonin MT1 receptor coupling in sections of male rat caudal arteries by [35S]GTPγS binding autoradiography. The melatonin MT1 receptor inverse agonist 4-phenyl-2-propionamidotetraline (4P-PDOT) (0.1-1 μM) significantly decreased [35S]GTPγS 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.

AB - This study assessed the state of melatonin MT1 receptor coupling in sections of male rat caudal arteries by [35S]GTPγS binding autoradiography. The melatonin MT1 receptor inverse agonist 4-phenyl-2-propionamidotetraline (4P-PDOT) (0.1-1 μM) significantly decreased [35S]GTPγS 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.

KW - 4P-PDOT (4-phenyl-2-propionamidotetraline)

KW - Constitutive activity

KW - Melatonin MT receptor

UR - https://www.scopus.com/pages/publications/0037192558

U2 - 10.1016/S0014-2999(02)01407-3

DO - 10.1016/S0014-2999(02)01407-3

M3 - Article

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AN - SCOPUS:0037192558

SN - 0014-2999

VL - 439

SP - 171

EP - 172

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1-3

ER -

Constitutively active melatonin MT₁ receptors in male rat caudal arteries

Abstract

Keywords

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