Agonist-induced desensitization of β-adrenergic receptors in rat myometrium

Here, the consequences of isoproterenol selective desensitization of the rat myometrium are analysed at the membrane beta -adrenergic receptor level. The authors show that the attenuated cAMP response to isoproterenol, when elicited by the agonist itself but not by PGE sub(2), is associated with bot...

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Bibliographic Details
Published in:FEBS letters 1981-11, Vol.135 (1), p.31-37
Main Authors: Tanfin-Tougui, Zahra, Do-Khac, Lien, Harbon, Simone
Format: Article
Language:English
Subjects:
[3H]DHA,(−)[3H] dihydroalprenolol
Adrenergic beta-Agonists - pharmacology
Animals
beta -adrenergic
Cell Membrane - metabolism
Cyclic AMP - metabolism
Dihydroalprenolol - metabolism
Estrogens - pharmacology
Female
Gpp-(NH)p, guanyl-5'-yl imidophosphate
hyposensitization
isoproterenol
Isoproterenol - pharmacology
Kinetics
Male
MIX, 3-isobutyl-1-methylxanthine
Myometrium - drug effects
Myometrium - metabolism
Rats
Receptors, Adrenergic - metabolism
Receptors, Adrenergic, beta - drug effects
Receptors, Adrenergic, beta - metabolism
uterus
Uterus - metabolism
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Summary:Here, the consequences of isoproterenol selective desensitization of the rat myometrium are analysed at the membrane beta -adrenergic receptor level. The authors show that the attenuated cAMP response to isoproterenol, when elicited by the agonist itself but not by PGE sub(2), is associated with both a reduction in the number of beta -adrenergic binding sites, i.e., "down regulation of receptors" and an impaired ability of the residual receptors to form a high affinity complex with the agonist, i.e. "uncoupling process".
ISSN:0014-5793
1873-3468
DOI:10.1016/0014-5793(81)80937-4