Oct 29, 1985

Characterization of alpha-adrenoceptors in myometrium of preparturient rats

European Journal of Pharmacology
J P Maltier, C Legrand

Abstract

We describe three methods for the quantitative analysis of the alpha-adrenoceptor subtypes in preparturient rat myometrial membrane fractions. A non-subtype-selective antagonist radioligand. [3H]dihydroergocryptine ([3H]DHE), was used to label all of the alpha-receptors. [3H]DHE bound to both alpha 1- and alpha 2-receptors with indistinguishable affinity. Computer modelling of competition curves of unlabeled selective antagonists or agonists was then required in order to determine reliably alpha 1 and alpha 2 affinities and proportions: the alpha 1-receptors represent 45% and the alpha 2-receptors 55% of the entire alpha-receptor population in rat uterus. The second approach involved the administration of phenoxybenzamine (POB) that irreversibly blocks the alpha 1-adrenoceptors. Myometrial membranes obtained from rats 1 h after the administration of varying amounts of POB showed a dose-dependent reduction in specific [3H]DHE binding. This reduction was accompanied by a progressive increase of the value of the dissociation constant. Our data indicate that a dose of 1 mg of POB left the alpha 2-receptors intact while entirely blocking the alpha 1-receptors in rat myometrium. The third approach utilized the selective radioligand a...Continue Reading

  • References29
  • Citations6

Citations

Mentioned in this Paper

Yohimbin Spiegel
Tissue Membrane
Phenoxybenzamine Hydrochloride
Myometrial
August Rats
Antagonist Muscle Action
Rauwolscine
Malignant Neoplasm of Myometrium
Entire Myometrium
Adrenergic Receptor

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.