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Pharmacological characteristics and species‐related variations of β 3 ‐adrenergic receptors
Author(s) -
PietriRouxel F.,
Strosberg AD
Publication year - 1995
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1995.tb00288.x
Subject(s) - chinese hamster ovary cell , receptor , adrenergic receptor , molecular pharmacology , propranolol , chemistry , biology , pharmacology , endocrinology , biochemistry
Summary— Beta‐adrenergic receptors (β/‐AR) belong to the large multigenic family of receptors coupled to GTP‐binding proteins. Three subtypes have been identified: β 1 ‐, β 2 ‐ and β 3 ‐AR. Much of the work delineating the precise pharmacological comparison of the three β‐ARs has come from investigations with stably transfected Chinese hamster ovary cells (CHO cells). This review discusses the structure and function of β 3 ‐AR in various species and presents new findings on a number of β 3 ‐AR ligands including carazolol, tertatolol and CL 316,243 which were found to be selective and potent β 3 ‐AR agonists and ZD 2079 and salmeterol which appear to display full but non‐subtype selective agonistic activity. Species‐related variations of the β 3 ‐AR pharmacology have been shown for propranolol and bupranolol. With the ongoing characterization of the β 3 ‐AR at the molecular and cellular level, and with the advent of computer‐assisted molecular modelling to aid in the determination of the three‐dimensional structure of the receptor, it is thought that novel β 3 ‐AR compounds will become available with improved selectivity and potency.