An agonist-specific effect of guanine nucleotides on binding to the beta adrenergic receptor.
نویسندگان
چکیده
منابع مشابه
Interaction between beta-adrenergic receptors and guanine nucleotide sites in turkey erythrocyte membranes.
beta 1-Adrenergic receptors from turkey erythrocyte membranes have been identified by specific binding of the radiolabeled antagonist (-)-[3H]dihydroalprenolol. These receptors are inactivated by the alkylating agent N-ethylmaleimide when occupied by beta-adrenergic agonists but not when occupied by antagonists or when unoccupied. A time-dependent decrease of the number of receptor sites is obs...
متن کاملA ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.
The unique properties of agonist binding to the frog erythrocyte beta-adrenergic receptor include the existence of two affinity forms of the receptor. The proportion and relative affinity of these two states of the receptor for ligands varies with the intrinsic activity of the agonist and the presence of guanine nucleotides. The simplest model for hormone-receptor interactions which can explain...
متن کاملCharacterization of adrenergic receptors in membranes from the rat seminal vesicle.
Characterization of adrenergic receptors in membranes from the rat seminal vesicle was studied by radioligand binding assay. Seminal vesicle membranes contained saturable and high affinity binding sites for the beta-adrenergic receptor antagonist 3H-dihydroalprenolol (3H-DHA) and for the alpha-adrenergic antagonist 3H-prazosin. The observed order of potency for adrenergic agonists in competing ...
متن کاملHeterogeneity of Radioligand Binding to a-Adrenergic Receptors ANALYSIS OF GUANINE NUCLEOTIDE REGULATION OF AGONIST BINDING IN RELATION TO RECEPTOR
Computer modeling of data obtained from agonist competition with [3H]dihydroergocryptine for binding to a-adrenergic receptors in human platelet, rabbit uterine, and rat liver membranes has been performed in an attempt to gain greater insight into the a-adrenergic receptor subtypes and their regulation by guanine nucleotides. In platelet membranes, which appear to contain only a2 adrenergic rec...
متن کاملCardiac adrenergic receptor effects of carvedilol.
Carvedilol is an adrenoceptor antagonist which modulates the activity not only of beta 1 and beta 2 but also of alpha 1 adrenergic receptors present on the cell surface membrane of the human cardiac myocyte. In the heart, carvedilol has approximately 7 times higher potency for beta 1 and beta 2 adrenoceptors, but in the doses 50-100 mg . day-1 used in clinical practice, it is essentially non-se...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Molecular pharmacology
دوره 12 2 شماره
صفحات -
تاریخ انتشار 1976