Agonist site and antagonist site for beta-adrenergic partial agonist.
نویسندگان
چکیده
منابع مشابه
Conversion of agonist site to metal-ion chelator site in the beta(2)-adrenergic receptor.
Previously metal-ion sites have been used as structural and functional probes in seven transmembrane receptors (7TM), but as yet all the engineered sites have been inactivating. Based on presumed agonist interaction points in transmembrane III (TM-III) and -VII of the beta(2)-adrenergic receptor, in this paper we construct an activating metal-ion site between the amine-binding Asp-113 in TM-III...
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BACKGROUND Salbutamol exhibits partial agonist/antagonist activity at airway beta 2 receptors in vitro in that it attenuates the bronchorelaxant effect of the full agonist isoprenaline. The aim of the present study was to characterise the partial beta 2 agonist/antagonist activity of salbutamol in vivo during supine rest and exercise, in states of low and high adrenergic tone. METHODS Eight n...
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Molecular-dynamics simulations with metadynamics enhanced sampling reveal three distinct binding sites for arginine vasopressin (AVP) within its V2 -receptor (V2 R). Two of these, the vestibule and intermediate sites, block (antagonize) the receptor, and the third is the orthosteric activation (agonist) site. The contacts found for the orthosteric site satisfy all the requirements deduced from ...
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Sustained stimulation of several G protein-coupled receptors is known to lead to a reduction in the signaling efficacy. This phenomenon, named agonist-induced desensitization, has been best studied for the beta 2-adrenergic receptor (AR) and is characterized by a decreased efficacy of beta-adrenergic agonists to stimulate the adenylyl cyclase activity. Recently, several beta-adrenergic ligands ...
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The effect of dietary Terbutaline, a beta adrenergic agonist, on carcass characteristics and blood attributes in 288 Japanese quails was studied from 21 through 49 days of age. Dietary treatments included four levels of Terbutaline [0 (T0), 1 (T1), 3 (T3), and 5 (T5) mg/Kg of the diet]. Quails were bled at the end of the trial for biochemical assays and the carcass characteristics were then mea...
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ژورنال
عنوان ژورنال: Japanese Journal of Pharmacology
سال: 1985
ISSN: 0021-5198
DOI: 10.1016/s0021-5198(19)63271-3