Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors
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چکیده
منابع مشابه
Beta-Adrenergic Receptors
ion fluxes in these cells, we have now examined the possibility that the decrease in beta receptor number might be associated with concomitant changes in catecholamine-dependent potassium ion transport. Hypothyroid turkey erythrocytes display decreased sensitivity to isoproterenol-stimulated potassium influx. Half-maximal stimulation of potassium influx occurs at 9.2±+1.7 nM in hypothyroid cell...
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The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that interacts with (binds) epinephrine, a hormone and neurotransmitter (ligand synonym, adrenaline) whose signaling, via a downstream Ltype calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. Unlike other adr...
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HISTORY OF MESOTHERAPY This review of basic pharmacology using ephedrine as an active medication is provided by Bryan Haycock, MS, CSCS, founder of HSN. As a sympathomimetic, ephedrine acts to stimulate the sympathetic nervous system. It does this by causing presynaptic nerve terminals to release norepinephrine, or what is commonly called noradrenaline (NA), into the synaptic space. It also has...
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catecholamine-induced desensitization of adenylate cyclase in human neutrophils have been investigated as has the ability of hydrocortisone to modify such alterations. Incubation of human neutrophils with isoproterenol for 3 h in vitro resulted in an 86% reduction in the ability of isoproterenol to stimulate cyclic AMP accumulation in the cells. Two types of receptor alterations were documented...
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Beta adrenergic receptors from membrane fragments of pigmented sheep eyes were studied and characterised by ligand binding techniques after the removal of melanin. In a representative experiment the beta max (total number of beta receptors) was 394.9 fmol/mg protein. The receptor affinity (Ka) was 440 pM. The potency series of drugs to displace 125I-HYP from the receptors was timolol = (-) pro...
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ژورنال
عنوان ژورنال: MedChemComm
سال: 2018
ISSN: 2040-2503,2040-2511
DOI: 10.1039/c7md00656j