Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1 , hM2 , hM3 , hM4 and hM5 using microphysiometry
نویسندگان
چکیده
منابع مشابه
Long-Term Activation upon Brief Exposure to Xanomleline Is Unique to M1 and M4 Subtypes of Muscarinic Acetylcholine Receptors
Xanomeline is an agonist endowed with functional preference for M1/M4 muscarinic acetylcholine receptors. It also exhibits both reversible and wash-resistant binding to and activation of these receptors. So far the mechanisms of xanomeline selectivity remain unknown. To address this question we employed microfluorometric measurements of intracellular calcium levels and radioligand binding to in...
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Sequestration of porcine muscarinic acetylcholine receptor m2 subtypes (m2 receptors) expressed in COS-7 cells is facilitated by coexpression of G protein-coupled receptor kinases 2 (GRK2). We examined the effect of coexpression of GRK2, GRK4 delta, GRK5 and GRK6 on sequestration of human m1-m5 receptors expressed in COS-7 cells, which was assessed as loss of [3H]N-methylscopolamine binding act...
متن کاملMuscarinic Receptor Agonists and Antagonists
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed. A selection of chemical routes are described, which illustrate contemporary methodology for the synthes...
متن کاملMuscarinic receptor subtypes in airways.
Muscarinic receptor subtypes in the airways appear to subserve different physiological functions. M1-receptors facilitate neurotransmission through parasympathetic ganglia and enhance cholinergic reflexes, but are also localized to alveolar walls. M2-receptors act as autoreceptors on post-ganglionic cholinergic nerves and inhibit acetylcholine release. There is some evidence that they may be de...
متن کاملMUSCARINIC RECEPTOR SUBTYPES IN SMOOTH MUSCLE FROM THE BODY OF HUMAN STOMACH
Up to date, there are four pharmacologically characterized subtypes of muscarinic receptors (M1, M2, M3 and M4). In our study we have investigated muscarinic receptor subtypes in smooth muscle layers of human stomach. Isolated preparations of longitudinal and circular muscle layers from human stomach were used. Acetylcholine, bethanechol, carbachol, pilocarpine and AHR -602 produced concen...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 1999
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0702463