Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists
نویسندگان
چکیده
منابع مشابه
[Selective muscarinic receptor antagonists].
3ubtypes of muscarmic receptors, first hypothesized by Birdsall et al. ~ to explain the anomalous binding of cholinergic agonists to brain receptors~ were later demonstrated with the seEective muscarinic antagonist, pirenzepine 2. Interestingly, the search for selective antagonists, which usually follows the acceptance of a concept, antedated by many years the notion of heterogeneity of rmecari...
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Muscarinic acetylcholine receptors, which comprise five subtypes (M1-M5 receptors), are expressed in both the CNS and PNS (particularly the target organs of parasympathetic neurons). M1-M5 receptors are integral membrane proteins with seven transmembrane segments, bind with acetylcholine (ACh) in the extracellular phase, and thereafter interact with and activate GTP-binding regulatory proteins ...
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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...
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Selective ligands are needed for distinguishing the functional roles of M2 receptors in tissues containing several muscarinic receptor subtypes. Because the venom of the green mamba Dendroaspis angusticeps contains the most specific antagonists known for M1 and M4 receptors (m1-toxin and m4-toxin), it was screened for toxins that inhibit the binding of [(3)H]N-methylscopolamine ([(3)H]NMS) to c...
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ژورنال
عنوان ژورنال: Life Sciences
سال: 1995
ISSN: 0024-3205
DOI: 10.1016/0024-3205(95)00016-y