FEBS Letters · 1988 · 69 citations · 17 references
MedicineEndocrinologyPharmacologyCell SignalingPharmacodynamicsSignal TransductionCholinergic PharmacologyCholinergic SignalingEndocrine PharmacologyPancreatic EndocrinologyPancreatic HormonesReceptor PharmacologyAcetylcholine Receptor PharmacologyCholinergic Receptor PharmacologyMuscarinic Receptor AntagonismMuscarinic Receptor PharmacologyMuscarinic Receptor SubtypesMuscarinic ReceptorsReceptor Subtype SpecificityReceptors
Isolated mouse islets were used to identify the muscarinic receptor subtype present in pancreatic B-cells. We thus compared the inhibitory potencies of atropine (non-specific), of pirenzepine (specific for M1 receptors) and of compound AF-DX 116 (specific for cardiac M2 receptors) on acetylcholine-induced insulin release, 86Rb+ efflux and 45Ca2+ efflux. The three antagonists inhibited all effects of acetylcholine, but EC50 values were markedly different: atropine = 1.5-5 nM, pirenzepine = 0.6-1.7 microM and AF-DX 116 = 1.7-11 microM. The results did not suggest that the various effects of ACh could result from the activation of different subtypes of receptors. It is concluded that muscarinic receptors of pancreatic B-cells belong to an M2 subtype distinct from the cardiac M2 receptors.
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Identification of a Family of Muscarinic Acetylcholine Receptor Genes
Tom I. Bonner, Noel J. Buckley, Alice C. Young et al. · Science · 1987 · 1.4K citations
Pirenzepine distinguishes between different subclasses of muscarinic receptors
Rudolf Hammer, Christopher P. Berrie, N.J.M. Birdsall et al. · Nature · 1980 · 1.3K citations
Medicine, Neuroscience, Pharmacology +16
An M2 Muscarinic Receptor Subtype Coupled to Both Adenylyl Cyclase and Phosphoinositide Turnover
Avi Ashkenazi, John Winslow, Ernest G. Peralta et al. · Science · 1987 · 397 citations