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- W2082016945 abstract "Cholinergic agonists and antagonists frequently used for gastrointestinal motility disorders often produce adverse effects. A possible explanation for this is the presence of similar muscarinic receptor subtypes on smooth muscle from different gastrointestinal organs. The aim of this study was to characterize muscarinic receptor subtypes in human gastric smooth muscle with receptor binding methods. N-[ 3 H]Methylscopolamine ([ 3 H]NMS) saturation experiments showed a homogeneous population of noninteracting binding sites (K D = 0.76 ± 0.07 nM, B max = 46.94 ± 3.69 fmol/mg of tissue protein, n H = 0.99 ± 0.01). The rank order of inhibition of [ 3 H]NMS binding by nonlabelled compounds was atropine [Formula: see text] otenzepad [Formula: see text] pirenzepine. Atropine and pirenzepine bound to a homogeneous population of binding sites. The inhibition of [ 3 H]NMS binding by otenzepad showed two populations of receptors (n H < 1, p < 0.01), whose apparent K i1 of 298 ± 40 nM and apparent K i2 of 3.463 ± 0.62 mM were similar to those reported for the M 2 and M 3 muscarinic receptor subtypes. The M 2 subtype was the more abundant of the two, representing 79.12 ± 5.48% of the total population. We conclude that two muscarinic receptor subpopulations similar to the M 2 and M 3 subtypes are present in human gastric smooth muscle and that the M 2 -like receptor is the more abundant of the two.Key words: human stomach, muscarinic receptor subtypes, smooth muscle." @default.
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- W2082016945 date "1995-01-01" @default.
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- W2082016945 title "Otenzepad shows two populations of binding sites in human gastric smooth muscle" @default.
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- W2082016945 doi "https://doi.org/10.1139/y95-017" @default.
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