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Department of Pharmacology, Byk Gulden Pharmaceuticals, Konstanz, F.R.G.
The affinity of cyproheptadine for different muscarinic receptor subtypes was investigated in vitro by functional experiments in field-stimulated vas deferens of the rabbit (ganglionic M1- and cardiac M2-receptors) and in guinea-pig ileum (smooth muscle M3-receptors). Cyproheptadine displayed high but similar affinity for all muscarinic receptor subtypes studied (pA2 = 7.99-8.02). In contrast, (+)-telenzepine (M1 over M2 and M3), and for mefurtramine (M2 over M3 and M1) were found to be selective.
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