title: Cyproheptadine displays high affinity for muscarinic receptors but does not discriminate between receptor subtypes.
abstract: 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.
authors.affiliation: Department of Pharmacology, Byk Gulden Pharmaceuticals, Konstanz, F.R.G.
authors.forename: M
authors.initials: M
authors.lastname: Eltze
authors.forename: G
authors.initials: G
authors.lastname: Lambrecht
authors.forename: E
authors.initials: E
authors.lastname: Mutschler
mesh_terms: D000818:Animals; D003533:Cyproheptadine / Q000494:pharmacology*; D004558:Electric Stimulation; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology; D010276:Parasympatholytics / Q000494:pharmacology; D011817:Rabbits; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014649:Vas Deferens / Q000187:drug effects / Q000378:metabolism / Q000502:physiology
chemical_list: D010276:Parasympatholytics; D011976:Receptors, Muscarinic; D003533:Cyproheptadine