Antidepressants and the muscarinic acetylcholine receptor.
Several tricyclic antidepressants have been assessed for their potency in binding to the muscarinic acetylcholine receptor of brain and intestine. Amitriptyline hydrochloride is about ten times as potent as imipramine hydrochloride. Dimethylated drugs are more potent than monomethylated ones. The relative anticholinergic activities of tricyclic antidepressants have implications for their use in patients who might be affected adversely by anticholinergic effects.
D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology*; D014150:Antipsychotic Agents / Q000494:pharmacology; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D008745:Methylation; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology; D010640:Phenothiazines; D051381:Rats; D011950:Receptors, Cholinergic / Q000187:drug effects*; D011976:Receptors, Muscarinic / Q000187:drug effects*; D013329:Structure-Activity Relationship
D000929:Antidepressive Agents, Tricyclic; D014150:Antipsychotic Agents; D008996:Monoamine Oxidase Inhibitors; D010640:Phenothiazines; D011950:Receptors, Cholinergic; D011976:Receptors, Muscarinic