The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart.
Article Details
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Ehlert FJ, Delen FM, Yun SH, Liem HA
The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart.
J Pharmacol Exp Ther. 1990 Apr;253(1):13-9.
- PubMed ID
- 2329499 [ View in PubMed]
- Abstract
The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary derivatives with muscarinic receptors was investigated in the brain and heart. The potency of the tricyclic derivatives for inhibiting the binding of 11[[2-[(diethylamino) methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b] [1,4] benzodiazepine-6-one to M2 muscarinic receptors in cerebral cortex was similar to that measured in competitive binding experiments with the nonselective muscarinic antagonist [3H]N-methylscopolamine in the corpus striatum and heart. Moreover, the tricyclic derivatives antagonized muscarinic receptor-mediated inhibition of adenylate cyclase activity with similar potency in the corpus striatum and heart, and there was good agreement between the affinities of the tricyclic derivatives when measured by radioligand binding and by antagonism of the adenylate cyclase response. Our results show that amitriptyline, doxepin and imipramine lack selectivity for subtypes of the muscarinic receptor.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Doxepin Muscarinic acetylcholine receptor M1 Protein Humans UnknownAntagonistDetails Doxepin Muscarinic acetylcholine receptor M2 Protein Humans UnknownAntagonistDetails Doxepin Muscarinic acetylcholine receptor M3 Protein Humans UnknownAntagonistDetails Doxepin Muscarinic acetylcholine receptor M4 Protein Humans UnknownAntagonistDetails Doxepin Muscarinic acetylcholine receptor M5 Protein Humans UnknownAntagonistDetails