Affinity of Nortriptyline and its E-10-Hydroxy Metabolite for Muscarinic Receptors
- 1 January 1991
- journal article
- Published by Wiley in Basic & Clinical Pharmacology & Toxicology
- Vol. 68 (1), 64-67
- https://doi.org/10.1111/j.1600-0773.1991.tb01210.x
Abstract
In the present investigation, the binding of nortriptyline and its active metabolite 10-hydroxynortriptyline (E-10-OH-NT) to muscarinic receptors was studied in the heart, parotid gland, cerebral cortex, urinary bladder and ileum from guinea pig. The affinity of E-10-OH-NT, as determined by competition with 1-quinuclidinyl (phenyl 4-3H)benzilate (-)3H-QNB), was about 10-12 times lower than that of nortriptyline in each tissue and none of the compounds seemed to exhibit any tissue selectivity. It is concluded that increased heart rate induced by E-10-OH-NT, but not by nortriptyline, cannot be attributed to a selective blockade of cardiac muscarinic receptors.Keywords
This publication has 11 references indexed in Scilit:
- A comparative study of the affinities of some tricyclic antidepressants for the muscarinic cholinergic receptor in human and guinea-pig bladder, ileum and brain in relation to differential drug potencyLife Sciences, 1987
- Dicyclomine, benzhexol and oxybutynine distinguish between subclasses of muscarinic binding sitesEuropean Journal of Pharmacology, 1986
- Affinity of nortriptyline to muscarinic receptors in the bladder and ileum of man and guinea-pigEuropean Journal of Pharmacology, 1984
- Differences between Binding Affinities of some Antimuscarinic Drugs in the Parotid Gland and those in the Urinary Bladder and IleumActa Pharmacologica et Toxicologica, 1983
- Muscarinic Receptor Binding in the Guinea Pig Urinary BladderActa Pharmacologica et Toxicologica, 1983
- Neuropharmacological Properties of Amitriptyline, Nortriptyline and their MetabolitesActa Pharmacologica et Toxicologica, 1980
- THE BINDING OF SOME ANTIDEPRESSANT DRUGS TO BRAIN MUSCARINIC ACETYLCHOLINE RECEPTORSBritish Journal of Pharmacology, 1980
- STRUCTURE‐ACTIVITY RELATIONSHIPS FOR THE ANTICHOLINOCEPTOR ACTION OF TRICYCLIC ANTIDEPRESSANTSBritish Journal of Pharmacology, 1978
- Antidepressants and the Muscarinic Acetylcholine ReceptorArchives of General Psychiatry, 1977
- Estimation of hormone receptor affinity by competitive displacement of labeled ligand: Effect of concentration of receptor and of labeled ligandBiochemical and Biophysical Research Communications, 1975