Literature DB >> 6482660

Weak binding of 10-hydroxymetabolites of nortriptyline to rat brain muscarinic acetylcholine receptors.

A Wägner, B Ekqvist, L Bertilsson, F Sjöqvist.   

Abstract

The relative affinities of nortriptyline (NT) and its 10-hydroxymetabolites to rat brain muscarinic acetylcholine receptors have been determined by competition with 3H-quinuclidinyl benzilate binding. It is shown that the major NT metabolite, E-10-OH-NT, has only 1/18 the affinity of NT for the muscarinic receptor. Since this metabolite is equipotent to NT in inhibiting neuronal noradrenaline uptake, it is suggested that it might be of clinical value as an antidepressant by virtue of having less anticholinergic side-effects than NT itself.

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Year:  1984        PMID: 6482660     DOI: 10.1016/0024-3205(84)90395-3

Source DB:  PubMed          Journal:  Life Sci        ISSN: 0024-3205            Impact factor:   5.037


  6 in total

1.  Attitudes to development of drug therapy in Scandinavia.

Authors:  F Sjöqvist; G Boethius
Journal:  Br J Clin Pharmacol       Date:  1986       Impact factor: 4.335

Review 2.  The Role of Metabolites of Antidepressants in the Treatment of Depression.

Authors:  M V Rudorfer; W Z Potter
Journal:  CNS Drugs       Date:  1997-04       Impact factor: 5.749

Review 3.  Active hydroxymetabolites of antidepressants. Emphasis on E-10-hydroxy-nortriptyline.

Authors:  C Nordin; L Bertilsson
Journal:  Clin Pharmacokinet       Date:  1995-01       Impact factor: 6.447

Review 4.  Metabolism of tricyclic antidepressants.

Authors:  M V Rudorfer; W Z Potter
Journal:  Cell Mol Neurobiol       Date:  1999-06       Impact factor: 5.046

5.  Plasma concentrations of nortriptyline and its 10-hydroxy metabolite in depressed patients--relationship to the debrisoquine hydroxylation metabolic ratio.

Authors:  C Nordin; B Siwers; J Benitez; L Bertilsson
Journal:  Br J Clin Pharmacol       Date:  1985-06       Impact factor: 4.335

6.  CSF and plasma levels of nortriptyline and its 10-hydroxy metabolite.

Authors:  C Nordin; L Bertilsson; B Siwers
Journal:  Br J Clin Pharmacol       Date:  1985-10       Impact factor: 4.335

  6 in total

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