Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1996-1-4
pubmed:abstractText
We hypothesize that 8-hydroxy-clomipramine (8-OH-CMI), the major hydroxy metabolite of clomipramine (CMI), may have antidepressant properties with less anticholinergic potency than CMI. We compared the potencies of 8-OH-CMI and CMI for inhibition of serotonin and norepinephrine reuptake and the potencies of these compounds for blockade of muscarinic receptors. We also compared the antimuscarinic potencies of desmethylclomipramine (DCMI) and 8-hydroxy-desmethylclomipramine (8-OH-DCMI). We found that 8-OH-CMI inhibits the uptake of serotonin and norepinephrine to the same extent as CMI and that 8-OH-CMI has far less antimuscarinic potency than CMI. We also found that 8-OH-DCMI has about one-tenth the antimuscarinic potency of DCMI. Since the therapeutic efficacy of CMI may be related to its effect on the reuptake of neurotransmitters, and since the extent of clinical anticholinergic effects of tricyclic antidepressants has been shown to be related to their in vitro antimuscarinic potencies, these results raise the possibility that 8-OH-CMI may be an analogue of CMI with fewer anticholinergic side effects than the parent compound.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0048-5764
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
217-21
pubmed:dateRevised
2009-11-11
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Comparative neurotransmitter reuptake and anticholinergic potencies of the 8-hydroxy metabolites of clomipramine.
pubmed:affiliation
Department of Pharmacology, School of Medicine, University of Pittsburgh, PA, USA.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't