Document Detail

Differences of sympathomimetic and anticholinergic action of OH-maprotiline and its R (-)-enantiomer.
MedLine Citation:
PMID:  7150458     Owner:  NLM     Status:  MEDLINE    
1 C 49802 B-Ba and CGP 12103/A are the racemate and the R (-)-enantiomer respectively of the hydroxylated derivative of the tetracyclic antidepressant maprotiline, which differed in their ability to block noradrenaline-uptake and in their anticholinergic activity in animal models. 2 The sympathomimetic and anticholinergic activities of both substances were evaluated in eight healthy subjects and compared with the treatment with placebo and amitriptyline. 3 Heart rate, pupillary diameter, stimulated salivary flow rate and blood pressure were measured over a 15 h period keeping a very strict protocol. Plasma catecholamine levels were determined. 4 Saliva production was diminished following the administration of C 49802 B-Ba, CGP 12103/A and amitriptyline. 5 A moderate, but significant increase in heart rate and mean arterial blood pressure in the recumbent position was observed when C 49802 B-Ba was given. 6 The results in man are in agreement with the different activities found in animal experiments. 7 It can be concluded that the S (+)-enantiomer which the racemate contains is more active than the R (-)-enantiomer as to the anticholinergic and the sympathomimetic property.
O Schmidlin; U Gundert-Remy; W Mäurer; E Weber
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Publication Detail:
Type:  Clinical Trial; Controlled Clinical Trial; Journal Article    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  14     ISSN:  0306-5251     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  1982 Dec 
Date Detail:
Created Date:  1983-03-11     Completed Date:  1983-03-11     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  799-804     Citation Subset:  IM    
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MeSH Terms
Anthracenes / pharmacology*
Blood Pressure / drug effects
Catecholamines / blood
Heart Rate / drug effects
Maprotiline / adverse effects,  analogs & derivatives,  pharmacology*
Pupil / drug effects
Salivation / drug effects
Time Factors
Reg. No./Substance:
0/Anthracenes; 0/Catecholamines; 0/Parasympatholytics; 0/Sympathomimetics; 10262-69-8/Maprotiline; 56433-44-4/hydroxymaprotilin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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