Document Detail

Effects of cadralazine on contractions induced by Ca2+ and norepinephrine in isolated rabbit aortic strips.
MedLine Citation:
PMID:  3382458     Owner:  NLM     Status:  MEDLINE    
Antagonistic effects of the new antihypertensive agent cadralazine (ethyl(+/-)-6-[ethyl(2-hydroxypropyl)-amino]-3-pyridazinecarbazate ) and its metabolite ISF-2405 [+/-)-6-[ethyl(2-hydroxypropyl)amino]-3-hydrazinopyridazine) on contractile responses to CaCl2 in K+-depolarised medium and to norepinephrine (NE) in Ca2+-free medium were compared with those of hydralazine using isolated rabbit abdominal aortic strips. Even at high doses of cadralazine (10(-4) mol/l), ISF-2405 (10(-5) mol/l) and hydralazine (10(-5) mol/l), only less than 10% inhibition was observed on dose-dependent contractions induced by CaCl2, 0.05 to 6.4 mmol/l, in K+ 40 mmol/l medium. NE produced dose-dependent contractions even in Ca2+-free medium at concentrations of 10(-9) to 3 X 10(-5) mol/l, and the maximal response was diminished to about 45% of the response in the presence of Ca2+. Cadralazine 10(-4) mol/l exerted no effect on Ca2+-free NE-induced contractions, while ISF-2405 and hydralazine at concentrations of 10(-7) to 10(-5) mol/l were equipotent, showing marked dose-dependent, non-competitive inhibition on NE-induced contractions. These results suggest that ISF-2405 and hydralazine show vasodilating effect through the inhibition of the Ca2+-release from intracellular storage but not via inhibition of the potential dependent Ca2+ influx.
T Higashio; K Kuroda
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  38     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1988 Mar 
Date Detail:
Created Date:  1988-07-20     Completed Date:  1988-07-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  346-9     Citation Subset:  IM    
Research and Development Subdivision, Ciba-Geigy Limited, Hyogo, Japan.
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MeSH Terms
Aorta, Abdominal / drug effects
Calcium / pharmacology*
Hydralazine / pharmacology
Muscle Contraction / drug effects
Muscle, Smooth, Vascular / drug effects*
Norepinephrine / pharmacology*
Pyridazines / pharmacology*
Reg. No./Substance:
0/Pyridazines; 51-41-2/Norepinephrine; 64241-34-5/cadralazine; 70887-18-2/ISF 2405; 7440-70-2/Calcium; 86-54-4/Hydralazine

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