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Effects of cicletanine on histamine-induced contractions of isolated rabbit mesenteric arteries

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Ebeigbe, A. B. Cabanie, M. Godfraind, Theophile [UCL]

The antagonism by cicletanine of contractile responses to histamine has been examined in vitro on ring preparations of rabbit mesenteric arteries. Cicletanine (10(-8)-10(-6) M) caused a parallel rightward shift of histamine concentration response curve, with a pA2 value of 7.48 (slope = 0.89 +/- 0.19, not significantly different from unity). Histamine-induced contractions were nifedipine-sensitive and associated with cicletanine-sensitive increased 45Ca uptake. Endothelium removal resulted in enhanced contractile responses to histamine, but did not significantly modify cicletanine-induced antagonism: KB (dissociation constant) values for cicletanine antagonism in the presence or absence of endothelium were: 3.7 (+/- 0.1) X 10(-8) M and 3.6 (+/- 0.3) X 10(-8) M, respectively. Cicletanine (greater than 10(-4) M) also significantly attenuated 10 mM caffeine-induced contractions in rings exposed to Ca-free 100 mM K+ depolarizing medium. The results suggest that cicletanine-induced antagonisms of histamine H1 receptor-mediated contractions of rabbit mesenteric arteries is associated with interference with calcium entry as well as at high concentrations, release from intracellular stores.

Document type Article de périodique (Journal article) – Article de recherche
Access type Accès restreint
Publication date 1989
Journal information "Fundamental and Clinical Pharmacology" - Vol. 3, no. 3, p. 223-235 (1989)
Peer reviewed yes
Publisher Wiley-Blackwell Publishing Ltd. (Chichester)
issn 0767-3981
e-issn 1472-8206
Publication status Publié
Affiliation UCL
MESH Subject Animals ; Anti-Arrhythmia Agents - pharmacology ; Caffeine - pharmacology ; Calcium - metabolism ; Calcium Radioisotopes - diagnostic use ; Diuretics - pharmacology ; Histamine - pharmacology ; Male ; Mesenteric Arteries - drug effects - metabolism ; Muscle Contraction - drug effects ; Muscle, Smooth, Vascular - drug effects - metabolism ; Nifedipine - pharmacology ; Pyridines ; Rabbits
Keywords Cicletanine ; Histamine H1 receptors ; Rabbit mesenteric artery ; Caffeine ; Calcium pools
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Bibliographic reference Ebeigbe, A. B. ; Cabanie, M. ; Godfraind, Theophile. Effects of cicletanine on histamine-induced contractions of isolated rabbit mesenteric arteries. In: Fundamental and Clinical Pharmacology, Vol. 3, no. 3, p. 223-235 (1989)
Permanent URL http://hdl.handle.net/2078.1/11659