Competitive and stereoselective histamine H1 antagonistic effect of cicletanide in guinea-pig isolated ileum.

Schoeffter, P.;Ghysel-Burton, J;Cabanie, M;Godfraind, Theophile
(1987) European Journal of Pharmacology — Vol. 136, n° 2, p. 235-237 (1987)

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Abstract
The histamine H1 antagonistic effects of the racemic form and the enantiomers of cicletanide, a new antihypertensive furopyridine derivative, were investigated in guinea-pig isolated ileum. Both the racemic and the (-) enantiomer behaved as competitive histamine antagonists (pA2 values of 6.8 and 7.2, respectively). The (+) enantiomer was at least 100 times less potent than the (-) enantiomer. The H1-blocking effect of cicletanide is the most potent and is the only stereoselective property so far reported for the drug.
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Schoeffter, P., Ghysel-Burton, J., Cabanie, M., & Godfraind, T. (1987). Competitive and stereoselective histamine H1 antagonistic effect of cicletanide in guinea-pig isolated ileum. European Journal of Pharmacology, 136(2), 235-237. https://hdl.handle.net/2078.5/130472 (Original work published 1987)