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.
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)