Literature DB >> 2885205

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

P Schoeffter, J Ghysel-Burton, M Cabanie, T Godfraind.   

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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Year:  1987        PMID： 2885205     DOI： 10.1016/0014-2999(87)90716-3

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  5 in total

1.  Short-term desensitization of the histamine H1 receptor in human HeLa cells: involvement of protein kinase C dependent and independent pathways.

Authors:  M J Smit; S M Bloemers; R Leurs; L G Tertoolen; A Bast; S W de Laat; H Timmerman
Journal:  Br J Pharmacol       Date:  1992-10       Impact factor: 8.739

2.  Acute effects of cicletanine in angina pectoris.

Authors:  D L Murdoch; E Henderson; H J Dargie; G T McInnes
Journal:  Eur J Clin Pharmacol       Date:  1993       Impact factor: 2.953

3.  A comparison of the acute effects of cicletanine and bendrofluazide on urinary electrolytes and plasma potassium in essential hypertension.

Authors:  D R Singer; N D Markandu; A L Sugden; G A MacGregor
Journal:  Eur J Clin Pharmacol       Date:  1990       Impact factor: 2.953

4.  Histamine H1-receptors mediate phosphoinositide and calcium response in cultured smooth muscle cells--interaction with cicletanine (CIC).

Authors:  M O Lonchampt; P Marche; C Demerle; A Girard; M Cabanie; A Esanu; P E Chabrier; P Braquet
Journal:  Agents Actions       Date:  1988-07

5.  In vitro vascular effects of cicletanine in pregnancy-induced hypertension.

Authors:  A B Ebeigbe; M Cabanie
Journal:  Br J Pharmacol       Date:  1991-08       Impact factor: 8.739
  5 in total

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