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Chemical Compound Review

Cetiedil     2-(azepan-1-yl)ethyl 2-cyclohexyl-2...

Synonyms: Cetiedilum, Fusten, Cetiedil [INN], AGN-PC-007RO9, CHEMBL419380, ...
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Disease relevance of Cetiedil

  • Cetiedil has been reported to relieve painful crises in sickle cell anemia and to have antisickling properties in vitro [1].
  • Cetiedil, at its highest dosage (0.4 mg/kg body weight), was found to be significantly superior to placebo both in reducing the number of painful sites present on all 4 treatment days and in shortening the total time in crisis [2].
  • Cetiedil was the most effective drug in blocking exercise-induced bronchospasm of the drugs studied [3].
  • Cetiedil), originally a molecule used for treatment of some vascular diseases, exhibits several pharmacological effects [4].
  • Most adverse reactions to cetiedil are related to its anticholinergic properties (dryness of mouth, blurred vision, spacy feelings, disorientation) or vasodilatory effects (light-headedness, vertigo, cold extremities); these side-effects were dose-related with regard to incidence, severity and duration [5].

High impact information on Cetiedil


Biological context of Cetiedil


Anatomical context of Cetiedil


Associations of Cetiedil with other chemical compounds


Gene context of Cetiedil

  • Paralleling the effect of the drug on PMN aggregation, 125 microM cetiedil inhibited release of superoxide by 55% and decreased the number of available 3H-FMLP receptors [8].
  • These results suggest that cetiedil affects the trigger mechanism of the plasma membrane to inhibit the activation of NADPH oxidase [16].
  • The actions of clotrimazole and cetiedil, two drugs known to inhibit the Gardos channel, have been studied on single intermediate conductance calcium-activated potassium (IKCa) channels in inside out patches from human red blood cells, and compared with those of TEA and Ba2+ applied to the cytoplasmic face of the membrane [17].
  • This action was investigated: 1.--In the rat: by measuring the P450 Cytochrome content of hepatic microsomes in rats treated with Cetiedil [18].
  • NH+4 blocked the channel completely. hIK was blocked by the classical inhibitors of the Gardos channel charybdotoxin (IC50 28 nM) and clotrimazole (IC50 153 nM) as well as by nitrendipine (IC50 27 nM), Stichodactyla toxin (IC50 291 nM), margatoxin (IC50 459 nM), miconazole (IC50 785 nM), econazole (IC50 2.4 microM), and cetiedil (IC50 79 microM) [19].

Analytical, diagnostic and therapeutic context of Cetiedil


  1. Effect of cetiedil, an in vitro antisickling agent, on erythrocyte membrane cation permeability. Berkowitz, L.R., Orringer, E.P. J. Clin. Invest. (1981) [Pubmed]
  2. A collaborative, double-blind randomized study of cetiedil citrate in sickle cell crisis. Benjamin, L.J., Berkowitz, L.R., Orringer, E., Mankad, V.N., Prasad, A.S., Lewkow, L.M., Chillar, R.K., Peterson, C.M. Blood (1986) [Pubmed]
  3. Comparative bronchodilatory activity of cetiedil citrate monohydrate, theophylline, orciprenaline and placebo in adult asthmatics. Cho, Y.W., Oh, S.Y., Han, H.C., Kuemmerle, H.P. International journal of clinical pharmacology and biopharmacy. (1978) [Pubmed]
  4. Antiarrhythmic activity of cetiedil and its analogues. Haring, J., Mesangeau, D., Huet, Y., Aurousseau, M. International journal of clinical pharmacology, therapy, and toxicology. (1980) [Pubmed]
  5. Clinical effects of intravenous cetiedil, a candidate anti-sickling agent. Mankad, V.N., Henderson, J.D., Glenn, T.M., Cho, Y.W. International journal of clinical pharmacology research. (1983) [Pubmed]
  6. Bepridil and cetiedil. Vasodilators which inhibit Ca2+-dependent calmodulin interactions with erythrocyte membranes. Agre, P., Virshup, D., Bennett, V. J. Clin. Invest. (1984) [Pubmed]
  7. Effect of cetiedil on cation and water movements in erythrocytes. Schmidt, W.F., Asakura, T., Schwartz, E. J. Clin. Invest. (1982) [Pubmed]
  8. Modulation of polymorphonuclear leukocyte function by cetiedil. Wolach, J.B., Coates, T.D., Tzeng, D.Y., Baehner, R.L., Boxer, L.A. Blood (1983) [Pubmed]
  9. Properties of a cell volume-sensitive potassium conductance in isolated guinea-pig and rat hepatocytes. Sandford, C.A., Sweiry, J.H., Jenkinson, D.H. J. Physiol. (Lond.) (1992) [Pubmed]
  10. Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca(2+)-activated K+ permeability of erythrocytes. Roxburgh, C.J., Ganellin, C.R., Athmani, S., Bisi, A., Quaglia, W., Benton, D.C., Shiner, M.A., Malik-Hall, M., Haylett, D.G., Jenkinson, D.H. J. Med. Chem. (2001) [Pubmed]
  11. A comparative study between the cardiovascular effects of cetiedil, a new vasodilator, and papaverine and aminophylline. Simaan, J.A., Aviado, D.M. J. Pharmacol. Exp. Ther. (1976) [Pubmed]
  12. Bepridil and cetiedil reversibly inhibit thyroid hormone stimulation in vitro of human red cell Ca2+-ATPase activity. Dube, M.P., Davis, F.B., Davis, P.J., Blas, S.D. Mol. Endocrinol. (1987) [Pubmed]
  13. Compared effects of two vesicular acetylcholine uptake blockers, AH5183 and cetiedil, on cholinergic functions in Torpedo synaptosomes: acetylcholine synthesis, choline transport, vesicular uptake, and evoked acetylcholine release. Gaudry-Talarmain, Y.M., Diebler, M.F., O'Regan, S. J. Neurochem. (1989) [Pubmed]
  14. AH5183 and cetiedil: two potent inhibitors of acetylcholine uptake into isolated synaptic vesicles from Torpedo marmorata. Diebler, M.F., Gaudry-Talarmain, Y.M. J. Neurochem. (1989) [Pubmed]
  15. Cetiedil, a drug that inhibits acetylcholine release in Torpedo electric organ. Gaudry-Talarmain, Y.M., Israël, M., Lesbats, B., Morel, N. J. Neurochem. (1987) [Pubmed]
  16. Effects of cetiedil on the oxidative metabolism of activated polymorphonuclear leucocytes. Kohzaki, H., Kakinuma, K., Asakura, T., Yamakawa, T. Br. J. Haematol. (1985) [Pubmed]
  17. The action of blocking agents applied to the inner face of Ca(2+)-activated K+ channels from human erythrocytes. Dunn, P.M. J. Membr. Biol. (1998) [Pubmed]
  18. Research on the eventual enzymatic induction activity of cetiedil in rat and man. Larousse, C., Kergueris, M.F., Le Normand, Y., Visset, J. International journal of clinical pharmacology, therapy, and toxicology. (1980) [Pubmed]
  19. Characterization of the cloned human intermediate-conductance Ca2+-activated K+ channel. Jensen, B.S., Strobaek, D., Christophersen, P., Jorgensen, T.D., Hansen, C., Silahtaroglu, A., Olesen, S.P., Ahring, P.K. Am. J. Physiol. (1998) [Pubmed]
  20. Spontaneous release of acetylcholine from Torpedo synaptosomes: effect of cetiedil and its analogue MR 16728. Moulian, N., Gaudry-Talarmain, Y.M., Israël, M. J. Neurochem. (1994) [Pubmed]
  21. Tolerance of healthy adult males in intravenous infusion of cetiedil, a vasoerythroactive drug. Lewis, G.P., Cho, Y.W. Journal of clinical pharmacology. (1982) [Pubmed]
  22. Human experience of cetiedil, a new vasodilator with anticholinergic properties. Soeterboek, A.M., Scaf, A.H., Lammers, W., Wesseling, H. Eur. J. Clin. Pharmacol. (1977) [Pubmed]
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