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Chemical Compound Review

Ketanserin     3-[2-[4-(4- fluorophenyl)carbonyl-1...

Synonyms: Perketal, Serefrex, Sufrexal, Ketaserin, R-41468, ...
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Disease relevance of Ketanserin


Psychiatry related information on Ketanserin


High impact information on Ketanserin


Chemical compound and disease context of Ketanserin


Biological context of Ketanserin


Anatomical context of Ketanserin

  • Although human coronary arteries may differ in their responsiveness to 5-HT or ketanserin, these data suggest that ischemia from ergonovine-induced coronary vasospasm is not mediated by 5-HT receptors [14].
  • In quiescent rings, platelets caused contractions, which were reduced in the presence of endothelium; the contractions were prevented by ketanserin (a 5-HT2 serotonergic blocker) or methiothepin but not by R 68 070 (a thromboxane A2 receptor blocker) or dazoxiben (a thromboxane-synthetase blocker) [21].
  • In a second group of dogs, CFVs were established after constrictor placement, abolished with the serotonin (5HT2) receptor antagonist ketanserin, and reestablished by the continuous infusion of serotonin into the left atrium [22].
  • Ketanserin inhibits depolarization-activated outward potassium current in rat ventricular myocytes [23].
  • Pretreatment with ketanserin, a 5-HT2A /2C receptor antagonist, significantly blocked the stress-induced downregulation of BDNF mRNA in hippocampus, in support of this hypothesis [24].

Associations of Ketanserin with other chemical compounds


Gene context of Ketanserin

  • Reserpine and ketanserin are slightly more potent inhibitors of VMAT2-mediated transport than of VMAT1-mediated transport, whereas tetrabenazine binds to and inhibits only VMAT2 [28].
  • In contrast, ketanserin, a specific 5-HT2 antagonist, and 5-HT3-selective drugs (ICS 205 930 and MDL 72222) were very weak in antagonizing the 5-HT-inhibited cAMP formation [29].
  • The pharmacological profile of the human 5-HT2B receptor was virtually identical to that of the rat 5-HT2B receptor, with the exceptions of the 5-HT2A receptor antagonists ketanserin and spiperone [30].
  • Similar treatment with the 5-HT2 receptor antagonist ketanserin (3 microM) had no significant effect on LTP [31].
  • The effect of 5-HT was insensitive to ketanserin (5-HT2) but antagonized by methiothepin (5-HT1/2) or by metergoline (5-HT1C/1D) [32].

Analytical, diagnostic and therapeutic context of Ketanserin


  1. Ketanserin for hypertension after upper gastrointestinal surgery. Mikulic, E., Rull, D., Puntoni, L. Lancet (1991) [Pubmed]
  2. Ketanserin in intermittent claudication. Ramsay, L.E. Lancet (1986) [Pubmed]
  3. Randomised controlled trial of ketanserin and aspirin in prevention of pre-eclampsia. Steyn, D.W., Odendaal, H.J. Lancet (1997) [Pubmed]
  4. Change in serum hyaluronan: a simple index of short-term drug-induced changes in hepatic sinusoidal perfusion. Gibson, P.R., Fraser, J.R., Colman, J.C., Jones, P.A., Jennings, G., Dudley, F.J. Gastroenterology (1993) [Pubmed]
  5. Ketanserin in acute superficial thrombophlebitis. de Roose, J., Symoens, J. Lancet (1982) [Pubmed]
  6. Ketanserin treatment of Tourette's syndrome in children. Bonnier, C., Nassogne, M.C., Evrard, P. The American journal of psychiatry. (1999) [Pubmed]
  7. Comparative effects of ketanserin, atropine and methysergide on the gastrointestinal effects of hyperserotoninemia in the awake dog. Jaffe, B.M., Ferrara, A., Sherlock, D.J. J. Pharmacol. Exp. Ther. (1986) [Pubmed]
  8. Effects of blockade of 5-HT2 receptors and activation of 5-HT1A receptors on the exploratory activity of rats in the elevated plus-maze. Motta, V., Maisonnette, S., Morato, S., Castrechini, P., Brandão, M.L. Psychopharmacology (Berl.) (1992) [Pubmed]
  9. Slow wave sleep in humans: role of 5-HT2A and 5-HT2C receptors. Sharpley, A.L., Elliott, J.M., Attenburrow, M.J., Cowen, P.J. Neuropharmacology (1994) [Pubmed]
  10. A serotonergic (5-HT2) receptor mechanism in the laterodorsal tegmental nucleus participates in regulating the pattern of rapid-eye-movement sleep occurrence in the rat. Amici, R., Sanford, L.D., Kearney, K., McInerney, B., Ross, R.J., Horner, R.L., Morrison, A.R. Brain Res. (2004) [Pubmed]
  11. Local effect of serotonin released during coronary angioplasty. Golino, P., Piscione, F., Benedict, C.R., Anderson, H.V., Cappelli-Bigazzi, M., Indolfi, C., Condorelli, M., Chiariello, M., Willerson, J.T. N. Engl. J. Med. (1994) [Pubmed]
  12. Novel flushing provoked by volatile anesthetics in Mastomys natalensis bearing a transplantable substrain of gastric carcinoid that predominantly secretes serotonin. Hosoda, S., Suyama, M., Saito, T., Kohmura, Y., Hosoda, R. J. Natl. Cancer Inst. (1984) [Pubmed]
  13. Contribution of 5-HT2A receptor in nematode infection-induced murine intestinal smooth muscle hypercontractility. Zhao, A., Urban, J.F., Morimoto, M., Elfrey, J.E., Madden, K.B., Finkelman, F.D., Shea-Donohue, T. Gastroenterology (2006) [Pubmed]
  14. Ergonovine-induced myocardial ischemia: no role for serotonergic receptors? Freedman, S.B., Chierchia, S., Rodriguez-Plaza, L., Bugiardini, R., Smith, G., Maseri, A. Circulation (1984) [Pubmed]
  15. Combination of ketanserin and verapamil or propranolol in patients with alcoholic cirrhosis: search for an additive effect. Hadengue, A., Moreau, R., Cerini, R., Koshy, A., Lee, S.S., Lebrec, D. Hepatology (1989) [Pubmed]
  16. The pentagastrin test in the diagnosis of the carcinoid syndrome. Blockade of gastrointestinal symptoms by ketanserin. Ahlman, H., Dahlström, A., Grönstad, K., Tisell, L.E., Oberg, K., Zinner, M.J., Jaffe, B.M. Ann. Surg. (1985) [Pubmed]
  17. 5-HT, alpha-adrenoceptors, and blood pressure. Effects of ketanserin in essential hypertension and autonomic insufficiency. Wenting, G.J., Woittiez, A.J., Man in't Veld, A.J., Schalekamp, M.A. Hypertension (1984) [Pubmed]
  18. Placebo-controlled double-blind trial of ketanserin in treatment of intermittent claudication. De Cree, J., Leempoels, J., Geukens, H., Verhaegen, H. Lancet (1984) [Pubmed]
  19. A double-blind, placebo-controlled study of ketanserin in patients with Prinzmetal's angina. Evidence against a role for serotonin in the genesis of coronary vasospasm. De Caterina, R., Carpeggiani, C., L'Abbate, A. Circulation (1984) [Pubmed]
  20. Vasoactive effects of serotonin on proximal coronary arteries in awake dogs. Chu, A., Cobb, F.R. Circ. Res. (1987) [Pubmed]
  21. Endothelium-dependent relaxation in response to aggregating platelets in porcine femoral veins and its modulation by diet. Komori, K., Shimokawa, H., Vanhoutte, P.M. Circulation (1989) [Pubmed]
  22. Cooperative mediation by serotonin S2 and thromboxane A2/prostaglandin H2 receptor activation of cyclic flow variations in dogs with severe coronary artery stenoses. Ashton, J.H., Ogletree, M.L., Michel, I.M., Golino, P., McNatt, J.M., Taylor, A.L., Raheja, S., Schmitz, J., Buja, L.M., Campbell, W.B. Circulation (1987) [Pubmed]
  23. Ketanserin inhibits depolarization-activated outward potassium current in rat ventricular myocytes. Zhang, Z.H., Boutjdir, M., el-Sherif, N. Circ. Res. (1994) [Pubmed]
  24. 5-HT2A receptor-mediated regulation of brain-derived neurotrophic factor mRNA in the hippocampus and the neocortex. Vaidya, V.A., Marek, G.J., Aghajanian, G.K., Duman, R.S. J. Neurosci. (1997) [Pubmed]
  25. Coexpression of 5-HT2A and 5-HT4 receptors coupled to distinct signaling pathways in human intestinal muscle cells. Kuemmerle, J.F., Murthy, K.S., Grider, J.R., Martin, D.C., Makhlouf, G.M. Gastroenterology (1995) [Pubmed]
  26. Allergic reactions of rat jejunal mucosa. Ion transport responses to luminal antigen and inflammatory mediators. Crowe, S.E., Sestini, P., Perdue, M.H. Gastroenterology (1990) [Pubmed]
  27. Serotonin as an alternative transmitter in sympathetic nerves of large cerebral arteries of the rabbit. Saito, A., Lee, T.J. Circ. Res. (1987) [Pubmed]
  28. Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter. Erickson, J.D., Schafer, M.K., Bonner, T.I., Eiden, L.E., Weihe, E. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  29. Pharmacology of 5-hydroxytryptamine-1A receptors which inhibit cAMP production in hippocampal and cortical neurons in primary culture. Dumuis, A., Sebben, M., Bockaert, J. Mol. Pharmacol. (1988) [Pubmed]
  30. Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. Kursar, J.D., Nelson, D.L., Wainscott, D.B., Baez, M. Mol. Pharmacol. (1994) [Pubmed]
  31. Induction and maintenance of ganglionic long-term potentiation require activation of 5-hydroxytryptamine (5-HT3) receptors. Alkadhi, K.A., Salgado-Commissariat, D., Hogan, Y.H., Akpaudo, S.B. J. Physiol. (Lond.) (1996) [Pubmed]
  32. Release-regulating serotonin 5-HT1D autoreceptors in human cerebral cortex. Maura, G., Thellung, S., Andrioli, G.C., Ruelle, A., Raiteri, M. J. Neurochem. (1993) [Pubmed]
  33. Intracoronary ketanserin after coronary angioplasty. Tousoulis, D., Davies, G., Toutouzas, P. N. Engl. J. Med. (1994) [Pubmed]
  34. Effect of ketanserin on proximal and distal coronary constrictor responses to intracoronary infusion of serotonin in patients with stable angina, patients with variant angina, and control patients. McFadden, E.P., Bauters, C., Lablanche, J.M., Leroy, F., Clarke, J.G., Henry, M., Schandrin, C., Davies, G.J., Maseri, A., Bertrand, M.E. Circulation (1992) [Pubmed]
  35. Evaluation of ketanserin in the prevention of restenosis after percutaneous transluminal coronary angioplasty. A multicenter randomized double-blind placebo-controlled trial. Serruys, P.W., Klein, W., Tijssen, J.P., Rutsch, W., Heyndrickx, G.R., Emanuelsson, H., Ball, S.G., Decoster, O., Schroeder, E., Liberman, H. Circulation (1993) [Pubmed]
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