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Chemical Compound Review

ritanserin     3-[2-[4-[bis(4- fluorophenyl)methylidene]- 1...

Synonyms: Tiserton, Ritanserina, Ritanserine, Ritanserinum, Lopac-R-103, ...
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Disease relevance of ritanserin


Psychiatry related information on ritanserin


High impact information on ritanserin

  • We have recently demonstrated that ritanserin, a serotonin 5-hydroxytryptamine receptor antagonist void of systemic effects, caused a significant reduction of portal pressure in conscious cirrhotic dogs [9].
  • The mechanism by which ritanserin lowers portal pressure is poorly defined [9].
  • Portal vascular resistance decreased significantly (-23%), whereas splanchnic arteriolar resistance was similar before and after ritanserin [9].
  • The requirement for functional 5-HT2B receptors between 8 and 9 days postcoitum is supported by culture of embryos exposed to 5-HT2-specific ligands; 5-HT2B high-affinity antagonist such as ritanserin, induced morphological defects in the cephalic region, heart and neural tube [10].
  • Ritanserin administration to rats subjected to bile duct ligation significantly reduced portal pressure (from 16.2 +/- 1.3 mm Hg to 12.3 +/- 0.7 mm Hg; mean decrease, 22% +/- 5%; p < 0.05) [1].

Chemical compound and disease context of ritanserin


Biological context of ritanserin


Anatomical context of ritanserin


Associations of ritanserin with other chemical compounds


Gene context of ritanserin

  • The latter was abolished by treatment with the 5-HT2 receptor antagonist, ritanserin [27].
  • Risperidone is at least as potent as the specific 5-HT2 receptor antagonist ritanserin in these tests [28].
  • The 5-HT receptor antagonists metergoline (non-specific receptor subtypes 1 and 2), or ritanserin (selective 2C), or GR55562 (selective l B) was injected into the PVN prior to enterostatin (0.01 nmol) injection into the amygdala [29].
  • The LTP-inhibiting effect of DOI (10 microM) was blocked by the 5-HT2,7 receptor antagonist ritanserin (10 microM), but not by the 5-HT1A receptor antagonist NAN-190 (10 microM) nor by the 5-HT3,4 receptor antagonist MDL72222 (10 microM) [30].
  • The 5-HT2 antagonists ketanserin and ritanserin, the 5-HT3 antagonist ICS 205-930 and the alpha 2 adrenoceptor antagonist idazoxan did not oppose the hypophagic effect of mCPP [31].

Analytical, diagnostic and therapeutic context of ritanserin

  • Using conscious dogs, we investigated the effect of the chronic oral administration of a new specific antiserotonergic drug, ritanserin (10 mg per day for 5 days), on portal pressure and systemic hemodynamics [15].
  • Two 5-HT2/1C receptor antagonists, ritanserin (0.05-10.0 mg/kg) and ICI 169.369 (0.3-10.0 mg/kg), were also devoid of specific effects upon defensive analgesia [32].
  • In the present study, this relationship was reevaluated by spectral analysis of the sleep electroencephalogram (EEG) and deconvolution analysis of the plasma GH concentrations during normal nocturnal sleep and after enrichment in SWS by means of ritanserin, a selective 5-HT2 receptor antagonist [33].
  • GBR 12909 reliably maintained self-administration, and ritanserin increased response rate maintained by the highest dose [34].
  • We demonstrated that intraperitoneal injection of 5 mg/kg DOI produced a long-lasting decrease in respiratory frequency and tidal volume, which could be blocked by the antagonist ritanserin [35].


  1. Effects of ritanserin, a selective and specific S2-serotonergic antagonist, on portal pressure and splanchnic hemodynamics in rats with long-term bile duct ligation. Fernández, M., Pizcueta, P., García-Pagán, J.C., Feu, F., Cirera, I., Bosch, J., Rodés, J. Hepatology (1993) [Pubmed]
  2. The effect of ritanserin, a 5-HT2 receptor antagonist, on ischemic cerebral blood flow and infarct volume in rat middle cerebral artery occlusion. Takagi, K., Ginsberg, M.D., Globus, M.Y., Busto, R., Dietrich, W.D. Stroke (1994) [Pubmed]
  3. Serotonergic modulation of ventilation and upper airway stability in obese Zucker rats. Nakano, H., Magalang, U.J., Lee, S.D., Krasney, J.A., Farkas, G.A. Am. J. Respir. Crit. Care Med. (2001) [Pubmed]
  4. Inhibition of acute platelet thrombosis formation in stenosed canine coronary arteries by specific serotonin 5HT2 receptor antagonist ritanserin. Torr, S., Noble, M.I., Folts, J.D. Cardiovasc. Res. (1990) [Pubmed]
  5. The 5-HT2 antagonist ritanserin decreases sleep in cats. Sommerfelt, L., Ursin, R. Sleep. (1993) [Pubmed]
  6. Ritanserin, imipramine, and placebo in the treatment of dysthymic disorder. Bakish, D., Lapierre, Y.D., Weinstein, R., Klein, J., Wiens, A., Jones, B., Horn, E., Browne, M., Bourget, D., Blanchard, A. Journal of clinical psychopharmacology. (1993) [Pubmed]
  7. Ritanserin, a 5-HT2 receptor blocker, as add-on treatment in narcolepsy. Lammers, G.J., Arends, J., Declerck, A.C., Kamphuisen, H.A., Schouwink, G., Troost, J. Sleep. (1991) [Pubmed]
  8. Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice. Gleason, S.D., Shannon, H.E. Psychopharmacology (Berl.) (1997) [Pubmed]
  9. Ritanserin decreases portal pressure in conscious and unrestrained cirrhotic rats. Mastai, R., Giroux, L., Semret, M., Huet, P.M. Gastroenterology (1990) [Pubmed]
  10. 5-HT2B receptor-mediated serotonin morphogenetic functions in mouse cranial neural crest and myocardiac cells. Choi, D.S., Ward, S.J., Messaddeq, N., Launay, J.M., Maroteaux, L. Development (1997) [Pubmed]
  11. Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. Zhang, M., Buttigieg, J., Nurse, C.A. J. Physiol. (Lond.) (2007) [Pubmed]
  12. Interference of ketanserin with baroreflex control of the circulation in the conscious spontaneously hypertensive rat. Smits, J., van Dorsten, F., Struyker Boudier, H. Drugs (1988) [Pubmed]
  13. 8-OH-DPAT, a 5-HT1A agonist and ritanserin, a 5-HT2A/C antagonist, reverse haloperidol-induced catalepsy in rats independently of striatal dopamine release. Lucas, G., Bonhomme, N., De Deurwaerdère, P., Le Moal, M., Spampinato, U. Psychopharmacology (Berl.) (1997) [Pubmed]
  14. Subchronic effects of the GABA-agonist lorazepam and the 5-HT2A/2C antagonist ritanserin on driving performance, slow wave sleep and daytime sleepiness in healthy volunteers. van Laar, M., Volkerts, E., Verbaten, M. Psychopharmacology (Berl.) (2001) [Pubmed]
  15. Serotonin blockade in conscious, unrestrained cirrhotic dogs with portal hypertension. Mastaï, R., Rocheleau, B., Huet, P.M. Hepatology (1989) [Pubmed]
  16. Beneficial effect of serotonin 5-HT2-receptor antagonism on renal blood flow autoregulation in cyclosporin-treated rats. Verbeke, M., Van de Voorde, J., de Ridder, L., Lameire, N. J. Am. Soc. Nephrol. (1999) [Pubmed]
  17. Are 5-hydroxytryptamine7 receptors involved in [3H]5-hydroxytryptamine binding to 5-hydroxytryptamine 1nonA-nonB receptors in rat hypothalamus? Gobbi, M., Parotti, L., Mennini, T. Mol. Pharmacol. (1996) [Pubmed]
  18. Effect of ritanserin, a 5-hydroxytryptamine2-receptor antagonist, on platelet function and thrombin generation at the site of plug formation in vivo. Wagner, B., Schneider, B., Blöchl-Daum, B., Speiser, W., Brenner, B., Eichler, H.G., Lechner, K., Kyrle, P.A. Clin. Pharmacol. Ther. (1990) [Pubmed]
  19. Effects of ritanserin, a selective and specific S2-serotonergic antagonist, on portal pressure and splanchnic hemodynamics in portal hypertensive rats. Nevens, F., Pizcueta, M.P., Fernández, M., Bosch, J., Rodés, J. Hepatology (1991) [Pubmed]
  20. Possible mechanism of action for the attenuation of ethanol intake induced by ritanserin in rats. Panocka, I., Ciccocioppo, R., Polidori, C., Romagnoli, S., Froldi, R., Massi, M. Psychopharmacology (Berl.) (1996) [Pubmed]
  21. Effect of atypical antipsychotic drugs on 5-HT2 receptors in the rat orbito-frontal cortex: an in vivo electrophysiological study. Bergqvist, P.B., Dong, J., Blier, P. Psychopharmacology (Berl.) (1999) [Pubmed]
  22. Effects of ritanserin on transmembrane action potentials in canine Purkinje fibers. Wu, K.M., Hunter, T.L., Proakis, A.G. Proc. Soc. Exp. Biol. Med. (1992) [Pubmed]
  23. The 5-HT2 antagonist ritanserin blocks dopamine re-uptake in the rat frontal cortex. Ruiu, S., Marchese, G., Saba, P.L., Gessa, G.L., Pani, L. Mol. Psychiatry (2000) [Pubmed]
  24. Ritanserin in the treatment of cocaine dependence. Johnson, B.A., Chen, Y.R., Swann, A.C., Schmitz, J., Lesser, J., Ruiz, P., Johnson, P., Clyde, C. Biol. Psychiatry (1997) [Pubmed]
  25. Effect of pharmacologic treatments on the sleep of depressed patients. Sharpley, A.L., Cowen, P.J. Biol. Psychiatry (1995) [Pubmed]
  26. 5-Hydroxytryptamine-stimulated inositol phospholipid hydrolysis in the mouse cortex has pharmacological characteristics compatible with mediation via 5-HT2 receptors but this response does not reflect altered 5-HT2 function after 5,7-dihydroxytryptamine lesioning or repeated antidepressant treatments. Godfrey, P.P., McClue, S.J., Young, M.M., Heal, D.J. J. Neurochem. (1988) [Pubmed]
  27. Functional study of rat 5-HT2A receptors using antisense oligonucleotides. Van Oekelen, D., Megens, A., Meert, T., Luyten, W.H., Leysen, J.E. J. Neurochem. (2003) [Pubmed]
  28. Survey on the pharmacodynamics of the new antipsychotic risperidone. Megens, A.A., Awouters, F.H., Schotte, A., Meert, T.F., Dugovic, C., Niemegeers, C.J., Leysen, J.E. Psychopharmacology (Berl.) (1994) [Pubmed]
  29. 5-HT1B receptors modulate the feeding inhibitory effects of enterostatin. Lin, L., York, D.A. Brain Res. (2005) [Pubmed]
  30. The serotonin 5-HT2 receptor-phospholipase C system inhibits the induction of long-term potentiation in the rat visual cortex. Edagawa, Y., Saito, H., Abe, K. Eur. J. Neurosci. (2000) [Pubmed]
  31. Evidence that hypophagia induced by mCPP and TFMPP requires 5-HT1C and 5-HT1B receptors; hypophagia induced by RU 24969 only requires 5-HT1B receptors. Kennett, G.A., Curzon, G. Psychopharmacology (Berl.) (1988) [Pubmed]
  32. Differential effects of novel ligands for 5-HT receptor subtypes on nonopioid defensive analgesia in male mice. Rodgers, R.J., Shepherd, J.K., Donát, P. Neuroscience and biobehavioral reviews. (1991) [Pubmed]
  33. A quantitative evaluation of the relationships between growth hormone secretion and delta wave electroencephalographic activity during normal sleep and after enrichment in delta waves. Gronfier, C., Luthringer, R., Follenius, M., Schaltenbrand, N., Macher, J.P., Muzet, A., Brandenberger, G. Sleep. (1996) [Pubmed]
  34. Pharmacological interactions between serotonin and dopamine on behavior in the squirrel monkey. Howell, L.L., Czoty, P.W., Byrd, L.D. Psychopharmacology (Berl.) (1997) [Pubmed]
  35. 5-HT(2A/2C) receptor-mediated hypopnea in the newborn rat: relationship to Fos immunoreactivity. Cayetanot, F., Gros, F., Larnicol, N. Pediatr. Res. (2001) [Pubmed]
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