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Ritanserin chemical structure

IUPAC name
CAS number
ATC code


Chemical formula {{{chemical_formula}}}
Molecular weight 477.569 g/mol
Elimination half-life
Pregnancy category
Legal status
Routes of administration

Ritanserin is a serotonin antagonist with wide-reaching possibilities for the treatment of many neurological disorders.

When used together with typical antipsychotics in the treatment of schizophrenia is able to decrease negative symptoms and adds some "atypicality" as parkinsonism is slightly decreased.

Possible effects on platelets have also been proposed.[1]


Ritanserin is a 5-HT2 receptor antagonist[2] (Ki = 0.39 nM). It has anxiolytic effects in vivo.


  1. Wagner B, Schneider B, Blöchl-Daum B, et al (October 1990). Effect of ritanserin, a 5-hydroxytryptamine2-receptor antagonist, on platelet function and thrombin generation at the site of plug formation in vivo. Clinical pharmacology and therapeutics 48 (4): 419–23.
  2. Akhondzadeh S, Malek-Hosseini M, Ghoreishi A, Raznahan M, Rezazadeh SA (September 2008). Effect of ritanserin, a 5HT2A/2C antagonist, on negative symptoms of schizophrenia: A double-blind randomized placebo-controlled study. Progress in neuro-psychopharmacology & biological psychiatry.

Further readingEdit


  • Baldwin, D. S. (2000). Dysthymia: Options in pharmacotherapy. Kwai Chung, Hong Kong: Adis International Publications.


  • Abi-Saab, W., Seibyl, J. P., D'Souza, D. C., Karper, L. P., Gueorgueva, R., Abi-Dargham, A., et al. (2002). Ritanserin antagonism of m-chlorophenylpiperazine effects in neuroleptic-free schizophrenics patients: Support for serotonin-2 receptor modulation of schizophrenia symptoms: Psychopharmacology Vol 162(1) Jun 2002, 55-62.
  • Amargos-Bosch, M., Lopez-Gil, X., Artigas, F., & Adell, A. (2006). Clozapine and olanzapine, but not haloperidol, suppress serotonin efflux in the medial prefrontal cortex elicited by phencyclidine and ketamine: International Journal of Neuropsychopharmacology Vol 9(5) Oct 2006, 565-573.
  • Bach, M., Aigner, M., & Lenz, G. (1997). Ritanserin as adjunct to fluoxetine treatment of OCD patients with psychotic features: Pharmacopsychiatry Vol 30(1) Jan 1997, 28-29.
  • Bollweg, G., & Sparber, S. (1996). Ritanserin blocks DOI-altered embryonic motility and posthatch learning in the developing chicken: Pharmacology, Biochemistry and Behavior Vol 55(3) Nov 1996, 397-403.
  • Bollweg, G., Wei, Y. X., & Sparber, S. B. (1998). Behavioral and neuroendocrine assessment of ritanserin exposure in the developing chicken: Lack of toxicity at effective doses: Pharmacology, Biochemistry and Behavior Vol 60(1) May 1998, 175-181.
  • Bubenikova-Valesova, V., Stuchlik, A., Svoboda, J., Bures, J., & Vales, K. (2008). Risperidone and ritanserin but not haloperidol block effect of dizocilpine on the active allothetic place avoidance task: PNAS Proceedings of the National Academy of Sciences of the United States of America Vol 105(3) Jan 2008, 1061-1066.
  • Ciccocioppo, R., Panocka, I., Stefanini, E., Gessa, G. L., & et al. (1995). Low responsiveness to agents evoking 5-HT-sub-2 receptor-mediated behaviors in Sardinian alcohol-preferring rats: Pharmacology, Biochemistry and Behavior Vol 51(1) May 1995, 21-27.
  • Clementi, G., Valerio, C., Emmi, I., Prato, A., & et al. (1996). Behavioral effects of amylin injected intracerebroventricularly in the rat: Peptides Vol 17(4) 1996, 589-591.
  • Cornish, J. W., Maany, I., Fudala, P. J., Ehrman, R. N., Robbins, S. J., & O'Brien, C. P. (2001). A randomized, double-blind, placebo-controlled study of ritanserin pharmacotherapy for cocaine dependence: Drug and Alcohol Dependence Vol 61(2) Jan 2001, 183-189.
  • de Leeuw, A. S., & Westenberg, H. G. M. (2008). Hypersensitivity of 5-HT-sub-2 receptors in OCD patients an increased prolactin response after a challenge with meta-chlorophenylpiperazine and pre-treatment with ritanserin and placebo: Journal of Psychiatric Research Vol 42(11) Sep 2008, 894-901.
  • de Lima, M. S., Hotoph, M., & Wessely, S. (1999). The efficacy of drug treatments for dysthymia: A systematic review and meta-analysis: Psychological Medicine Vol 29(6) Nov 1999, 1273-1289.
  • de Mello Cruz, A. P., Pinheiro, G., Alves, S. H., Ferreira, G., Mendes, M., Faria, L., et al. (2005). Behavioral effects of systemically administered MK-212 are prevented by ritanserin microinfusion into the basolateral amygdala of rats exposed to the elevated plus-maze: Psychopharmacology Vol 182(3) Nov 2005, 345-354.
  • Den Boer, J. A., Vahlne, J. O., Post, P., Heck, A. H., Daubenton, F., & Olbrich, R. (2000). Ritanserin as add-on medication to neuroleptic therapy for patients with chronic or subchronic schizophrenia: Human Psychopharmacology: Clinical and Experimental Vol 15(3) Apr 2000, 179-189.
  • Detari, L., Szentgyorgyi, V., Hajnik, T., Szenasi, G., Gacsalyi, I., & Kukorelli, T. (1999). Differential EEG effects of the anxiolytic drugs, deramciclane (EGIS-3886), ritanserin and chlordiazepoxide in rats: Psychopharmacology Vol 142(3) Mar 1999, 318-326.
  • Ehrman, R. N., Robbins, S. J., Cornish, J. W., Childress, A. R., & O'Brien, C. P. (1996). Failure of ritanserin to block cocaine cue reactivity in humans: Drug and Alcohol Dependence Vol 42(3) Nov 1996, 167-174.
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  • Fletcher, P. J. (1998). A comparison of the effects of risperidone, raclopride, and ritanserin on intravenous self-administration of d-amphetamine: Pharmacology, Biochemistry and Behavior Vol 60(1) May 1998, 55-60.
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  • Kuroki, T., Kawahara, T., Yonezawa, Y., & Tashiro, N. (1999). Effects of the serotonin-sub(2A/2C ) receptor agonist and antagonist on phencyclidine-induced dopamine release in rat medial prefrontal cortex: Progress in Neuro-Psychopharmacology & Biological Psychiatry Vol 23(7) Oct 1999, 1259-1275.
  • Lucas, G., Bonhomme, N., De Deurwaerdere, P., Le Moal, M., & Spampinato, U. (1997). 8-OH-DPAT, a 5-HT-sub(1A ) agonist and ritanserin, a 5-HTsuperscript 2A/C ) antagonist, reverse haloperidol-induced catalepsy in rats independently of striatal dopamine release: Psychopharmacology Vol 131(1) May 1997, 57-63.
  • Lundberg, T., Lindstrom, L., Hartvig, P., Reibring, L., & et al. (1996). Serotonin-2 and dopamine-1 binding components of clozapine in frontal cortex and striatum in the human brain visualized by positron emission tomography: Psychiatry Research: Neuroimaging Vol 67(1) May 1996, 1-10.
  • Mayer, G. (2003). Ritanserin Improves Sleep Quality in Narcolepsy: Pharmacopsychiatry Vol 36(4) Jul 2003, 150-155.
  • Mazzola-Pomietto, P., Aulakh, C. S., Tolliver, T., & Murphy, D. L. (1997). Functional subsensitivity of 5-HT-sub(2A) and 5-HT-sub(2C) receptors mediating hyperthermia following acute and chronic treatment with 5-HT-sub(2A/2C) receptor antagonists: Psychopharmacology Vol 130(2) Mar 1997, 144-151.
  • McLean, J. H., Darby-King, A., & Hodge, E. (1996). 5-HT-sub-2 receptor involvement in conditioned olfactory learning in the neonate rat pup: Behavioral Neuroscience Vol 110(6) Dec 1996, 1426-1434.
  • Naghdi, N., & Harooni, H. E. (2005). The effect of intrahippocampal injections of ritanserin (5HT-sub(2A/2C) antagonist) and granisetron (5HT-sub-3 antagonist) on learning as assessed in the spatial version of the water maze: Behavioural Brain Research Vol 157(2) Feb 2005, 205-210.
  • Naghdi, N., Rezaei, M., & Fathollahi, Y. (2006). Microinjection of ritanserin into the CA1 region of hippocampus improves scopolamine-induced amnesia in adult male rats: Behavioural Brain Research Vol 168(2) Mar 2006, 215-220.
  • Naranjo, C. A., Bremner, K. E., & Poulos, C. X. (1996). Research strategies to assess pharmacotherapies for alcoholism: Progress in Neuro-Psychopharmacology & Biological Psychiatry Vol 20(4) May 1996, 543-560.
  • O'Neill, M. F., Heron-Maxwell, C. L., & Shaw, G. (1999). 5-HT-sub-2 receptor antagonism reduces hyperactivity induced by amphetamine, cocaine and MK-801 but not D-sub-1 agonist C-APB: Pharmacology, Biochemistry and Behavior Vol 63(2) Jun 1999, 237-243.
  • Overstreet, D. H., Knapp, D. J., Moy, S. S., & Breese, G. R. (2003). A 5-HT1A agonist and a 5-HT2C antagonist reduce social interaction deficit induced by multiple ethanol withdrawals in rats: Psychopharmacology Vol 167(4) Jun 2003, 344-352.
  • Panocka, I., Ciccocioppo, R., Polidori, C., & Romagnoli, S. (1996). Possible mechanism of action for the attenuation of ethanol intake induced by ritanserin in rats: Psychopharmacology Vol 128(2) Nov 1996, 181-190.
  • Pitchot, W., Wauthy, J., Legros, J.-J., & Ansseau, M. (2004). Hormonal and temperature responses to flesinoxan in normal volunteers: An antagonist study: European Neuropsychopharmacology Vol 14(2) Mar 2004, 151-155.
  • Poyurovsky, M., Epshtein, S., Fuchs, C., Schneidman, M., Weizman, R., & Weizman, A. (2003). Efficacy of low-dose mirtazapine in neuroleptic-induced akathisia: A double-blind randomized placebo-controlled pilot study: Journal of Clinical Psychopharmacology Vol 23(3) Jun 2003, 305-308.
  • Prinssen, E. P. M., Kleven, M. S., & Koek, W. (1996). Effects of dopamine antagonists in a two-way active avoidance procedure in rats: Interactions with 8-OH-DPAT, ritanserin, and prazosin: Psychopharmacology Vol 128(2) Nov 1996, 191-197.
  • Raghavendra, V., & Kulkarni, S. K. (2000). Melatonin reversal of DOI-induced hypophagia in rats: Possible mechanism by suppressing 5-HT-sub(2A ) receptor-mediated activation of HPA axis: Brain Research Vol 860(1-2) Mar 2000, 112-118.
  • Rex, A., Voigt, P., & Fink, H. (1998). Pharmacological evaluation of a modified open-field test sensitive to anxiolytic drugs: Pharmacology, Biochemistry and Behavior Vol 59(3) Mar 1998, 677-683.
  • Sanchez, H., & Velazquez-Martinez, D. N. (2001). Discriminative stimulus properties of indorenate, a 5-HT-sub(1A), 5-HT-sub(1B ) and 5-HT-sub(2C ) agonist: A study in rats: Journal of Psychopharmacology Vol 15(1) 2001, 29-36.
  • Schenk, S. (2000). Effects of the serotonin 5-HT-sub-2 antagonist, ritanserin, and the serotonin 5-HT-sub(1A ) antagonist, WAY 100635, on cocaine-seeking in rats: Pharmacology, Biochemistry and Behavior Vol 67(2) Oct 2000, 363-369.
  • Schrott, L. M., Getty, M. E., Wacnik, P. W., & Sparber, S. B. (1998). Open-field and LPS-induced sickness behavior in young chickens: Effects of embryonic cocaine and/or ritanserin: Pharmacology, Biochemistry and Behavior Vol 61(1) Sep 1998, 9-17.
  • Shadach, E., Gaisler, I., Schiller, D., & Weiner, I. (2000). The latent inhibition model dissociates between clozapine, haloperidol, and ritanserin: Neuropsychopharmacology Vol 23(2) Aug 2000, 151-161.
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