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Chemical Compound Review

Osanetant     N-[1-[3-[(3S)-3-(3,4- dichlorophenyl)-1...

Synonyms: CHEMBL346178, SureCN119440, CHEBI:354086, SR-14280, CID219077, ...
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Disease relevance of Osanetant


Psychiatry related information on Osanetant


High impact information on Osanetant

  • In the present study, we have investigated the effects of a tachykinin NK3 receptor antagonist, SR 142801 (osanetant), on cough, bronchoconstriction, and bronchial hyperresponsiveness induced by aerosolized citric acid (0.4 M) in guinea pigs [3].
  • Since the structure and the pharmacology of the human neurokinin receptor resembles that of gerbils, rather than that of mice or rats, we decided to investigate the anxiolytic- and /or antidepressant-like effects of NK1 (SSR240600), NK2 (saredutant) and NK3 (osanetant) receptor antagonists in gerbils [2].
  • However, recent data from clinical trials of selective neurokinin 3 (NK(3)) receptor antagonists in schizophrenia - osanetant and talnetant - have shown significant improvement in positive symptoms, with no major side-effects reported as yet [4].
  • Osanetant was the first potent and selective non-peptide antagonist described for the NK3 tachykinin receptor [176305] [5].

Associations of Osanetant with other chemical compounds

  • In the tonic immobility test in gerbils, saredutant (5-10 mg/kg, i.p.) and osanetant (5-10 mg/kg, i.p.) produced similar effects to those observed with fluoxetine (7.5-15 mg/kg, i.p.), SSR149415 (10-30 mg/kg, p.o.) and buspirone (3 mg/kg, i.p.). Diazepam and SSR240600 were inactive in this paradigm [2].

Analytical, diagnostic and therapeutic context of Osanetant

  • Following phase IIa clinical trials [307656], [328910], [359231], osanetant entered phase IIb development in February 2001 [409432] [5].


  1. Tachykinin receptors antagonists: from research to clinic. Quartara, L., Altamura, M. Current drug targets. (2006) [Pubmed]
  2. Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils. Salomé, N., Stemmelin, J., Cohen, C., Griebel, G. Pharmacol. Biochem. Behav. (2006) [Pubmed]
  3. Involvement of tachykinin NK3 receptors in citric acid-induced cough and bronchial responses in guinea pigs. Daoui, S., Cognon, C., Naline, E., Emonds-Alt, X., Advenier, C. Am. J. Respir. Crit. Care Med. (1998) [Pubmed]
  4. Opinion: NK3 receptor antagonists: the next generation of antipsychotics? Spooren, W., Riemer, C., Meltzer, H. Nature reviews. Drug discovery. (2005) [Pubmed]
  5. Osanetant Sanofi-Synthélabo. Kamali, F. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
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