Osanetant

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Osanetant
Systematic (IUPAC) name
N-[1-[3-[(3R)-1-(benzoyl)-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N-methylacetamide
Identifiers
CAS number 160492-56-8
ATC code  ?
PubChem 219077
Chemical data
Formula C35H41Cl2N3O2 
Mol. mass 606.625 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?
Legal status
Routes  ?

Osanetant (SR-142,801) is a neurokinin 3 receptor antagonist developed by Sanofi-Synthélabo, which is being researched for the treatment of schizophrenia.[1] It was the first non-peptide NK3 antagonist developed in the mid-1990s,[2] and has still not made it to market, although clinical trials are continuing.[3] Another potential application for osanetant is in the treatment of drug addiction, as it has been found to block the effects of cocaine in animal models.[4][5]

[edit] References

  1. ^ Kamali F. Osanetant Sanofi-Synthélabo. Current Opinion in Investigational Drugs. 2001 Jul;2(7):950-6. PMID 11757797
  2. ^ Emonds-Alt X, Bichon D, Ducoux JP, Heaulme M, Miloux B, Poncelet M, Proietto V, Van Broeck D, Vilain P, Neliat G, et al. SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor. Life Sciences. 1995;56(1):PL27-32. PMID 7830490
  3. ^ Quartara L, Altamura M. Tachykinin receptors antagonists: from research to clinic. Current Drug Targets. 2006 Aug;7(8):975-92. PMID 16918326
  4. ^ De Souza Silva MA, Mello EL Jr, Müller CP, Jocham G, Maior RS, Huston JP, Tomaz C, Barros M. The tachykinin NK3 receptor antagonist SR142801 blocks the behavioral effects of cocaine in marmoset monkeys. European Journal of Pharmacology. 2006 May 1;536(3):269-78. PMID 16603151
  5. ^ Jocham G, Lezoch K, Müller CP, Kart-Teke E, Huston JP, de Souza Silva MA. Neurokinin receptor antagonism attenuates cocaine's behavioural activating effects yet potentiates its dopamine-enhancing action in the nucleus accumbens core. European Journal of Neuroscience. 2006 Sep;24(6):1721-32. PMID 17004936


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