| Identification | Back Directory | [Name]
Osanetant | [CAS]
160492-56-8 | [Synonyms]
SR142801
SR-142801
Osanetant
Osanetant >=98% (HPLC)
N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N-methylacetamide
N-[1-[3-[(3R)-1-Benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-methylacetamide
(R)-N-{{3-[1-Benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamine
AcetaMide, N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-Methyl-
Osanetant AcetaMide, N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-Methyl- | [Molecular Formula]
C35H41Cl2N3O2 | [MDL Number]
MFCD00938554 | [MOL File]
160492-56-8.mol | [Molecular Weight]
606.62 |
| Chemical Properties | Back Directory | [Boiling point ]
727.9±60.0 °C(Predicted) | [density ]
1.25 | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble15mg/mL, clear | [form ]
powder | [pka]
8.33±0.10(Predicted) | [color ]
white to beige | [Optical Rotation]
[α]/D +18 to +24°, c = 1 in methanol |
| Hazard Information | Back Directory | [Uses]
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia[1]. | [Biochem/physiol Actions]
Osanetant is a selective antagonist of neurokinin 3 receptor NK3. Neurokinins (tachykinins) are members of a family of at least three neuropeptides, substance P, neurokinin A, and neurokinin B (NKB), with each mediating their biological effects through binding to a preferred G-protein-coupled receptor termed NK1, NK2, or NK3, respectively. All three NK receptors are expressed in regions of the central nervous system that are related to emotion and cognition (i.e., amygdala and hippocampus) and have been linked to various degrees in psychiatric disorders. Neurokinin receptors, including NK3 receptors, are also expressed in the motor and sensory systems of the digestive tract. Osanetant was in clinical trials for both irritable bowel syndrome and schizophrenia. | [in vivo]
Osanetant (SR142801; po; 1-10 mg/kg; 60 min before testing) significantly increases social interaction time[1].
Osanetant (ip; 5 and 10 mg/kg; 30 min before testing) decreases immobility time[1].
| Animal Model: | Male Mongolian gerbils of 7 weeks old (50-60 g)[1] | | Dosage: | 1, 3 and 10 mg/kg | | Administration: | Po; 60 min before testing | | Result: | Significantly increased social interaction time.
|
| [IC 50]
NK3 | [storage]
Store at -20°C | [References]
[1] Salomé N, et al. Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils. Pharmacol Biochem Behav. 2006 Apr;83(4):533-9. DOI:10.1016/j.pbb.2006.03.013 |
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