Osanetant
Osanetant Basic information
- Product Name:
- Osanetant
- Synonyms:
-
- Osanetant
- AcetaMide, N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-Methyl-
- 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
- SR142801
- SR-142801
- Osanetant AcetaMide, N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-Methyl-
- N-[1-[3-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N-methylacetamide
- CAS:
- 160492-56-8
- MF:
- C35H41Cl2N3O2
- MW:
- 606.62
- Mol File:
- 160492-56-8.mol
Osanetant Chemical Properties
- Boiling point:
- 727.9±60.0 °C(Predicted)
- Density
- 1.25
- storage temp.
- -20°C
- solubility
- DMSO: soluble15mg/mL, clear
- pka
- 8.33±0.10(Predicted)
- form
- powder
- color
- white to beige
- optical activity
- [α]/D +18 to +24°, c = 1 in methanol
- InChIKey
- DZOJBGLFWINFBF-UMSFTDKQSA-N
- SMILES
- Clc1c(ccc(c1)[C@@]4(CN(CCC4)C(=O)c5ccccc5)CCCN2CCC(CC2)(N(C)C(=O)C)c3ccccc3)Cl
Osanetant Usage And Synthesis
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
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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