SB 223412
SB 223412 Basic information
- Product Name:
- SB 223412
- Synonyms:
-
- SB 223412
- 3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide
- (-)-(S)-N-(alpha-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxaMide
- TALNETANT//SB223412//3-hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxaMide
- SB-223412; SB223412; SB 223412
- Talnetant (SB 223412)
- CS-1123
- Talnetant/(S)-3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide
- CAS:
- 174636-32-9
- MF:
- C25H22N2O2
- MW:
- 382.45
- Mol File:
- 174636-32-9.mol
SB 223412 Chemical Properties
- Melting point:
- 125.1-126.2℃
- Boiling point:
- 580.4±50.0 °C(Predicted)
- Density
- 1.212±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: soluble25mg/mL, clear
- pka
- 6.70±0.50(Predicted)
- form
- powder
- color
- white to beige
- optical activity
- [α]/D -25 to -31°, c = 0.5 in methanol
SB 223412 Usage And Synthesis
Description
Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM). It is selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide in isolated rabbit iris sphincter muscle (pD2 = 9.1). Talnetant (5-20 mg/kg) reduces senktide-induced head shakes and tail whips in mice. It also inhibits senktide-induced wet-dog shakes, increases extracellular dopamine and norepinephrine in the medial prefrontal cortex, and attenuates haloperidol-induced increases in nucleus accumbens dopamine levels in guinea pigs.
Uses
Talnetant acts as a neurokinin 3 (NK3) receptor antagonist used as an antispychotic.
in vivo
Talnetant (SB 223412) (0.5-2 mg/kg i.v., 2 min pretreatment) can inhibit the miosis induced by senktide (25 μg, i.v.) in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits[1].
Talnetant (SB 223412) (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs[3].
| Animal Model: | Male Dunkin-Hartley guinea pig[3] |
| Dosage: | 1, 3, 10, 30 or 100?mg/kg |
| Administration: | Intraperitoneal injection; 1 h |
| Result: | Showed a significant attenuation of wet dog shake (WDS) behavior from 31.1 to 16.7 at 30 mg/kg. Significantly increased extracellular DA levels to 238% and NE levels to 227.1%, without affecting 5-HT levels. |
IC 50
NK3
References
[1] H M SARAU. Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.[J]. Journal of Pharmacology and Experimental Therapeutics, 1997, 281 3: 1303-1311.
[2] LEE A DAWSON. In Vitro and In Vivo Characterization of the Non-peptide NK3 Receptor Antagonist SB-223412 (Talnetant): Potential Therapeutic Utility in the Treatment of Schizophrenia[J]. Neuropsychopharmacology, 2007, 33 7: 1642-1652. DOI: 10.1038/sj.npp.1301549
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