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编 号:F209428
分子式:C25H22N2O2
分子量:382.45
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.

体内研究:
Talnetant (SB 223412) (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis induced by senktide (25μg, iv) in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits.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.Animal Model:Male Dunkin-Hartley guinea pig
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.

体外研究:
Talnetant (SB 223412) (0.1-1?μM) can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor.
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