Talnetant

Research use only, not for human use.

Talnetant is a selective competitive brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission.

Talnetant is a selective competitive brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission.(In Vitro):Talnetant (SB 223412) (0.1-1?μM) can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor.(In Vivo):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.

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

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.

SB 223412

GPCR/G Protein

Neurokinin Receptor

NK3

Metabolic Disease

Chronic obstructive pulmonary disease; Cough; Irritable bowel syndrome

174636-32-9

382.45

C25H22N2O2

>98% (HPLC)

DMSO:100 mg/mL (261.47 mM)

CCC(NC(=O)c1c(O)c(-c2ccccc2)nc2ccccc12)c1ccccc1

3-hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years