Talnetant hydrochloride

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CAS NO:

204519-66-4

SB 223412 hydrochloride
SB 223412-A

Talnetant (SB 223412) hydrochloride 是一种选择性、竞争性、脑渗透性的NK3受体拮抗剂，在 hNK-3-CHO 细胞中K_i为 1.4 nM。相对于 hNK-2 受体，Talnetant hydrochloride 对于 hNK-3 有 100 倍的选择性，对 hNK-1 无亲和性。Talnetant hydrochloride 可用于精神分裂症的相关研究。

生物活性

Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeableNK3receptor antagonist with aK_iof 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies^[1]^[2]^[3].

体外研究
(In Vitro)

Talnetant (SB 223412) (0.1-1 μM) hydrochloride can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor^[3].

体内研究
(In Vivo)

Talnetant (SB 223412) hydrochloride (0.5-2 mg/kg iv, 2min pretreatment) can inhibit the miosis induced by senktide (25μg, iv) in a dose-dependent manner with an ED₅₀of 0.44mg/kg in conscious rabbits^[1].
Talnetant (SB 223412) hydrochloride (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.

Clinical Trial

分子量

418.92

Formula

C₂₅H₂₃ClN₂O₂

CAS 号

204519-66-4

中文名称

盐酸他奈坦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.