SNAP 94847 (hydrochloride)

中文名称:

SNAP 94847 (hydrochloride)

中文同义词:

英文名称:

SNAP 94847 (hydrochloride)

英文同义词:

SNAP 94847 HCL

CAS号:

1781934-47-1

分子式:

分子量:

0

EINECS号:

相关类别:

API

Mol文件:

Mol File

生物活性

SNAP 94847 hydrochloride 是一种具有抗抑郁样活性的新型高亲和力选择性黑色素浓缩激素受体1 (MCHR1) 拮抗剂。SNAP 94847 hydrochloride 以高亲和力结合大小鼠 MCHR1，与其他 GPCR，离子通道，酶和转运蛋白具有最小的交叉反应性。SNAP 94847 hydrochloride 是 MCH 诱发的肌醇磷酸形成的高亲和力拮抗剂 (pA2=7.81)。

靶点

Ki: 2.2 nM (MCHR1); Kd: 530 pM (MCHR1)

体内研究

SNAP 94847 hydrochloride (oral gavage; 20 mg/kg; 14 days) shows an exaggerated locomotor response to acute quinpirole [treatment: F(2,19)=11.31, treatment × time: F(34,323) = 4.061], the effect of SNAP 94847 on quinpirole-evoked ambulations over the entire observation period is significant compared to the untreated animals. SNAP 94847 hydrochloride (oral administration; 20 mg/kg; 21 days) in drink water, produces a significant increase in ambulation relative to untreated animals [treatment: F(3,28) = 8.971; treatment × time: F(51,476)=11.50]. shows a marked increase in locomotion is apparent after 40 min in the SNAP 94847-treated group,this effect is significant over 180 min. SNAP 94847 hydrochloride (oral administration; 10 mg/kg), has a good bioavailability (59%), low plasma and blood clearances of 4.2 L/hr/kg and 3.3 L/hr/kg, respectively, and the half-life was shown to be 5.2 h in rats in a PK study. Animal Model: Rat Dosage: 20 mg/kg Administration: Oral administration; 20 mg/kg; 14 days Result: Exhibited a exaggerated locomotor response to acute quinpirole. Animal Model: Rat Dosage: 10 mg/kg Administration: Oral administration; 10 mg/kg Result: Exhibited good physicochemical properties in rats.

Animal Model:

Rat

Dosage:

20 mg/kg

Administration:

Oral administration; 20 mg/kg; 14 days

Result:

Exhibited a exaggerated locomotor response to acute quinpirole.

Animal Model:

Rat

Dosage:

10 mg/kg

Administration:

Oral administration; 10 mg/kg

Result:

Exhibited good physicochemical properties in rats.