阿拉莫林盐酸盐

中文名称:

阿拉莫林盐酸盐

中文同义词:

盐酸阿拉莫林;阿拉莫林盐酸盐;饥饿素受体(GHRELIN RECEPTOR)激动剂(ANAMORELIN HYDROCHLORIDE)

英文名称:

AnaMorelin hydrochloride

英文同义词:

AnaMorelin hydrochloride;ONO-7643 hydrochloride;RC 1291 hydrochloride;AnaMorelin HCl;(3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid trimethylhydrazide monohydrochloride;RC 1291 HCl;Anamorelin (RC-1291) HCl;Anamorelin hydrochloride (RC-1291 hydrochloride

CAS号:

861998-00-7

分子式:

C31H43ClN6O3

分子量:

583.16452

EINECS号:

相关类别:

细胞生物学试剂;医用原料;医药原料药-科研原料;医用原料

Mol文件:

861998-00-7.mol

生物活性

Anamorelin (RC-1291) hydrochloride 是一种有效的 ghrelin receptor 激动剂，FLIPR 检测中，EC50 为 0.74 nM。

靶点

Ki: 0.7 nM (ghrelin receptor) EC50: 0.74 nM (ghrelin receptor)

体外研究

In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC 50 value of 0.74 nM. No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000 nM. In the binding experiments, Anamorelin binds to the ghrelin receptor with a binding affinity constant (K i ) of 0.70 nM. In the competition assay with radiolabeled ibutamoren ( 35 S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC 50 =0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC 50 ) is 1.5 nM. Anamorelin is screened for activity against a set of over 100 receptors, ion channels, transporters, and enzymes. Anamorelin demonstrates binding to the tachykinin neurokinin 2 (NK 2 ) site (IC 50 =0.021 μM); however, a subsequent NK 2 functional assay demonstrates no functional activity.

体内研究

In rats, Anamorelin (ANAM) at an oral dose of 3, 10, or 30 mg/kg once daily significantly increases both food intake and body weight from Day 2 to Day 7 of treatment compared with the vehicle control. The cumulative change in food intake and weight gain increases dose-dependently, and these changes are significant at all dose levels (P<0.05) compared to the control. Administration of Anamorelin at a single oral dose of 3, 10, or 30 mg/kg induces a dose-dependent increase in plasma GH levels and GH AUC 0-6h in rats.