化学性质:
规格 | 10mg 50mg |
CAS | 757949-98-7 |
别名 |
|
化学名 | 2-((3-fluorophenyl)ethynyl)-4,6-dimethylpyridin-3-amine hydrochloride |
分子式 | C15H13FN2.HCl |
分子量 | 276.74 |
溶解度 | <6.92mg/ml in H2O; <27.67mg/ml in DMSO |
储存条件 | Desiccate at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
ADX 10059 hydrochloride is a potent and selective negative allosteric modulator of mGlu5 receptor with IC50 value of 17.1 nM [1].
Metabotropic glutamate receptor 5 (mGlu5 receptor) is a G protein-coupled receptor and is a receptor for glutamate, which is a primary neurotransmitter involved in signaling in the central nervous system [2].
ADX 10059 hydrochloride is a potent and selective mGlu5 receptor negative allosteric modulator. In patients with migraine, ADX10059 caused pain-free response in 16.1% patients compared with placebo of 4.5% [1]. In patients with gastro-oesophageal reflux disease (GORD) underwent 24-h oesophageal pH-metry, ADX10059 (250 mg) significantly reduced the percentage of acid exposure time with pH < 4 from 7.2% to 3.6%. Also, ADX 10059 significantly decreased the duration and number of symptomatic reflux episodes and reduced oesophageal acid exposure [2].
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