Negative allosteric modulator at mGlu5
CAS：757949-98-7
分子式：C15H13FN2.HCl
分子量：276.74
纯度：98%
存储：Store at -20°C

Background:

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].

参考文献:
[1].  Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine Expert Opin Investig Drugs, 2010, 19(4): 555-561.
[2].  Keywood C, Wakefield M, Tack J. A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease. Gut, 2009, 58(9): 1192-1199.