Biological Activity
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].
References
[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.
