| Identification | Back Directory | [Name]
ADX 10059 hydrochloride | [CAS]
757949-98-7 | [Synonyms]
ADX 10059 hydrochloride
2-[(3-Fluorophenyl)ethynyl]-4,6-dimethyl-3-pyridinamine hydrochloride
3-PyridinaMine, 2-[2-(3-fluorophenyl)ethynyl]-4,6-diMethyl-, hydrochloride | [Molecular Formula]
C15H14ClFN2 | [MDL Number]
MFCD22683822 | [MOL File]
757949-98-7.mol | [Molecular Weight]
276.74 |
| Hazard Information | Back Directory | [Uses]
ADX 10059 Hydrochloride is used in the synthetic preparation of novel 2-(hetero)arylalkynylpyridin-3-amines as mGluR5 antagonists. | [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]. | [storage]
Desiccate at RT | [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. |
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