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ADX 10059 hydrochloride is a chemical compound that serves as a key intermediate in the synthesis of novel 2-(hetero)arylalkynylpyridin-3-amines, which are known as mGluR5 antagonists.

757949-98-7

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757949-98-7 Usage

Uses

Used in Pharmaceutical Industry:
ADX 10059 hydrochloride is used as a synthetic precursor for the development of mGluR5 antagonists, which are compounds that target and inhibit the activity of the metabotropic glutamate receptor 5 (mGluR5). These antagonists have potential therapeutic applications in the treatment of various neurological and psychiatric disorders, such as anxiety, depression, and schizophrenia, due to their ability to modulate glutamate signaling pathways in the brain.

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.

Check Digit Verification of cas no

The CAS Registry Mumber 757949-98-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,5,7,9,4 and 9 respectively; the second part has 2 digits, 9 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 757949-98:
(8*7)+(7*5)+(6*7)+(5*9)+(4*4)+(3*9)+(2*9)+(1*8)=247
247 % 10 = 7
So 757949-98-7 is a valid CAS Registry Number.

757949-98-7Downstream Products

757949-98-7Relevant academic research and scientific papers

Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

Font, Joan,López-Cano, Marc,Notartomaso, Serena,Scarselli, Pamela,Di Pietro, Paola,Bresolí-Obach, Roger,Battaglia, Giuseppe,Malhaire, Fanny,Rovira, Xavier,Catena, Juanlo,Giraldo, Jesús,Pin, Jean-Philippe,Fernández-Due?as, Víctor,Goudet, Cyril,Nonell, Santi,Nicoletti, Ferdinando,Llebaria, Amadeu,Ciruela, Francisco

, (2017)

Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type

NOVEL AMINOPYRIDINE DERIVATIVES AS mGIuR5 ANTAGONISTS

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Page 17, (2008/06/13)

The invention relates to novel aminopyridine derivatives of formula (I) wherein R1 is methyl an R4 and amino group NR6R7 and R5 forms an arylalkynyl- or heteroarylalkynyl-group. The compounds are useful in the p

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