1-((3-(4-Chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1H-purin-6(7H)-one, 1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-Purin-6-one, AM 0902, AMG0902
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AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca2+ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.
Brain-penetrant, orally active, potent and selective transient receptor potential A1 (TRPA1) antagonist with efficacy against AITC-induced flinching in rats in vivo.
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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The transient receptor potential ankyrin 1 (TRPA1) channel has been implicated in pathophysiological processes that include asthma, cough, and inflammatory pain. Agonists of TRPA1 such as mustard oil and its key component allyl isothiocyanate (AITC) cause pain and neurogenic inflammation
Journal of medicinal chemistry, 59(6), 2794-2809 (2016-03-05)
There has been significant interest in developing a transient receptor potential A1 (TRPA1) antagonist for the treatment of pain due to a wealth of data implicating its role in pain pathways. Despite this, identification of a potent small molecule tool
The anthelmintic praziquantel (±PZQ) serves as a highly effective antischistosomal therapy. ±PZQ causes a rapid paralysis of adult schistosome worms and deleterious effects on the worm tegument. In addition to these activities against the parasite, ±PZQ also modulates host vascular
Cancer cell survival is dependent on oxidative-stress defenses against reactive oxygen species (ROS) that accumulate during tumorigenesis. Here, we show a non-canonical oxidative-stress defense mechanism through TRPA1, a neuronal redox-sensing Ca2+-influx channel. In TRPA1-enriched breast and lung cancer spheroids, TRPA1
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