A potent and selective orexin 2 receptor antagonist for studying Ox2R physiological functions both in cultures and in mice and rats in vivo.
TCS OX2 29 or TCS-OX2-29 is a potent and selective orexin 2 receptor (Ox2R, Ox2-R, Ox-2-R) antagonist (IC50 = 40 nM/Ox2R, >10 μM/Ox1R) with little potency toward 50 other receptors, ion channels, and transporters tested (<30% inhibition at 10 μM). TCS OX2 29 is widely used for elucidating various physiological functions mediated by Ox2R both in cultures and in mice and rats in vivo.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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The identification of potent and selective orexin-2 receptor (OX(2)R) antagonists is described based on the modification of N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogue 1, recently discovered during high throughput screening (HTS). Substitution of an acyl group in 1 with tert-Leucine (tert-Leu), and introduction
Orexins are associated with drug relapse in rodents. Here, we show that acute restraint stress in mice activates lateral hypothalamic (LH) orexin neurons, increases levels of orexin A and 2-arachidonoylglycerol (2-AG) in the ventral tegmental area (VTA), and reinstates extinguished
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