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品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D 80 to 94°, c = 1 in methanol
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O=[N+]([O-])C[C@H](C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42
生化／生理作用
GAT228 is the R-(+)-enantiomer of GAT211, a positive allosteric modulator (PAM) of cannabinoid CB1 receptor signaling that was found to amplify the therapeutic effect of endocannabinoids without the negative side effects of psychoactivity or tolerance. GAT228 was found to be an unbiased CB1 allosteric agonist, while the S-(-)-enantiomer, GAT229,was found to be a potent, Gαi/o-biased CB1 PAM without intrinsic activity. In radioligand binding assays, both GAT228 and GAT229 behaved as PAMs of orthosteric ligand binding. Allosteric CB1R activation by GAT211 and its enantiomers could be a better therapeutic strategy for enhancing endogenous cannabinergic activity than targeting endocannabinoid-degrading enzymes with small-molecule inhibitors, with a lower likelihood of tolerance and dependence.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Robert B Laprairie et al.
ACS chemical neuroscience, 8(6), 1188-1203 (2017-01-20)
The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G protein-coupled receptors in brain, and its participation in various (patho)physiological processes has made CB1R activation a viable therapeutic modality. Adverse psychotropic effects limit the clinical utility
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