GAT229

GAT229

Biochem/physiol Actions

GAT229 is the S-(-)-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. GAT229 was found to be a potent, Gαi/o-biased CB1 PAM without intrinsic activity, while the R-(+)-enantiomer, GAT228, was found to be an unbiased CB1 allosteric agonist. In radioligand binding assays, both GAT228 and GAT229 behaved as PAMs of orthosteric ligand binding, with GAT229 exhibiting higher potency and efficacy. 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.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575606 GAT229 white to beige SIGMA-ALDRICH 2-8°C DMSO: 20 mg/mL, clear
£515.36 (exc VAT) per 25MG
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3575607 GAT229 white to beige SIGMA-ALDRICH 2-8°C DMSO: 20 mg/mL, clear
£136.50 (exc VAT) per 5MG
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