Compound class:
Synthetic organic
Comment: GAT211 is an agonist and positive allosteric modulator (ago-PAM) of cannabinoid receptor 1 (CB1R) and is a racemic mixture of GAT228 (R-enantiomer) and GAT229 (S-enantiomer), each of which contribute different components of GAT211's molecular pharmacology. GAT228 provides the CB1R partial agonist activity, whereas PAM activity resides with GAT229 [1].
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References |
1. Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP, Denovan-Wright EM et al.. (2017)
Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor. ACS Chem Neurosci, 8 (6): 1188-1203. [PMID:28103441] |