ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 potentiated binding of [(3)H]CP55,940 to the CB1 receptor as well as enhancing AEA-stimulated [(35)S]GTPγS binding in mouse brain membranes and β-arrestin recruitment and ERK phosphorylation in hCB1 cells. In the whole animal, ZCZ011 is brain penetrant, increased the potency of these orthosteric agonists in mouse behaviorally bioavailable assays indicative of cannabimimetic activity, including antinociception, hypothermia, catalepsy, locomotor activity, and in the drug discrimination paradigm. ZCZ011 acts as a CB1 PAM and provide the first proof of principle that CB1 PAMs offer a promising strategy to treat neuropathic and inflammatory pain with minimal or no cannabimimetic side effects. References: Ignatowska-Jankowska BM, Baillie GL, Kinsey S, Crowe M, Ghosh S, Owens RA, Damaj IM, Poklis J, Wiley JL, Zanda M, Zanato C, Greig IR, Lichtman AH, Ross RA. A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects. Neuropsychopharmacology. 2015 Dec;40(13):2948-59. doi: 10.1038/npp.2015.148. PubMed PMID: 26052038; PubMed Central PMCID: PMC4864630.

纯度：≥98%

CAS：1998197-39-9