EC21a

EC21a (also known as VU6043295) is a synthetic small molecule positive allosteric modulator (PAM) of the cannabinoid receptor type 2 (CB2). It was originally discovered by researchers at the University of Pisa, University of Florence, and University of Aberdeen by modifying the structure of 2-oxopyridine-3-carboxamide derivatives. EC21a acts by binding to an allosteric site on the CB2 receptor, enhancing the binding and signaling efficiency of orthosteric agonists such as CP55940 and 2-arachidonoylglycerol (2-AG). Preclinical studies have demonstrated that EC21a possesses antinociceptive efficacy in animal models of neuropathic pain, increases resistance to induced seizures in wild-type and SCN1A-mutant epilepsy mouse models, and exhibits antipsychotic-like efficacy in rodent models of schizophrenia. However, in vitro characterization has also revealed complex, assay-dependent pharmacology, including inverse agonist activity at CB2 and mixed agonist/negative allosteric modulator activity at CB1.

Other names

Ec21aEc-21aEc 21aN-(1,2-dihydro-4-methyl-2-oxopyridin-3-yl)cycloheptanecarboxamide