The cannabinoid CB₂ receptor positive allosteric modulator EC21a exhibits complicated pharmacology <i>in vitro</i>.

ABSTRACT: Schizophrenia is a complex disease involving the dysregulation of numerous brain circuits and patients exhibit positive symptoms (hallucinations, delusions), negative symptoms (anhedonia), and cognitive impairments. We have shown that the antipsychotic efficacy of positive allosteric modulators (PAMs) of both the M₄ muscarinic receptor and metabotropic glutamate receptor 1 (mGlu₁) involve the retrograde activation of the presynaptic cannabinoid type-2 (CB₂) receptor, indicating that CB₂ activation or potentiation could result in a novel therapeutic strategy for schizophrenia. We used two complementary assays, receptor-mediated phosphoinositide hydrolysis and GIRK channel activation, to characterize a CB₂ PAM scaffold, represented by th

SUBMITTER: Qi A 

PROVIDER: S-EPMC11636628 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature