PSB-CB5 (CID-85469571) is a compound which acts as an

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.orphan receptor In biochemistry, an orphan receptor is a protein that has a similar structure to other identified receptors but whose endogenous ligand has not yet been identified. If a ligand for an orphan receptor is later discovered, the receptor is referred ...

GPR18 ''N''-Arachidonyl glycine receptor (NAGly receptor), also known as G protein-coupled receptor 18 (GPR18), is a protein that in humans is encoded by the ''GPR18'' gene. Along with the other previously orphan receptors GPR55 and GPR119, GPR18 has b ...

, and is the first selective antagonist characterised for this receptor, with an IC₅₀ of 279nM, and good selectivity over related receptors (over 36x selectivity vs CB₁ and

GPR55 G protein-coupled receptor 55 also known as GPR55 is a G protein-coupled receptor that in humans is encoded by the ''GPR55'' gene. GPR55, along with GPR119 and GPR18, have been implicated as novel cannabinoid receptors. History GPR55 was ide ...

, and 14x vs CB₂.) As all previously known antagonists for GPR18 also antagonise GPR55, it has been difficult to separate the effects of these two receptor targets, so the discovery of a selective GPR18 antagonist is expected to be useful in research into the actions of this receptor.

References

{{Cannabinoidergics Cannabinoids

See also

References