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 chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

at the former

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 t ...

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 ...

, 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 In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian unit ...

, 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.

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{{Cannabinoidergics Cannabinoids

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