GABA B Modulators

The GABA-B receptor is a heterodimeric G protein-coupled receptor built from a GABBR1 and a GABBR2 subunit: only GABBR1 appears to bind agonists, while GABBR2 mediates coupling to the G proteins, and signalling inhibits adenylate cyclase, activates potassium channels and inactivates voltage-dependent calcium channels. This class, however, has no verifiable content. UniProt Q9UBS5 carries no activity-regulation record and names no allosteric modulator of the receptor - only (-)-baclofen as an activator and phaclofen as a blocker - and the MED-RT class cited holds a single drug, secobarbital, which is also filed in the GABA-A modulator class N0000000118 and whose modulator action is at GABA-A. Until a drug with documented GABA-B allosteric modulation is placed here, this class should not be used to describe a mechanism.