GABABRs are similar in structure to and in the same receptor family with metabotropic glutamate receptors. There are two subtypes of the receptor, GABAB1 and GABAB2, and these appear to assemble as heterodimers in neuronal membranes by linking up by their intracellular C termini.
It is speculated that binding of GABA causes the subunits to swing shut around the agonist like a venus fly trap.
Agonists and antagonists
Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy.
Saclofen, phaclofen and SCH-50911 are selective GABAB antagonists.
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