The γ-aminobutyric acid B (GABA B) receptor was first demonstrated on presynaptic
terminals where it serves as an autoreceptor and also as a heteroreceptor to influence
transmitter release by suppressing neuronal Ca 2+ conductance. Subsequent studies
showed the presence of the receptor on postsynaptic neurones where activation produces
an increase in membrane K+ conductance and associated neuronal hyperpolarization.(−)-
Baclofen is a highly selective agonist for GABA B receptors, whereas the established GABA …