Regulation of striatal dopamine release by gamma-aminobutyric acid (GABA) neurotransmission was investigated using voltammetry in freely moving rats, following focal injection of the GABA(B) receptor agonist baclofen or the GABA(B) receptor antagonist 5-aminovaleric acid (5-AVA) in either the substantia nigra pars reticulata (SNr) or the substantia nigra pars compacta (SNc). Administration in the SNr of baclofen and 5-AVA at the dose of 2 pg, but not of 0.2 pg, resulted in a decrease and an increase in striatal dopamine release, respectively. In contrast, when injected in the SNc, 5-AVA only produced a transient increase in striatal dopamine release, while baclofen remained ineffective. This suggests that GABA(B) receptors in the SNr, but not the SNc, may play a major role in the control of nigrostriatal dopamine (DA) activity and the release of DA in the striatum.