By controlling spike timing and sculpting neuronal rhythms, inhibitory interneurons play a key role in brain function. GABAergic interneurons are highly diverse. The respective γ-aminobutyric acid (GABA) A receptor subtypes, therefore, provide new opportunities for targeting selective neuronal circuits. In addition, multiple sites for drug interactions are present on GABA A receptor subtypes. Their pharmacological relevance is increasingly being recognized. A new central nervous system (CNS) pharmacology is on the horizon.