Substituted imidazolylmethyl pyridine and pyrazine derivatives that bind to GABA_A receptors are provided. Such compounds may be used to modulate ligand binding to GABA_A receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABA_A receptors (e.g., receptor localization studies).