The enhancement of GABA-mediated synaptic transmission underlies the pharma
cotherapy of various neurological and psychiatric disorders, GABA(A) recept
ors are pluripotent drug targets that display an extraordinary structural h
eterogeneity: they are assembled from a repertoire of at least 18 subunits
(alpha1-6, beta1-3, gamma1-3, delta,epsilon,theta, rho1-3). However, differ
entiating defined GABA, receptor subtypes on the basis of function has had
to await recent progress in the genetic dissection of receptor subtypes in
vivo. Evidence that the various actions of allosteric modulators of GABA(A)
receptors, in particular the benzodiazepines, can be attributed to specifi
c GABA(A) receptor subtypes will be discussed, Such discoveries could open
up new avenues for drug development.