Presynaptic receptors for virtually all transmitters have been identif
ied throughout the nervous system. Recent studies in the hippocampus p
rovide new insights into the mechanisms by which the activation of the
se receptors leads to presynaptic inhibition of transmitter release, a
nd characterize the second messengers involved in coupling presynaptic
receptors to their effectors. Presynaptic receptors also provide a tr
actable route via which the amount of transmitter release may be selec
tively regulated in therapeutically useful ways.