The neuropeptide somatostatin (SRIF) is widely expressed in the brain
and in the periphery in two main forms, SRIF-14 and SRIF-28. Similarly
, the presence of SRIF receptors throughout the whole body has been re
ported. SRIF produces a variety of effects including modulation of hor
mone release (e.g. GH, glucagon, insulin), of neurotransmitter release
(e.g. acetylcholine, dopamine, 5-HT), and its own release is modulated
by many neurotransmitters. SRIF affects cognitive and behavioural pro
cesses, the endocrine system, the gastrointestinal tract and the cardi
ovascular system and also has tumor growth inhibiting effects. Initial
ly, two classes of SRIF receptors have been proposed on the basis of b
iochemical and functional studies. However, the recent cloning of five
putative SRIF receptor subtypes which belong to the G-protein coupled
receptor superfamily suggests that SRIF mediates its various effects
via a whole family of receptors. Here we review, in this new context,
the molecular pharmacology of the SRIF receptor subtypes present in th
e brain and in the periphery, and address the question of nomenclature
of SRIF receptors.