Somatostatin (sst) Receptors

Supporting information

Somatostatin (somatotropin release inhibiting factor, SRIF) is an endogenous cyclic polypeptide with two biologically active forms. It is an abundant neuropeptide and has a wide range of physiological effects on neurotransmission, secretion and cell proliferation. The somatostatin receptor family consists of five subtypes, sst1-5, each differentially distributed throughout the central nervous system and periphery. Endogenous somatostatin receptor ligands include somatostatin-14 and somatostatin-28.

Somatostatin receptors have diverse biological functions due to their varied distribution and the fact that they couple to different second messengers - namely adenylyl cyclase, PLC, K+ channels and Ca2+ channels, amongst others.

Somatostatin receptors in the hypothalamus are involved in the regulation of growth hormone secretion. Other hormones regulated by somatostatin receptors include thyrotropin and prolactin. Somatostatin has antiproliferative effects via stimulation of protein tyrosine phosphatase activity and of the MAPK signaling cascade, with subsequent induction of G1 cell cycle arrest (sst1, sst4, sst5) and promotion of apoptosis (sst2, sst3). It also exhibits antiangiogenic activity via activation of sst3. Somatostatin regulates neuronal activity by regulating AMPA/kainate-mediated responses to glutamate. Different sst subtypes have opposing effects in this system.

Somatostatin receptors also play a role in blood glucose homeostasis; sst5 receptors in the pancreatic β-cells stimulate insulin secretion, whilst sst2 receptors are involved in glucagon secretion from α-cells. In addition, sst2 receptors inhibit gastric acid secretion and peristalsis in the jejunum. Somatostatin suppresses the release of numerous gastrointestinal hormones, including gastrin, cholecystokinin, secretin and VIP, and consequently plays an integral role in gastrointestinal endocrinology.

To view external sources of pharmacological information for Somatostatin (sst) Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
sst1 Human SSTR1 NM_001049 P30872
Mouse Sstr1 NM_009216 P30873
Rat Sstr1 NM_012719 P28646
sst2 Human SSTR2 NM_001050 P30874
Mouse Sstr2 NM_001042606 P30875
Rat Sstr2 NM_019348 P30680
View all Somatostatin Receptor Gene Data »

Literature for Somatostatin (sst) Receptors

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A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

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Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

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Peptide Hormone Receptors Product Listing

Peptide Hormone Receptors Product Listing

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Regulation of Vascular Reactivity by GPCRs

Written by J.J. Maguire and A.P. Davenport

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