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, sst_1-5, 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
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Literature for Somatostatin (sst) Receptors

Cardiovascular Poster

Written by Janet Maguire and Anthony Davenport, this poster summarizes different GPCR classes of the vascular system and their cognate ligands. The predominant vasoactive response of blood vessels to specific receptor activation is also described. Endogenous ligands and Tocris compounds are listed.

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7-TM Receptor Signaling Poster

Written by Terry Kenakin et al, this poster highlights the multiple behaviors of seven-transmembrane (7-TM) receptors, including G-protein-dependent and -independent signaling and the concept of collateral efficacy. Compounds available from Tocris are listed.

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Regulation of Vascular Reactivity by GPCRs

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

'Regulation of Vascular Reactivity by G-protein-coupled Receptors' summarizes the key GPCRs regulating vascular reactivity.

7-TM Receptor Signaling

Written by T. Kenakin et al

'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy

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