Nomenclature: sst3 receptor

Family: Somatostatin receptors

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 418 22q13.1 SSTR3 somatostatin receptor 3 6,51-52
Mouse 7 428 15 E1 Sstr3 somatostatin receptor 3 54
Rat 7 428 7q34 Sstr3 somatostatin receptor 3 29
Previous and Unofficial Names
SSTR3
SRIF1
SRIF1C
SSTR
Smstr28
SS-3-R
SS3-R
SS3R
SSR-28
somatostatin receptor 28
somatostatin receptor 3
somatostatin receptor subtype 3
somatostatin receptor type 3
sst3
Smstr-3
Smstr3
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
CST-14 {Sp: Mouse, Rat}
CST-17 {Sp: Human}
SRIF-14 {Sp: Human, Mouse, Rat}
SRIF-28 {Sp: Human, Mouse, Rat}
Comments: SRIF-14 and SRIF-28 are the active fragments of precursor somatostatin
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]Tyr10-CST14 Hs Full agonist 10.1 pKd 45-46
pKd 10.1 [45-46]
[125I]LTT-SRIF-28 Hs Full agonist 9.4 – 10.3 pKd 6,38,45-46
pKd 9.7 – 10.3 [6,45-46]
pKd 9.4 [38]
[125I]CGP 23996 Hs Full agonist 9.8 pKd 46
pKd 9.8 [46]
[125I]Tyr7-Sst3-ODN-8 Hs Full agonist 9.6 pKd 37
pKd 9.6 [37]
[125I]CGP 23996 Mm Full agonist 9.4 pKd 34
pKd 9.4 [34]
NC 8-12 Hs Full agonist 10.0 pKi 31
pKi 10.0 [31]
CST-14 {Sp: Mouse, Rat} Hs Full agonist 9.1 – 9.9 pKi 45-46
pKi 9.1 – 9.9 [45-46]
SRIF-14 {Sp: Human, Mouse, Rat} Hs Full agonist 8.7 – 10.0 pKi 4,6,8,31,33,38,45-46,53
pKi 8.7 – 10.0 [4,6,8,31,33,38,45-46,53]
CST-17 {Sp: Human} Hs Full agonist 8.7 – 9.9 pKi 8,45-46
pKi 8.7 – 9.9 [8,45-46]
BN-81,644 Hs Full agonist 9.2 pKi 33
pKi 9.2 [33]
SRIF-28 {Sp: Human, Mouse, Rat} Rn Full agonist 9.1 pKi 28
pKi 9.1 [28]
CGP 23996 Hs Full agonist 8.8 – 9.3 pKi 45-46
pKi 8.8 – 9.3 [45-46]
BIM 23052 Hs Full agonist 8.4 – 9.7 pKi 4,45-46
pKi 8.4 – 9.7 [4,45-46]
BN-81,674 Hs Full agonist 9.0 pKi 33
pKi 9.0 [33]
SRIF-28 {Sp: Human, Mouse, Rat} Hs Full agonist 8.1 – 9.9 pKi 4,6,8,28,31,45-46
pKi 8.1 – 9.9 [4,6,8,28,31,45-46]
SRIF-14 {Sp: Human, Mouse, Rat} Rn Full agonist 8.9 pKi 28
pKi 8.9 [28]
BIM 23058 Hs Full agonist 8.8 pKi 31
pKi 8.8 [31]
BIM 23068 Hs Full agonist 8.8 pKi 31
pKi 8.8 [31]
BIM 23052 Rn Full agonist 8.5 pKi 28
pKi 8.5 [28]
BIM 23068 Rn Full agonist 8.4 pKi 28
pKi 8.4 [28]
BIM 23295 Rn Full agonist 8.2 pKi 28
pKi 8.2 [28]
BIM 23023 Hs Full agonist 8.1 pKi 31
pKi 8.1 [31]
BIM 23034 Hs Full agonist 8.1 pKi 31
pKi 8.1 [31]
octreotide Hs Full agonist 7.4 – 8.6 pKi 4,6,31,45-46,53
pKi 7.4 – 8.6 [4,6,31,45-46,53]
NC 4-28B Hs Full agonist 8.0 pKi 31
pKi 8.0 [31]
L-362,855 Hs Full agonist 7.6 – 8.3 pKi 45-46
pKi 7.6 – 8.3 [45-46]
octreotide Rn Full agonist 7.8 pKi 28
pKi 7.8 [28]
BIM 23050 Hs Full agonist 7.8 pKi 31
pKi 7.8 [31]
vapreotide Hs Full agonist 7.4 – 7.9 pKi 4,31,45
pKi 7.4 – 7.9 [4,31,45]
lanreotide Hs Full agonist 7.2 – 8.0 pKi 4,31,45-46
pKi 7.2 – 8.0 [4,31,45-46]
L-796,778 Hs Full agonist 7.6 pKi 38
pKi 7.6 [38]
BIM 23030 Hs Full agonist 7.2 – 7.8 pKi 45-46
pKi 7.2 – 7.8 [45-46]
MK-678 Rn Full agonist 7.4 pKi 28
pKi 7.4 [28]
MK-678 Hs Full agonist 6.6 – 7.9 pKi 4,31,45-46,53
pKi 6.6 – 7.9 [4,31,45-46,53]
vapreotide Rn Full agonist 7.1 pKi 28
pKi 7.1 [28]
BIM 23056 Hs Full agonist 6.9 – 7.2 pKi 45-46
pKi 6.9 – 7.2 [45-46]
BIM 23023 Rn Full agonist 7.0 pKi 28
pKi 7.0 [28]
lanreotide Rn Full agonist 6.9 pKi 28
pKi 6.9 [28]
L-363,301 Hs Full agonist 6.3 – 7.0 pKi 45-46
pKi 6.3 – 7.0 [45-46]
BIM 23056 Mm Full agonist 10.7 pIC50 34
pIC50 10.7 [34]
BIM 23058 Mm Full agonist 10.4 pIC50 34
pIC50 10.4 [34]
SRIF-28 {Sp: Human, Mouse, Rat} Mm Full agonist 10.2 pIC50 34
pIC50 10.2 [34]
L-362,823 Mm Full agonist 10.1 pIC50 34
pIC50 10.1 [34]
SRIF-14 {Sp: Human, Mouse, Rat} Mm Full agonist 10.1 pIC50 34
pIC50 10.1 [34]
BIM 23052 Mm Full agonist 9.4 pIC50 34
pIC50 9.4 [34]
BIM 23068 Mm Full agonist 9.1 pIC50 34
pIC50 9.1 [34]
BIM 23066 Mm Full agonist 9.0 pIC50 34
pIC50 9.0 [34]
pasireotide Hs Full agonist 8.8 pIC50 41
pIC50 8.8 [41]
KE 108 Hs Full agonist 8.8 pIC50 36
pIC50 8.8 [36]
octreotide Mm Full agonist 8.5 pIC50 34
pIC50 8.5 [34]
Des-AA5-[D-Trp8]SRIF Hs Full agonist 8.4 – 8.5 pIC50 10
pIC50 8.4 – 8.5 [10]
[111In]DOTA-BOC-ATE Hs Full agonist 8.3 pIC50 13
pIC50 8.3 [13]
BIM 23050 Mm Full agonist 8.3 pIC50 34
pIC50 8.3 [34]
lanreotide Mm Full agonist 8.2 pIC50 34
pIC50 8.2 [34]
BIM 23059 Mm Full agonist 8.2 pIC50 34
pIC50 8.2 [34]
[111In]DOTA-NOC Hs Full agonist 8.1 pIC50 50
pIC50 8.1 [50]
[111In]DOTA-NOC-ATE Hs Full agonist 7.9 pIC50 13
pIC50 7.9 [13]
MK-678 Mm Full agonist 7.9 pIC50 34
pIC50 7.9 [34]
BIM 23023 Mm Full agonist 7.9 pIC50 34
pIC50 7.9 [34]
[111In,90Y]DOTA-NOC Hs Full agonist 7.6 pIC50 50
pIC50 7.6 [50]
BIM 23197 Hs Full agonist 7.6 pIC50 42
pIC50 7.6 [42]
[111In,90Y]DOTA-OC Hs Full agonist 7.6 pIC50 50
pIC50 7.6 [50]
BOC-ATE Hs Full agonist 7.5 pIC50 13
pIC50 7.5 [13]
BIM 23034 Mm Full agonist 7.2 pIC50 34
pIC50 7.2 [34]
NC 4-28B Mm Full agonist 7.0 pIC50 34
pIC50 7.0 [34]
BIM 23056 Rn Full agonist 6.5 pIC50 49
pIC50 6.5 [49]
[111In,90Y]DOTA-LAN Hs Full agonist 6.5 pIC50 50
pIC50 6.5 [50]
NOC-ATE Hs Full agonist 6.5 pIC50 13
pIC50 6.5 [13]
[111In,90Y]DOTA-TOC Hs Full agonist 6.4 pIC50 50
pIC50 6.4 [50]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
NVP ACQ090 Hs Antagonist 7.9 pKi 16
pKi 7.9 [16]
PRL-2915 Hs Antagonist 7.0 pKi 15
pKi 7.0 [15]
PRL-2970 Hs Antagonist 7.0 pKi 15
pKi 7.0 [15]
[L-Tyr8]CYN 154806 Hs Antagonist 6.2 – 6.8 pKi 11
pKi 6.2 – 6.8 [11]
[D-Tyr8]CYN 154806 Hs Antagonist 6.2 – 6.7 pKi 11
pKi 6.2 – 6.7 [11]
sst3-ODN-8 Hs Antagonist 8.2 pIC50 37
pIC50 8.2 [37]
BIM 23627 Hs Antagonist 7.4 pIC50 48
pIC50 7.4 [48]
BIM 23454 Hs Antagonist 7.3 pIC50 48
pIC50 7.3 [48]
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  18,43,54
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family
G protein (identity unknown)
Phospholipase C stimulation
Comments:  Stimulation of PLC is via the Gq G-protein. There is also inhibition of the Na+/H+ exchanger (NHE1) and activation of protein tyrosine phosphatases via unknown G-proteins.
References:  1,26,35,44
Tissue Distribution
T cells (Jurkat).
Species:  Human
Technique:  RT-PCR.
References:  5
Cerebellum (Purkinje cells and Golgi cells), frontal cortex (pyramidal cells), hippocampus (CA1-4 subfields and some granule cells of the dentate gyrus).
Species:  Human
Technique:  RT-PCR and in situ hybridisation.
References:  40
Anterior pituitary, pancreatic islets, enteric ganglion cells of the intestine, non-functioning, ACTH- and GH-producing pituitary adenomas
Species:  Human
Technique:  Immunohistochemistry
References:  27
Poorly expressed in pancreatic islets, mainly in β-cells.
Species:  Human
Technique:  immunocytochemistry.
References:  22
Primary neuronal cilia.
Species:  Mouse
Technique:  Immunohistochemistry and electron microscopy
References:  17
High levels in the cerebellum, amygdala, hippocampus, striatum, olfactory bulb and cortex. Medium levels in the hypothalamus, thalamus, midbrain and preoptic area.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  3
Cortex, hippocampus (indeseum griseum, granular layer of the dentate gyrus, piriform cortex, amygdaloid nuclei), amygdala, habenula, hypothalamus, cerebellum (granular cell layer and interpositus cerebellar nuclei).
Species:  Rat
Technique:  immunocytochemistry.
References:  14
Aorta.
Species:  Rat
Technique:  RT-PCR and immunocytochemistry.
References:  19
Pituitary.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  3
Pituitary.
Species:  Rat
Technique:  RT-PCR.
References:  7,9
Spleen, kidney, liver.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  3
Fundic gastric mucosa of the stomach.
Species:  Rat
Technique:  RT-PCT.
References:  23
Expression Datasets

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of PLC activity in CCL39 cells stably transfected with human sst3 receptors.
Species:  Human
Tissue:  CCL39 cells.
Response measured:  Stimulation of PLC activity.
References:  44
Measurement of cAMP accumulation (AC activity) in CHO-K1 cells stably transfected with human sst3 receptors.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  33
Measurement of NHE1 (Na-H exchanger) activity (pH recovery) in Ltk- cells stably expressing rat sst3 receptors.
Species:  Rat
Tissue:  Mouse fibroblast Ltk- cells.
Response measured:  Inhibition of NHE1 activity.
References:  26
Measurement of protein tyrosine phosphatase and Raf-1 activity in NIH 3T3 cells stably transfected with human sst3 receptors.
Species:  Human
Tissue:  NIH 3T3 cells.
Response measured:  Activation of protein tyrosine phosphatase, inactivation of Raf-1 serine kinase.
References:  35
Measurement of cAMP accumulation (AC activity) in HEK 293 cells stably transfected with human sst3 receptors.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  18
Measurement of AC activity (cAMP levels) in CCL39 cells stably transfected with human sst3 receptors.
Species:  Human
Tissue:  CCL39 cells.
Response measured:  Inhibition of AC activity.
References:  43
Measurement of GIRK currents (inward potassium currents) in Xenopus oocyte cells stably transfected with rat sst3 receptors and GIRK1 channels.
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Activation of GIRK current.
References:  20
Measurement of AC activity (cAMP accumulation) in COS-1 cells stably expressing mouse sst3 receptors.
Species:  Mouse
Tissue:  COS-1 cells.
Response measured:  Inhibition of AC activity.
References:  54
Measurement of NOS activity (NO production) in CHO-K1 cells stably transfected with rat sst3 receptors.
Species:  Rat
Tissue:  CHO-K1 cells.
Response measured:  Inhibition of NO production.
References:  2
SOM230 and octreotide induce internalization, signaling and rapid down-regulation of human sst3 receptors
Species:  Human
Tissue:  HEK 293 cells
Response measured:  Time-dependent ERK1/2 activation measured by ELISA, Western blot analysis.
References:  24
Human somatostatin receptor (sst) subtypes sst2A and sst3 exist as homodimers at the plasma membrane.
Species:  Human
Tissue:  HEK 293 cells
Response measured:  Immuncytochemistry and co-immunoprecipitation
References:  32
Somatostatin inhibits tumor angiogenesis through inhibition of both eNOS and MAPK activities
Species:  Human
Tissue:  Human EAhy926 cell line; KS cell cultures
Response measured:  In vivo angiogenesis, cell survival studies, cell proliferation studies, determination of nitric oxide production and Western blot analysis
References:  12
Human sst3 interacts with the multiple PDZ protein MUPP1
Species:  Human
Tissue:  MCF7 cells
Response measured:  Immuncytochemistry and co-immunoprecipitation
References:  25
Sst3 traffics through Rab4-, Rab21-, and Rab11-containing endosomes, but largely bypasses Rab5 and Rab7 endosomes
Species:  Mouse
Tissue:  IMCD3
Response measured:  Immunofluorescence microscopy and live cell imaging
References:  47
Agonist-dependent internalization of the rat sst3 requires four hydroxyl amino acids (Ser341, Ser346, Ser351, Thr357) in the receptor C terminus
Species:  Rat
Tissue:  HEK 293 cells
Response measured:  Co-immunoprecipitation and Western blot analysis
References:  39
α-adaptin, clathrin and Rab11 colocalize with the receptor. Agonist-induced endocytosis of sst3 depends on its interaction with β-arrestin.
Species:  Rat
Tissue:  Neuroendocrine rat insulinoma 1046-38
Response measured:  Immuncytochemistry and electron microscopy
References:  21
Physiological Functions
Inhibition of IL-2 secretion and cell proliferation.
Species:  Human
Tissue:  T cells (Jurkat)
References:  5
Inhibition of GH release (with sst2).
Species:  Rat
Tissue:  Hepatocytes (liver cells).
References:  30
Available Assays
DiscoveRx PathHunter® CHO-K1 SSTR3 β-Arrestin Cell Line (Cat no. 93-0244C2)
PathHunter® eXpress SSTR3 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0244E2CP0M)
PathHunter® HEK 293 SSTR3 β-Arrestin Cell Line (Cat no. 93-0244C1)
more info

REFERENCES

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To cite this database page, please use the following:

Jacques Epelbaum, Wasyl Feniuk, Anthony Harmar, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Wolfgang Meyerhof, Anne-Marie O'Carroll, Yogesh C. Patel, Terry Reisine, Jean-Claude Reubi, Marcus Schindler, Agnes Schonbrunn, John E. Taylor, Annamaria Vezzani.
Somatostatin receptors: sst3 receptor. Last modified on 09/06/2014. Accessed on 02/09/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=357.

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