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sst3 receptor

Family: Somatostatin receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
References
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 6,42-43
Mouse 7 428 15 E1 Sstr3 somatostatin receptor 3 45
Rat 7 428 7q34 Sstr3 somatostatin receptor 3 23
Previous and Unofficial Names
SSTR3
SRIF1C
SRIF1
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
Entrez Gene
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.
UniProt
Wikipedia
Search for 3D structures on the PDB
Search by keyword: Somatostatin receptors sst3 receptor
Natural/Endogenous Ligand(s)
CST-14 {Sp: Mouse, Rat}
CST-17 {Sp: Human}
SRIF-14 {Sp: Human, Mouse, Rat}
SRIF-28 {Sp: Human, Mouse, Rat}
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 37-38
[125I]LTT-SRIF-28 Hs Full agonist 9.7 – 10.3 pKd 6,37-38
[125I]CGP 23996 Hs Full agonist 9.8 pKd 38
[125I]Tyr7-Sst3-ODN-8 Hs Full agonist 9.6 pKd 30
[125I]CGP 23996 Mm Full agonist 9.4 pKd 27
[125I]LTT-SRIF-28 Hs Full agonist 9.4 pKd 31
NC 8-12 Hs Full agonist 10.0 pKi 25
CST-14 {Sp: Mouse, Rat} Hs Full agonist 9.1 – 9.9 pKi 37-38
SRIF-14 {Sp: Human, Mouse, Rat} Hs Full agonist 8.7 – 10.0 pKi 4,6,8,25-26,31,37-38,44
CST-17 {Sp: Human} Hs Full agonist 8.7 – 9.9 pKi 8,37-38
BN-81,644 Hs Full agonist 9.2 pKi 26
SRIF-28 {Sp: Human, Mouse, Rat} Rn Full agonist 9.1 pKi 22
CGP 23996 Hs Full agonist 8.8 – 9.3 pKi 37-38
BIM 23052 Hs Full agonist 8.4 – 9.7 pKi 4,37-38
BN-81,674 Hs Full agonist 9.0 pKi 26
SRIF-28 {Sp: Human, Mouse, Rat} Hs Full agonist 8.1 – 9.9 pKi 4,6,8,22,25,37-38
SRIF-14 {Sp: Human, Mouse, Rat} Rn Full agonist 8.9 pKi 22
BIM 23058 Hs Full agonist 8.8 pKi 25
BIM 23068 Hs Full agonist 8.8 pKi 25
BIM 23052 Rn Full agonist 8.5 pKi 22
BIM 23068 Rn Full agonist 8.4 pKi 22
BIM 23295 Rn Full agonist 8.2 pKi 22
BIM 23023 Hs Full agonist 8.1 pKi 25
BIM 23034 Hs Full agonist 8.1 pKi 25
NC 4-28B Hs Full agonist 8.0 pKi 25
octreotide Hs Full agonist 7.4 – 8.6 pKi 4,6,25,37-38,44
L-362,855 Hs Full agonist 7.6 – 8.3 pKi 37-38
BIM 23050 Hs Full agonist 7.8 pKi 25
octreotide Rn Full agonist 7.8 pKi 22
vapreotide Hs Full agonist 7.4 – 7.9 pKi 4,25,37
L-796,778 Hs Full agonist 7.6 pKi 31
lanreotide Hs Full agonist 7.2 – 8.0 pKi 4,25,37-38
BIM 23030 Hs Full agonist 7.2 – 7.8 pKi 37-38
MK-678 Rn Full agonist 7.4 pKi 22
MK-678 Hs Full agonist 6.6 – 7.9 pKi 4,25,37-38,44
vapreotide Rn Full agonist 7.1 pKi 22
BIM 23056 Hs Full agonist 6.9 – 7.2 pKi 37-38
BIM 23023 Rn Full agonist 7.0 pKi 22
lanreotide Rn Full agonist 6.9 pKi 22
L-363,301 Hs Full agonist 6.3 – 7.0 pKi 37-38
BIM 23056 Mm Full agonist 10.7 pIC50 27
BIM 23058 Mm Full agonist 10.4 pIC50 27
SRIF-28 {Sp: Human, Mouse, Rat} Mm Full agonist 10.2 pIC50 27
L-362,823 Mm Full agonist 10.1 pIC50 27
SRIF-14 {Sp: Human, Mouse, Rat} Mm Full agonist 10.1 pIC50 27
BIM 23052 Mm Full agonist 9.4 pIC50 27
BIM 23068 Mm Full agonist 9.1 pIC50 27
BIM 23066 Mm Full agonist 9.0 pIC50 27
KE 108 Hs Full agonist 8.8 pIC50 29
SOM-230 Hs Full agonist 8.8 pIC50 33
octreotide Mm Full agonist 8.5 pIC50 27
Des-AA5-[D-Trp8]SRIF Hs Full agonist 8.4 – 8.5 pIC50 10
BIM 23050 Mm Full agonist 8.3 pIC50 27
[111In]DOTA-BOC-ATE Hs Full agonist 8.3 pIC50 12
BIM 23059 Mm Full agonist 8.2 pIC50 27
lanreotide Mm Full agonist 8.2 pIC50 27
[111In]DOTA-NOC Hs Full agonist 8.1 pIC50 41
BIM 23023 Mm Full agonist 7.9 pIC50 27
MK-678 Mm Full agonist 7.9 pIC50 27
[111In]DOTA-NOC-ATE Hs Full agonist 7.9 pIC50 12
BIM 23197 Hs Full agonist 7.6 pIC50 34
[111In,90Y]DOTA-NOC Hs Full agonist 7.6 pIC50 41
[111In,90Y]DOTA-OC Hs Full agonist 7.6 pIC50 41
BOC-ATE Hs Full agonist 7.5 pIC50 12
BIM 23034 Mm Full agonist 7.2 pIC50 27
NC 4-28B Mm Full agonist 7.0 pIC50 27
BIM 23056 Rn Full agonist 6.5 pIC50 40
NOC-ATE Hs Full agonist 6.5 pIC50 12
[111In,90Y]DOTA-LAN Hs Full agonist 6.5 pIC50 41
[111In,90Y]DOTA-TOC Hs Full agonist 6.4 pIC50 41
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 15
PRL-2915 Hs Antagonist 7.0 pKi 14
PRL-2970 Hs Antagonist 7.0 pKi 14
[L-Tyr8]CYN 154806 Hs Antagonist 6.2 – 6.8 pKi 11
[D-Tyr8]CYN 154806 Hs Antagonist 6.2 – 6.7 pKi 11
sst3-ODN-8 Hs Antagonist 8.2 pIC50 30
BIM 23627 Hs Antagonist 7.4 pIC50 39
BIM 23454 Hs Antagonist 7.3 pIC50 39

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  16,36,45
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:  1,21,28,35
Tissue Distribution
Poorly expressed in pancreatic islets, mainly in beta-cells.
Species:  Human
Technique:  immunocytochemistry.
References:  19
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:  32
Spleen, kidney, liver.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  3
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
Aorta.
Species:  Rat
Technique:  RT-PCR and immunocytochemistry.
References:  17
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:  13
Fundic gastric mucosa of the stomach.
Species:  Rat
Technique:  RT-PCT.
References:  20
Pituitary.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  3
Pituitary.
Species:  Rat
Technique:  RT-PCR.
References:  7,9
Expression Datasets

Click here to show/hide data

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 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:  26
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:  21
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:  35
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:  28
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:  16
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:  36
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:  18
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:  45
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
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:  24

REFERENCES

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 07/01/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=357.


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