SST2 receptor

Target id: 356

Nomenclature: SST2 receptor

Family: Somatostatin receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for SST2 receptor in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 369 17q24 SSTR2 somatostatin receptor 2 155-156
Mouse 7 369 11 E2 Sstr2 somatostatin receptor 2 145,155
Rat 7 369 10q32.1 Sstr2 somatostatin receptor 2 70
Previous and Unofficial Names
somatotropin release-inhibiting factor receptor | SRIF-1
Database Links
Specialist databases
GPCRDB ssr2_human (Hs), ssr2_mouse (Mm), ssr2_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
cortistatin-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

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]LTT-SRIF-28 Hs Full agonist 9.9 – 10.0 pKd 125,130-131
pKd 9.9 – 10.0 [125,130-131]
[125I]Tyr3 SMS 201-995 Hs Full agonist 9.9 pKd 131-132
pKd 9.9 (Kd 1.3x10-10 M) [131-132]
[125I]CGP 23996 Hs Full agonist 9.8 pKd 131-132
pKd 9.8 [131-132]
[125I]MK-678 Mm Full agonist 9.6 pKd 106
pKd 9.6 [106]
[125I]Tyr3 SMS 201-995 Rn Full agonist 9.5 pKd 109
pKd 9.5 (Kd 2.9x10-10 M) [109]
[125I]Tyr10-CST14 Hs Full agonist 9.4 pKd 130,132
pKd 9.4 [130,132]
[125I]Tyr11-SRIF-14 Mm Full agonist 9.2 pKd 83
pKd 9.2 [83]
[125I]LTT-SRIF-28 Rn Full agonist 9.0 – 9.3 pKd 118-119
pKd 9.0 – 9.3 (Kd 9.5x10-10 – 4.6x10-10 M) [118-119]
[125I]Tyr11-SRIF-14 Rn Full agonist 9.0 pKd 118
pKd 9.0 (Kd 1.09x10-9 M) [118]
L-054,522 Hs Full agonist 11.0 pKi 157
pKi 11.0 [157]
EC 5-21 Hs Full agonist 10.6 pKi 102
pKi 10.6 [102]
NC 8-12 Hs Full agonist 10.6 pKi 102
pKi 10.6 [102]
L-779,976 Hs Full agonist 10.3 pKi 125
pKi 10.3 [125]
SRIF-14 {Sp: Human, Mouse, Rat} Hs Full agonist 8.9 – 10.5 pKi 23,45,102,105,125,130-132,157
pKi 8.9 – 10.5 [23,45,102,105,125,130-132,157]
DC 23-60 Hs Full agonist 9.6 pKi 102
pKi 9.6 [102]
seglitide Hs Full agonist 8.8 – 10.3 pKi 23,102,130-132,157
pKi 8.8 – 10.3 [23,102,130-132,157]
BIM 23023 Hs Full agonist 9.4 pKi 102
pKi 9.4 [102]
BIM 23059 Hs Full agonist 9.4 pKi 102
pKi 9.4 [102]
L-363,377 Hs Full agonist 9.3 pKi 125,157
pKi 9.3 [125,157]
seglitide Rn Full agonist 9.3 pKi 92
pKi 9.3 [92]
SRIF-28 {Sp: Human, Mouse, Rat} Hs Full agonist 8.4 – 10.2 pKi 23,45,102,130-132
pKi 8.4 – 10.2 [23,45,102,130-132]
octreotide Hs Full agonist 8.7 – 9.9 pKi 23,102,130-132,157
pKi 8.7 – 9.9 [23,102,130-132,157]
SRIF-14 {Sp: Human, Mouse, Rat} Mm Full agonist 8.8 – 9.6 pKi 92
pKi 8.8 – 9.6 [92]
vapreotide Hs Full agonist 8.3 – 10.1 pKi 23,102
pKi 8.3 – 10.1 [23,102]
BIM 23023 Rn Full agonist 9.2 pKi 92
pKi 9.2 [92]
BIM 23060 Hs Full agonist 9.2 pKi 102
pKi 9.2 [102]
lanreotide Hs Full agonist 8.7 – 9.6 pKi 23,102,130-132
pKi 8.7 – 9.6 [23,102,130-132]
vapreotide Rn Full agonist 9.1 pKi 92
pKi 9.1 [92]
CST-17 {Sp: Human} Hs Full agonist 8.8 – 9.3 pKi 45,130,132
pKi 8.8 – 9.3 [45,130,132]
CGP 23996 Hs Full agonist 8.6 – 9.1 pKi 23,130-132
pKi 8.6 – 9.1 [23,130-132]
SRIF-14 {Sp: Human, Mouse, Rat} Rn Full agonist 8.8 pKi 92
pKi 8.8 [92]
SRIF-28 {Sp: Human, Mouse, Rat} Rn Full agonist 8.8 pKi 92
pKi 8.8 [92]
lanreotide Rn Full agonist 8.8 pKi 92
pKi 8.8 [92]
BIM 23068 Hs Full agonist 8.8 pKi 102
pKi 8.8 [102]
cortistatin-14 {Sp: Mouse, Rat} Hs Full agonist 8.4 – 9.0 pKi 130-132
pKi 8.4 – 9.0 [130-132]
octreotide Rn Full agonist 8.7 pKi 92
pKi 8.7 [92]
L-362,855 Hs Full agonist 8.4 – 8.8 pKi 130-132
pKi 8.4 – 8.8 [130-132]
BIM 23034 Hs Full agonist 8.6 pKi 102
pKi 8.6 [102]
seglitide Mm Full agonist 7.1 – 9.9 pKi 92
pKi 7.1 – 9.9 [92]
BIM 23052 Hs Full agonist 8.1 – 8.8 pKi 23,130-132
pKi 8.1 – 8.8 [23,130-132]
NC 4-28B Hs Full agonist 8.4 pKi 102
pKi 8.4 [102]
L-363,301 Hs Full agonist 8.3 – 8.5 pKi 130,132
pKi 8.3 – 8.5 [130,132]
octreotide Mm Full agonist 7.5 – 9.2 pKi 92
pKi 7.5 – 9.2 [92]
BIM 23023 Mm Full agonist 7.0 – 9.4 pKi 92
pKi 7.0 – 9.4 [92]
lanreotide Mm Full agonist 6.9 – 9.1 pKi 92
pKi 6.9 – 9.1 [92]
L-362,855 Rn Full agonist 7.9 pKi 92
pKi 7.9 [92]
BIM 23030 Hs Full agonist 7.7 – 7.9 pKi 130-132
pKi 7.7 – 7.9 [130-132]
L-362,855 Mm Full agonist 7.0 – 8.5 pKi 92
pKi 7.0 – 8.5 [92]
vapreotide Mm Full agonist 6.1 – 9.2 pKi 92
pKi 6.1 – 9.2 [92]
BIM 23056 Hs Full agonist 6.2 – 6.7 pKi 23,130-132
pKi 6.2 – 6.7 [23,130-132]
L-779,976 Rn Agonist 10.1 pEC50 86
pEC50 10.1 (EC50 9x10-11 M) [86]
L-779,976 Rn Partial agonist 9.3 pEC50 86
pEC50 9.3 (EC50 5.6x10-10 M) [86]
KE 108 Rn Agonist 7.9 – 10.2 pEC50 33,67
pEC50 7.9 – 10.2 (EC50 1.21x10-8 – 5.7x10-11 M) [33,67]
SRIF-14 {Sp: Human, Mouse, Rat} Rn Agonist 9.0 – 9.1 pEC50 86
pEC50 9.0 – 9.1 (EC50 1.02x10-9 – 7.3x10-10 M) [86]
pasireotide Rn Agonist 7.8 – 9.1 pEC50 33,67
pEC50 7.8 – 9.1 (EC50 1.75x10-8 – 8.6x10-10 M) [33,67]
KE 108 Rn Partial agonist 7.6 pEC50 67
pEC50 7.6 (EC50 2.36x10-8 M) [67]
pasireotide Rn Partial agonist 7.6 pEC50 67
pEC50 7.6 (EC50 2.33x10-8 M) [67]
L-363,409 Mm Full agonist 12.0 pIC50 83
pIC50 12.0 [83]
BIM 23034 Mm Full agonist 11.7 pIC50 106
pIC50 11.7 [106]
BIM 23027 Mm Full agonist 10.2 – 12.0 pIC50 83,106
pIC50 10.2 – 12.0 [83,106]
BIM 23059 Mm Full agonist 11.1 pIC50 106
pIC50 11.1 [106]
BIM 23060 Mm Full agonist 10.9 pIC50 106
pIC50 10.9 [106]
NC 4-28B Mm Full agonist 10.0 – 11.7 pIC50 83,106
pIC50 10.0 – 11.7 [83,106]
BIM 23027 Hs Agonist 10.9 pIC50 28
pIC50 10.9 (IC50 1.4x10-11 M) [28]
BIM 23068 Mm Full agonist 9.8 pIC50 106
pIC50 9.8 [106]
BIM 23027 Rn Agonist 9.7 pIC50 64
pIC50 9.7 (IC50 2x10-10 M) [64]
BIM 23197 Hs Full agonist 9.7 pIC50 128
pIC50 9.7 [128]
[125I]BIM23027 Rn Full agonist 9.7 pIC50 64
pIC50 9.7 (IC50 2.2x10-10 M) [64]
[Ga-DOTA,Tyr3,Thr8]octreotide Hs Full agonist 9.7 pIC50 7,120
pIC50 9.7 (IC50 2x10-10 M) [7,120]
NC 8-12 Mm Full agonist 9.5 pIC50 83
pIC50 9.5 [83]
L-363,377 Mm Full agonist 9.4 pIC50 83
pIC50 9.4 [83]
[125I][Tyr3,Thr8]octreotide Hs Full agonist 9.3 pIC50 151
pIC50 9.3 (IC50 4.7x10-10 M) [151]
SRIF-28 {Sp: Human, Mouse, Rat} Mm Full agonist 9.0 – 9.5 pIC50 92
pIC50 9.0 – 9.5 [92]
BOC-ATE Hs Full agonist 9.1 pIC50 54
pIC50 9.1 [54]
maltotriose-[125I][Tyr3,Thr8]octreotide Hs Full agonist 9.0 pIC50 151
pIC50 9.0 (IC50 9.5x10-10 M) [151]
KE 108 Hs Full agonist 9.0 pIC50 111
pIC50 9.0 [111]
pasireotide Hs Full agonist 9.0 pIC50 127
pIC50 9.0 [127]
DC 23-60 Mm Full agonist 9.0 pIC50 106
pIC50 9.0 [106]
[125I]Tyr3 SMS 201-995 Hs Full agonist 8.9 pIC50 151
pIC50 8.9 (IC50 1.3x10-9 M) [151]
[111In]DOTA-BOC-ATE Hs Full agonist 8.8 pIC50 54
pIC50 8.8 [54]
In-NODAGATOC Hs Full agonist 8.8 pIC50 43
pIC50 8.8 (IC50 1.7x10-9 M) [43]
Ga-DOTA-NOC Hs Full agonist 8.7 pIC50 7
pIC50 8.7 (IC50 1.9x10-9 M) [7]
[111In]DOTA-NOC-ATE Hs Full agonist 8.7 pIC50 54
pIC50 8.7 [54]
AM3 Hs Full agonist 8.6 pIC50 48
pIC50 8.6 (IC50 2.3x10-9 M) [48]
L-363,301 Mm Full agonist 8.1 – 9.1 pIC50 83,106
pIC50 8.1 – 9.1 [83,106]
Ga-DOTA-TOC Hs Full agonist 8.6 pIC50 120
pIC50 8.6 (IC50 2.5x10-9 M) [120]
BIM 23066 Mm Full agonist 8.5 pIC50 106
pIC50 8.5 [106]
[111In]DOTA-NOC Hs Full agonist 8.5 pIC50 152
pIC50 8.5 [152]
NODAGA-[Tyr3]-octreotide Hs Full agonist 8.5 pIC50 43
pIC50 8.5 (IC50 3.2x10-9 M) [43]
demotate 2 Hs Full agonist 8.5 pIC50 89
pIC50 8.5 (IC50 3.2x10-9 M) [89]
SiFA-Asn(AcNH-β-Glc)-PEG-Tyr3-octreotate Hs Full agonist 8.5 pIC50 154
pIC50 8.5 (IC50 3.3x10-9 M) [154]
[67Ga]NODAGA-[Tyr3]octreotide Hs Full agonist 8.5 pIC50 43
pIC50 8.5 (IC50 3.5x10-9 M) [43]
NOC-ATE Hs Full agonist 8.4 pIC50 54
pIC50 8.4 [54]
[111In,90Y]DOTA-NOC Hs Full agonist 8.4 pIC50 152
pIC50 8.4 [152]
Ga-KE88 Hs Full agonist 8.4 pIC50 55
pIC50 8.4 (IC50 4.1x10-9 M) [55]
SiFA-Asn(AcNH-β-Glc)-Tyr3-octreotate Hs Full agonist 8.4 pIC50 154
pIC50 8.4 (IC50 4.4x10-9 M) [154]
EC 5-21 Mm Full agonist 8.3 pIC50 106
pIC50 8.3 [106]
BIM 23030 Mm Full agonist 8.2 pIC50 106
pIC50 8.2 [106]
Y-KE88 Hs Full agonist 8.0 pIC50 55
pIC50 8.0 (IC50 9.9x10-9 M) [55]
[111In,90Y]DOTA-TOC Hs Full agonist 7.9 pIC50 152
pIC50 7.9 [152]
[111In,90Y]DOTA-OC Hs Full agonist 7.7 pIC50 152
pIC50 7.7 [152]
[111In,90Y]DOTA-LAN Hs Full agonist 7.6 pIC50 152
pIC50 7.6 [152]
Tyr3-octreotide Hs Agonist - -
View species-specific agonist tables
Agonist Comments
Liu et al (2005) [98] describe L-779,976 as a full agonist in its ability to inhibit cAMP accumulation, whereas at high concentration it acts as a partial agonist of receptor internalisation (endocytosis). Similarly, SOM-230 and KE 108 have been reported to act as full or partial agonists depending on which outcome of receptor occupation is measured [33,67]. Both ligands exhibit biased agonism: they activate and antagonise distinct signalling pathways [33]. Although SOM-230 and KE 108 potently inhibited cAMP accumulation in sst2A expressing HEK cells, as would be expected of a somatostatin analog, these compounds were also able to antagonise somatostatin induced increase in intracellular calcium and behaved as partial agonists/antagonists for ERK phosphorylation [33].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[D-Tyr8]CYN 154806 Hs Antagonist 8.1 – 8.9 pKd 100
pKd 8.1 – 8.9 [100]
BASS antagonist Hs Antagonist 9.5 pKi 14
pKi 9.5 (Ki 3x10-10 M) [14]
[L-Tyr8]CYN 154806 Hs Antagonist 8.1 – 8.4 pKi 100
pKi 8.1 – 8.4 [100]
PRL-2915 Rn Antagonist 7.9 pKi 63
pKi 7.9 [63]
PRL-2970 Rn Antagonist 7.6 pKi 63
pKi 7.6 [63]
AC-178,335 Rn Antagonist 6.8 pKi 15
pKi 6.8 [15]
KE 108 Rn Antagonist <5.0 pEC50 33
pEC50 <5.0 (EC50 >1x10-5 M) [33]
pasireotide Rn Antagonist <5.0 pEC50 33
pEC50 <5.0 (EC50 >1x10-5 M) [33]
analog 31 [PMID:18543899] Hs Antagonist 9.1 pIC50 32
pIC50 9.1 (IC50 7x10-10 M) [32]
analog 3 [PMID:18543899] Hs Antagonist 9.1 pIC50 32
pIC50 9.1 (IC50 7.5x10-10 M) [32]
analog 32 [PMID:18543899] Hs Antagonist 8.9 pIC50 32
pIC50 8.9 (IC50 1.2x10-9 M) [32]
Ga-NODAGA-LM3 Hs Antagonist 8.9 pIC50 47
pIC50 8.9 (IC50 1.3x10-9 M) [47]
DOTA-BASS Hs Antagonist 8.8 pIC50 32
pIC50 8.8 (IC50 1.5x10-9 M) [32]
analog 30 [PMID:18543899] Hs Antagonist 8.8 pIC50 32
pIC50 8.8 (IC50 1.7x10-9 M) [32]
BIM 23627 Hs Antagonist 8.2 pIC50 144
pIC50 8.2 [144]
BIM 23454 Hs Antagonist 7.5 pIC50 144
pIC50 7.5 [144]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
G protein independent mechanism
G protein (identity unknown)
Adenylate cyclase inhibition
Potassium channel
Calcium channel
Other - See Comments
Comments:  G protein independent: Inhibition of phosphoinositide 3-kinase activity through direct molecular interactions (and competition) between sst2 first intracellular loop and the regulatory PI3K p85 subunit or filamin-A [19,97].
G-protein-dependent: activation of ERK and PI3K activity in sst2-transfected CHO cells [75] and [59].
Other: Inhibition of L and N voltage gated Ca2++ channels activity [158].
References:  65,68,79,129
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
Gq/G11 family
G protein independent mechanism
G protein (identity unknown)
Adenylate cyclase stimulation
Phospholipase C stimulation
Potassium channel
Calcium channel
Phospholipase D stimulation
Other - See Comments
Comments:  PLC activation is via the Gq G-protein.
K+ channel activation and Ca2+ channel inhibition is via Gi/Go.
There is also protein tyrosine phosphatase (PTP) activation via a PTX-insensitive G-protein.
sst2 activates PLC via a mechanism involving Galpha14 and has also been shown to activate PLD in clonal beta cells HIT-T15 [35,62,84].
Adenylate cyclase stimulation has been reported at very high agonist doses in overexpression systems.
Other downstream events reported to be consequential to somatostatin binding include inhibition of the PI3K-mTOR pathway and cap-dependent translation [11,30,141], activation of the protein-tyrosine phosphatases SHP-1, SHP-2 or PTPeta [13,49] and inhibition of eNOS activity [8].
References:  4,8,11,13,24,30,35,40,49,62,72,79,84,107,140-141
Tissue Distribution
A and B pancreatic islet cells, but not in adjacent acinar cells.
Species:  Human
Technique:  Immunohistochemistry, autoradiography
References:  115
Pituitary.
Species:  Human
Technique:  RT-PCR.
References:  94
Spleen.
Species:  Human
Technique:  Immunohistochemistry.
References:  50
Macrophages.
Species:  Human
Technique:  RT-PCR.
References:  9
Pancreatic islets: co-localised with glucagon in alpha-cells.
Species:  Human
Technique:  immunocytochemistry.
References:  73
Lymphoid cells.
Species:  Human
Technique:  RT-PCR.
References:  143
Lymphoid tissue.
Species:  Human
Technique:  Autoradiography, in vivo scintigraphy
References:  114,122
Proliferating endothelium.
Species:  Human
Technique:  Immunocytochemistry.
References:  3
Kidney.
Species:  Human
Technique:  Autoradiography.
References:  113
Pancreatic exocrine tissue and pancreatic ductal adenocarcinoma.
Species:  Human
Technique:  Immunohistochemistry, RT-PCR
References:  25,76,142
Peritumoral veins of human tumours.
Species:  Human
Technique:  Radioligand binding.
References:  41
GI tract (gastrointestinal lymphatic and nervous components, but not in gastrointestinal circular and longitudinal smooth muscle).
Species:  Human
Technique:  Immunohistochemistry.
References:  57,116
Lymphoid tissue, plexus.
Species:  Human
Technique:  Immunohistochemistry, autoradiography.
References:  116
Brain.
Species:  Human
Technique:  Autoradiography.
References:  110
Vessels.
Species:  Human
Technique:  Autoradiography.
References:  41,112,117
Thymocytes.
Species:  Human
Technique:  RT-PCR.
References:  51
Parietal cells and ECL cells in stomach, and myenteric neurons.
Species:  Mouse
Technique:  Immunohistochemistry and LacZ knock-in.
References:  5
High levels in the cerebrum and kidney. Low levels in the jejunum, colon and liver.
Species:  Mouse
Technique:  RNA blotting.
References:  155
Cortex, amygdala, claustrum, endopiriform nucleus, arcuate and periventricular nuclei of the hypothalamus, medial habenular nucleus.
Species:  Mouse
Technique:  in situ hybridisation.
References:  20
Hippocampus and many other brain areas.
Species:  Rat
Technique:  Immunohistochemistry.
References:  42
Hypothalamus: Medial preoptic area, suprachiasmatic nucleus, arcuate nucleus, anterior hypothalamic nucleus, ventromedial and dorsomedial nuclei, medial tuberal nucleus.
Species:  Rat
Technique:  in situ hybridisation.
References:  16
High levels in the amygdala, cortex, hypothalamus and hippocampus. Medium levels in the striatum, midbrain, thalamus, cerebellum and spinal cord.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  22
Pituitary: somatotrophs (GH release), thyrotrophs (TSH release), lactotrophs (PRL release), as well as gonadotrophs and corticotrophs.
Species:  Rat
Technique:  double label in situ hybridisation.
References:  38
Fundic gastric mucosa of the stomach.
Species:  Rat
Technique:  RT-PCR.
References:  80
Pancreas.
Species:  Rat
Technique:  Immunohistochemistry.
References:  66,137
Aorta.
Species:  Rat
Technique:  RT-PCR and immunocytochemistry.
References:  69
Pituitary.
Species:  Rat
Technique:  RT-PCR.
References:  38,46
Adrenal gland.
Species:  Rat
Technique:  Autoradiography.
References:  91
Anterior pituitary.
Species:  Rat
Technique:  Immunohistochemistry.
References:  93
Pituitary, spleen and pancreas.
Species:  Rat
Technique:  Nuclease protection analysis.
References:  22
Expression Datasets

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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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