Somatostatin Receptor Gene Data

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
sst3 Human SSTR3 NM_001051 P32745
Mouse Sstr3 NM_009218 P30935
Rat Sstr3 NM_133522 P30936
sst4 Human SSTR4 NM_001052 P31391
Mouse Sstr4 NM_009219 P49660
Rat Sstr4 NM_031547 P08485
sst5 Human SSTR5 NM_001053 P35346
Mouse Sstr5 NM_011425 O08858
Rat Sstr5 NM_012882 P30938

Somatostatin Receptor Data

Receptor Subtype sst1 sst2 sst3 sst4 sst5
Transduction Mechanism Gi Gi Gi Gi Gi
Primary Distribution Stomach, jejunum, pituitary Cerebrum, kidney, pituitary Cerebrum, pituitary, pancreas Cortex, hypothalamus, lung Pituitary, hypothalamus, small intestine
Key Compounds Ki/IC50 (nM)
Agonists BIM 23052 (2842)
L-803,087 (1979)
L-817,818 (1980)
Octreotide (1818)
RC 160 (3139)
Seglitide (1836)
Somatostatin (1157)
Somatostatin 1-28 (1165)
31.3
199
3.3
> 1000
> 1000
> 1000
1.1
2.2
13.5
4720
52
2.1
5.4
1.5
1.3
4.1 -
-
1280
64
4.4
30.9
27
1.6
6.1
141
82
0.7
> 1000
45
127
0.53
1.1
7.3
3880
0.4
5.6
0.7
2
0.9
0.07
Antagonists BIM 23056 (1844)
CYN 154806 (1843)
142
5.41*
> 1000
8.85*
10.8
6.07*
16.6
5.76*
5.7
6.48*

* pIC50 values

References

Moller et al (2003) Somatostatin Receptors. Biochem.Biophys.Acta. 1616 1. Alexander et al (2004) Guide to receptors and channels. Br.J.Pharmacol. 141 Suppl.1. Patel and Srikant (1995) Subtype selectivity of peptide analogues for all five cloned human somatostatin receptors (hsstr 1-5). Endocrinology 135 2814. Fenuik et al (2000) Selective somatostatin sst2 receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology 39 1443. Rohrer and Schaeffer (2000) Identification and characterization of subtype selective somatostatin receptor agonists. J.Physiol. 94 211.