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Gene Review

SSTR1  -  somatostatin receptor 1

Homo sapiens

Synonyms: SRIF-2, SS-1-R, SS1-R, SS1R, Somatostatin receptor type 1
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Disease relevance of SSTR1


Psychiatry related information on SSTR1


High impact information on SSTR1


Chemical compound and disease context of SSTR1


Biological context of SSTR1

  • Both analogues caused an inhibition of cell proliferation at a concentration higher than 10 nM in accordance with their affinities for the SSTR1 receptor subtype [20].
  • There is 46% identity and 70% similarity between the amino acid sequences of SSTR1 and SSTR2 [21].
  • Binding experiments were performed on crude membranes by using [125I-labeled Tyr11] somatostatin-14; RC-160 exhibited moderate-to-high affinities for SSTR2, -3, and -5 (IC50, 0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC50, 200 and 620 nM, respectively) [22].
  • On the other hand, in the nonresponder group, CT secretion was reduced by the SSTR1 selective agonist, whereas cell viability was inhibited by SSTR2 selective agonists [23].
  • Highly informative simple tandem repeat DNA polymorphisms were identified in SSTR1 and SSTR2 [24].

Anatomical context of SSTR1


Associations of SSTR1 with chemical compounds


Physical interactions of SSTR1

  • Currently available somatostatin analogs predominantly bind to the somatostatin receptor subtype (SSTR)2 subtype, and control GH and IGF-I secretion in approximately 65% of patients with acromegaly, their efficacy relating to receptor density and subtype expression [30].
  • SRIF2 receptors are not efficiently coupled to G proteins and have a distinct but overlapping distribution in brain with SRIF1 receptors [31].
  • SPET with 111In-SMS and 123I-IBZM after therapy revealed no change or a possible increase in somatostatin receptor binding potential and a possible decrease in dopamine D2 receptor binding potential [32].
  • Gi alpha 1 selectively couples somatostatin receptor subtype 3 to adenylyl cyclase: identification of the functional domains of this alpha subunit necessary for mediating the inhibition by somatostatin of cAMP formation [33].
  • CONTEXT: Cortistatin binds all somatostatin receptor subtypes but also has particular central actions; moreover, a specific cortistatin receptor has also been discovered [34].

Regulatory relationships of SSTR1


Other interactions of SSTR1


Analytical, diagnostic and therapeutic context of SSTR1

  • Tyrosine phosphatase was stimulated by both these analogues in SSTR2 and by RC-160 in SSTR1 at affinities similar to their ability to inhibit growth and bind to receptors, implicating tyrosine phosphatase as a transducer of the growth inhibition signal [20].
  • This is the first demonstration of the presence of SSTR1, SSTR2, and SSTR3 in primary human tumors using in situ hybridization [38].
  • Quantitative RT-PCR showed SSTR1 mRNA mean levels of 6 +/- 2.2 x 10(4) molecules/ microg reverse-transcribed total RNA [40].
  • Immunohistochemistry for SSTR1 and SSTR2 was performed on eight pairs of normal human eyes (28-74 years) imbedded in paraffin [41].
  • Effects of SSTR agonists on proliferation and apoptosis of tumour cells and HSCs were assessed by the 5-bromo-2' deoxyuridine and TUNEL methods, respectively [42].


  1. Identification of somatostatin receptor subtypes and an implication for the efficacy of somatostatin analogue SMS 201-995 in treatment of human endocrine tumors. Kubota, A., Yamada, Y., Kagimoto, S., Shimatsu, A., Imamura, M., Tsuda, K., Imura, H., Seino, S., Seino, Y. J. Clin. Invest. (1994) [Pubmed]
  2. Subtype-specific signaling mechanisms of somatostatin receptors SSTR1 and SSTR2. Hou, C., Gilbert, R.L., Barber, D.L. J. Biol. Chem. (1994) [Pubmed]
  3. Different expression patterns of somatostatin receptor subtypes in cultured epithelial cells from human normal prostate and prostate cancer. Sinisi, A.A., Bellastella, A., Prezioso, D., Nicchio, M.R., Lotti, T., Salvatore, M., Pasquali, D. J. Clin. Endocrinol. Metab. (1997) [Pubmed]
  4. Quantitative and functional expression of somatostatin receptor subtypes in human prolactinomas. Jaquet, P., Ouafik, L., Saveanu, A., Gunz, G., Fina, F., Dufour, H., Culler, M.D., Moreau, J.P., Enjalbert, A. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  5. Expression of somatostatin receptor subtypes (SSTR1-5) in Alzheimer's disease brain: an immunohistochemical analysis. Kumar, U. Neuroscience (2005) [Pubmed]
  6. Developmental changes in the expression of somatostatin receptors (1-5) in the brain, hypothalamus, pituitary and spinal cord of the human fetus. Goodyer, C.G., Grigorakis, S.I., Patel, Y.C., Kumar, U. Neuroscience (2004) [Pubmed]
  7. Somatostatin binding sites in human and monkey brain: localization and characterization. Beal, M.F., Tran, V.T., Mazurek, M.F., Chattha, G., Martin, J.B. J. Neurochem. (1986) [Pubmed]
  8. Is there a gender difference of somatostatin-receptor density in the human brain? Pichler, R., Maschek, W., Crespillo, C., Esteva, I., Soriguer, F. Neuro Endocrinol. Lett. (2002) [Pubmed]
  9. Clinical impact of somatostatin receptor scintigraphy in the management of patients with neuroendocrine gastroenteropancreatic tumors. Lebtahi, R., Cadiot, G., Sarda, L., Daou, D., Faraggi, M., Petegnief, Y., Mignon, M., le Guludec, D. J. Nucl. Med. (1997) [Pubmed]
  10. The pathophysiological consequences of somatostatin receptor internalization and resistance. Hofland, L.J., Lamberts, S.W. Endocr. Rev. (2003) [Pubmed]
  11. Receptors for dopamine and somatostatin: formation of hetero-oligomers with enhanced functional activity. Rocheville, M., Lange, D.C., Kumar, U., Patel, S.C., Patel, R.C., Patel, Y.C. Science (2000) [Pubmed]
  12. Reduced numbers of somatostatin receptors in the cerebral cortex in Alzheimer's disease. Beal, M.F., Mazurek, M.F., Tran, V.T., Chattha, G., Bird, E.D., Martin, J.B. Science (1985) [Pubmed]
  13. Somatostatin receptor expression in primary gastric versus nongastric extranodal B-cell lymphoma of mucosa-associated lymphoid tissue type. Raderer, M., Valencak, J., Pfeffel, F., Drach, J., Pangerl, T., Kurtaran, A., Hejna, M., Vorbeck, F., Chott, A., Virgolini, I. J. Natl. Cancer Inst. (1999) [Pubmed]
  14. Expression of human somatostatin receptor subtype 3 in pancreatic cancer in vitro and in vivo. Raderer, M., Pangerl, T., Leimer, M., Valencak, J., Kurtaran, A., Hamilton, G., Scheithauer, W., Virgolini, I. J. Natl. Cancer Inst. (1998) [Pubmed]
  15. Pharmacological properties of two cloned somatostatin receptors. Rens-Domiano, S., Law, S.F., Yamada, Y., Seino, S., Bell, G.I., Reisine, T. Mol. Pharmacol. (1992) [Pubmed]
  16. Thyroid hormone-induced expression of specific somatostatin receptor subtypes correlates with involution of the TtT-97 murine thyrotrope tumor. James, R.A., Sarapura, V.D., Bruns, C., Raulf, F., Dowding, J.M., Gordon, D.F., Wood, W.M., Ridgway, E.C. Endocrinology (1997) [Pubmed]
  17. Expression of mRNA for all five human somatostatin receptors (hSSTR1-5) in pituitary tumors. Panetta, R., Patel, Y.C. Life Sci. (1995) [Pubmed]
  18. Differential regulation of somatostatin receptors 1 and 2 mRNA and protein expression by tamoxifen and estradiol in breast cancer cells. Rivera, J.A., Alturaihi, H., Kumar, U. Journal of carcinogenesis [electronic resource]. (2005) [Pubmed]
  19. Distribution and functional significance of somatostatin receptors in malignant melanoma. Lum, S.S., Fletcher, W.S., O'Dorisio, M.S., Nance, R.W., Pommier, R.F., Caprara, M. World journal of surgery. (2001) [Pubmed]
  20. Stimulation of tyrosine phosphatase and inhibition of cell proliferation by somatostatin analogues: mediation by human somatostatin receptor subtypes SSTR1 and SSTR2. Buscail, L., Delesque, N., Estève, J.P., Saint-Laurent, N., Prats, H., Clerc, P., Robberecht, P., Bell, G.I., Liebow, C., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  21. Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. Yamada, Y., Post, S.R., Wang, K., Tager, H.S., Bell, G.I., Seino, S. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  22. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. Buscail, L., Estève, J.P., Saint-Laurent, N., Bertrand, V., Reisine, T., O'Carroll, A.M., Bell, G.I., Schally, A.V., Vaysse, N., Susini, C. Proc. Natl. Acad. Sci. U.S.A. (1995) [Pubmed]
  23. Selective activation of somatostatin receptor subtypes differentially modulates secretion and viability in human medullary thyroid carcinoma primary cultures: potential clinical perspectives. Zatelli, M.C., Piccin, D., Tagliati, F., Bottoni, A., Luchin, A., Vignali, C., Margutti, A., Bondanelli, M., Pansini, G.C., Pelizzo, M.R., Culler, M.D., Degli Uberti, E.C. J. Clin. Endocrinol. Metab. (2006) [Pubmed]
  24. Human somatostatin receptor genes: localization to human chromosomes 14, 17, and 22 and identification of simple tandem repeat polymorphisms. Yamada, Y., Stoffel, M., Espinosa, R., Xiang, K.S., Seino, M., Seino, S., Le Beau, M.M., Bell, G.I. Genomics (1993) [Pubmed]
  25. Subtype-selective expression of the five somatostatin receptors (hSSTR1-5) in human pancreatic islet cells: a quantitative double-label immunohistochemical analysis. Kumar, U., Sasi, R., Suresh, S., Patel, A., Thangaraju, M., Metrakos, P., Patel, S.C., Patel, Y.C. Diabetes (1999) [Pubmed]
  26. Subtypes of the somatostatin receptor assemble as functional homo- and heterodimers. Rocheville, M., Lange, D.C., Kumar, U., Sasi, R., Patel, R.C., Patel, Y.C. J. Biol. Chem. (2000) [Pubmed]
  27. Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS 201-995 for the SSTR2 somatostatin receptor. Kaupmann, K., Bruns, C., Raulf, F., Weber, H.P., Mattes, H., Lübbert, H. EMBO J. (1995) [Pubmed]
  28. The somatostatin receptor SSTR1 is coupled to phosphotyrosine phosphatase activity in CHO-K1 cells. Florio, T., Rim, C., Hershberger, R.E., Loda, M., Stork, P.J. Mol. Endocrinol. (1994) [Pubmed]
  29. Somatostatin analogs in vitro effects in a growth hormone-releasing hormone-secreting bronchial carcinoid. Zatelli, M.C., Maffei, P., Piccin, D., Martini, C., Rea, F., Rubello, D., Margutti, A., Culler, M.D., Sicolo, N., degli Uberti, E.C. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  30. The novel somatostatin ligand (SOM230) regulates human and rat anterior pituitary hormone secretion. Murray, R.D., Kim, K., Ren, S.G., Lewis, I., Weckbecker, G., Bruns, C., Melmed, S. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  31. Somatostatin receptors. Raynor, K., Reisine, T. Critical reviews in neurobiology. (1992) [Pubmed]
  32. Imaging of dopamine D2 and somatostatin receptors in vivo using single-photon emission tomography in a patient with a TSH/PRL-producing pituitary macroadenoma. Verhoeff, N.P., Bemelman, F.J., Wiersinga, W.M., van Royen, E.A. European journal of nuclear medicine. (1993) [Pubmed]
  33. Gi alpha 1 selectively couples somatostatin receptor subtype 3 to adenylyl cyclase: identification of the functional domains of this alpha subunit necessary for mediating the inhibition by somatostatin of cAMP formation. Law, S.F., Zaina, S., Sweet, R., Yasuda, K., Bell, G.I., Stadel, J., Reisine, T. Mol. Pharmacol. (1994) [Pubmed]
  34. Cortistatin-17 and somatostatin-14 display the same effects on growth hormone, prolactin, and insulin secretion in patients with acromegaly or prolactinoma. Grottoli, S., Gasco, V., Broglio, F., Baldelli, R., Ragazzoni, F., Gallenca, F., Mainolfi, A., Prodam, F., Muccioli, G., Ghigo, E. J. Clin. Endocrinol. Metab. (2006) [Pubmed]
  35. Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation. Shimon, I., Taylor, J.E., Dong, J.Z., Bitonte, R.A., Kim, S., Morgan, B., Coy, D.H., Culler, M.D., Melmed, S. J. Clin. Invest. (1997) [Pubmed]
  36. Agonist-dependent up-regulation of human somatostatin receptor type 1 requires molecular signals in the cytoplasmic C-tail. Hukovic, N., Rocheville, M., Kumar, U., Sasi, R., Khare, S., Patel, Y.C. J. Biol. Chem. (1999) [Pubmed]
  37. Bim-23244, a somatostatin receptor subtype 2- and 5-selective analog with enhanced efficacy in suppressing growth hormone (GH) from octreotide-resistant human GH-secreting adenomas. Saveanu, A., Gunz, G., Dufour, H., Caron, P., Fina, F., Ouafik, L., Culler, M.D., Moreau, J.P., Enjalbert, A., Jaquet, P. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  38. Expression and localization of somatostatin receptor SSTR1, SSTR2, and SSTR3 messenger RNAs in primary human tumors using in situ hybridization. Reubi, J.C., Schaer, J.C., Waser, B., Mengod, G. Cancer Res. (1994) [Pubmed]
  39. Cortistatin inhibits growth hormone release from human fetal and adenoma pituitary cells and prolactin secretion from cultured prolactinomas. Rubinfeld, H., Hadani, M., Barkai, G., Taylor, J.E., Culler, M.D., Shimon, I. J. Clin. Endocrinol. Metab. (2006) [Pubmed]
  40. Somatostatin receptor subtype 1 selective activation in human growth hormone (GH)- and prolactin (PRL)-secreting pituitary adenomas: effects on cell viability, GH, and PRL secretion. Zatelli, M.C., Piccin, D., Tagliati, F., Ambrosio, M.R., Margutti, A., Padovani, R., Scanarini, M., Culler, M.D., degli Uberti, E.C. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  41. Somatostatin receptor gene expression in human ocular tissues: RT-PCR and immunohistochemical study. Klisovic, D.D., O'Dorisio, M.S., Katz, S.E., Sall, J.W., Balster, D., O'Dorisio, T.M., Craig, E., Lubow, M. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  42. Expression of somatostatin receptors in normal and cirrhotic human liver and in hepatocellular carcinoma. Reynaert, H., Rombouts, K., Vandermonde, A., Urbain, D., Kumar, U., Bioulac-Sage, P., Pinzani, M., Rosenbaum, J., Geerts, A. Gut (2004) [Pubmed]
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