More information on this family may be found on the IUPHAR-DB family and introduction pages.
Somatostatin (somatotropin release inhibiting factor) is an abundant neuropeptide, which acts on five subtypes of somatostatin receptor (sst1–sst5; nomenclature approved by the NC-IUPHAR Subcommittee on Somatostatin Receptors, [6]). Activation of these receptors produces a wide range of physiological effects throughout the body including inhibiting the secretion of many hormones. The relationship of the cloned receptors to endogenously expressed receptors is not yet well established in some cases. Endogenous ligands for these receptors are somatostatin-14 (SRIF-14) and somatostatin-28 (SRIF-28). Cortistatin (CST-14) has also been suggested to be an endogenous ligand for somatostatin receptors [3].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Crider, AM; Witt, KA. (2007) Somatostatin sst4 ligands: chemistry and pharmacology. Mini Rev Med Chem, 7 (3): 213-20. [PMID:17346214]
Csaba, Z; Dournaud, P. (2001) Cellular biology of somatostatin receptors. Neuropeptides, 35 (1): 1-23. [PMID:11346306]
Dasgupta, P. (2004) Somatostatin analogues: multiple roles in cellular proliferation, neoplasia, and angiogenesis. Pharmacol Ther, 102: 61-85. [PMID:15056499]
Durán-Prado, M; Malagón, MM; Gracia-Navarro, F; Castaño, JP. (2008) Dimerization of G protein-coupled receptors: new avenues for somatostatin receptor signalling, control and functioning. Mol. Cell. Endocrinol., 286 (1-2): 63-8. [PMID:18242821]
Hannon, JP; Nunn, C; Stolz, B; Bruns, C; Weckbecker, G; Lewis, I; Troxler, T; Hurth, K; Hoyer, D. (2002) Drug design at peptide receptors: somatostatin receptor ligands. J. Mol. Neurosci., 18 (1-2): 15-27. [PMID:11931345]
Hofland, LJ; Feelders, RA; de Herder, WW; Lamberts, SW. (2010) Pituitary tumours: the sst/D2 receptors as molecular targets. Mol. Cell. Endocrinol., 326 (1-2): 89-98. [PMID:20438803]
Hoyer D, Epelbaum J, Feniuk W, Humphrey PPA, Meyerhof W, O'Carroll AM, et al. (2000) Somatostatin receptors. in The IUPHAR Compendium of Receptor Characterization and Classification, 2nd edn. Edited by In: Watson SP, Girdlestone D (eds). IUPHAR Media:. pp. 354–364.
Lahlou, H; Guillermet, J; Hortala, M; Vernejoul, F; Pyronnet, S; Bousquet, C; Susini, C. (2004) Molecular signaling of somatostatin receptors. Ann. N. Y. Acad. Sci., 1014: 121-31. [PMID:15153426]
Moller, L. N., Stidsen, C. E., Hartmann, B. and Holst, J. J. (2003) Somatostatin receptors. Biochim Biophys Acta, 1616: 1-84. [PMID:14507421]
Olias, G; Viollet, C; Kusserow, H; Epelbaum, J; Meyerhof, W. (2004) Regulation and function of somatostatin receptors. J. Neurochem., 89 (5): 1057-91. [PMID:15147500]
Patel, Y. C. (1999) Somatostatin and its receptor family. Front Neuroendocrinol, 20: 157-198. [PMID:10433861]
Patel, Y. C., Greenwood, M. T., Panetta, R., Demchyshyn, L., Niznik, H. and Srikant, C. B. (1995) The somatostatin receptor family. Life Sci, 57: 1249-1265. [PMID:7674817]
Rashid, AJ; O'Dowd, BF; George, SR. (2004) Minireview: Diversity and complexity of signaling through peptidergic G protein-coupled receptors. Endocrinology, 145 (6): 2645-52. [PMID:15044354]
Siehler, S; Nunn, C; Hannon, J; Feuerbach, D; Hoyer, D. (2008) Pharmacological profile of somatostatin and cortistatin receptors. Mol. Cell. Endocrinol., 286 (1-2): 26-34. [PMID:18243519]
van der Hoek, J; Hofland, LJ; Lamberts, SW. (2005) Novel subtype specific and universal somatostatin analogues: clinical potential and pitfalls. Curr. Pharm. Des., 11 (12): 1573-92. [PMID:15892663]
Van Op den Bosch, J; Adriaensen, D; Van Nassauw, L; Timmermans, JP. (2009) The role(s) of somatostatin, structurally related peptides and somatostatin receptors in the gastrointestinal tract: a review. Regul. Pept., 156 (1-3): 1-8. [PMID:19362110]
Weckbecker, G; Lewis, I; Albert, R; Schmid, HA; Hoyer, D; Bruns, C. (2003) Opportunities in somatostatin research: biological, chemical and therapeutic aspects. Nat Rev Drug Discov, 2 (12): 999-1017. [PMID:14654798]
Zatelli, MC; degli Uberti, E. (2009) The significance of new somatostatin analogs as therapeutic agents. Curr Opin Investig Drugs, 10 (10): 1025-31. [PMID:19777390]
1. Bruns, C., Raulf, F., Hoyer, D., Schloos, J., Lubbert, H. and Weckbecker, G. (1996) Binding properties of somatostatin receptor subtypes. Metabolism, 45: 17-20. [PMID:8769372]
2. Castro, SW; Buell, G; Feniuk, W; Humphrey, PP. (1996) Differences in the operational characteristics of the human recombinant somatostatin receptor types, sst1 and sst2, in mouse fibroblast (Ltk-) cells. Br. J. Pharmacol., 117 (4): 639-46. [PMID:8646408]
3. De Lecea, L., Criado, J. R., Prospero-Garcia, O., Gautvik, K. M., Schweitzer, P., Danielson, P. E., Dunlop, C. L., Siggins, G. R., Henriksen, S. J. and Sutcliffe, J. G. (1996) A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature, 381: 242-245. [PMID:8622767]
4. Erchegyi, J., Hoeger, C. A., Low, W., Hoyer, D., Waser, B., Eltschinger, V., Schaer, J. C., Cescato, R., Reubi, J. C. and Rivier, J. E. (2005) Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan. J Med Chem, 48: 507-514. [PMID:15658864]
5. Holloway, S; Feniuk, W; Kidd, EJ; Humphrey, PP. (1996) A quantitative autoradiographical study on the distribution of somatostatin sst2 receptors in the rat central nervous system using [125I]-BIM-23027. Neuropharmacology, 35 (8): 1109-20. [PMID:9121614]
6. Hoyer D, Epelbaum J, Feniuk W, Humphrey PPA, Meyerhof W, O'Carroll AM, et al. (2000) Somatostatin receptors. in The IUPHAR Compendium of Receptor Characterization and Classification, 2nd edn. Edited by In: Watson SP, Girdlestone D (eds). IUPHAR Media:. pp. 354–364.
7. Hoyer, D., Nunn, C., Hannon, J., Schoeffter, P., Feuerbach, D., Schuepbach, E., Langenegger, D., Bouhelal, R., Hurth, K., Neumann, P., Troxler, T. and Pfaeffli, P. (2004) SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist. Neurosci Lett, 361: 132-135. [PMID:15135911]
8. Hoyer, D., Vassout, A., Gentsch, C., Enz, A., Vigouret, J. M., Jaton, A., Schoeffter, P., Kelly, P., Wrynn, A., Hurth, K. and Troxler, T. (2004) Functional characterization of NVP ACQ090, a somatostatin sst3 receptor antagonist. Soc Neuroscience Abs, : -.
9. Liu, S., Tang, C., Ho, B., Ankersen, M., Stidsen, C. E. and Crider, A. M. (1998) Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas. J Med Chem, 41: 4693-4705. [PMID:9822540]
10. Meyerhof, W. (1998) The elucidation of somatostatin receptor functions: a current view. Rev Physiol Biochem Pharmacol, 133: 55-108. [PMID:9600011]
11. Nunn, C., Schoeffter, P., Langenegger, D. and Hoyer, D. (2003) Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806. Naunyn Schmiedebergs Arch Pharmacol, 367: 1-9. [PMID:12616335]
12. Patel, Y. C. and Srikant, C. B. (1994) Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). Endocrinology, 135: 2814-2817. [PMID:7988476]
13. Rohrer, S. P., Birzin, E. T., Mosley, R. T., Berk, S. C., Hutchins, S. M., Shen, D. M., Xiong, Y., Hayes, E. C., Parmar, R. M., Foor, F., Mitra, S. W., Degrado, S. J., Shu, M., Klopp, J. M., Cai, S. J., Blake, A., Chan, W. W., Pasternak, A., Yang, L., Patchett, A. A., Smith, R. G., Chapman, K. T. and Schaeffer, J. M. (1998) Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science, 282: 737-740. [PMID:9784130]
14. Siehler, S., Seuwen, K. and Hoyer, D. (1998) [125I]Tyr10-cortistatin14 labels all five somatostatin receptors. Naunyn Schmiedebergs Arch Pharmacol, 357: 483-489. [PMID:9650799]
15. Siehler, S., Seuwen, K. and Hoyer, D. (1998) [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur J Pharmacol, 348: 311-320. [PMID:9652348]
16. Siehler, S., Seuwen, K. and Hoyer, D. (1999) Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn Schmiedebergs Arch Pharmacol, 360: 488-499. [PMID:10598788]
17. Tulipano, G., Soldi, D., Bagnasco, M., Culler, M. D., Taylor, J. E., Cocchi, D. and Giustina, A. (2002) Characterization of new selective somatostatin receptor subtype-2 (sst2) antagonists, BIM-23627 and BIM-23454. Effects of BIM-23627 on GH release in anesthetized male rats after short-term high-dose dexamethasone treatment. Endocrinology, 143: 1218-1224. [PMID:11897676]
18. Yang, L., Berk, S. C., Rohrer, S. P., Mosley, R. T., Guo, L., Underwood, D. J., Arison, B. H., Birzin, E. T., Hayes, E. C., Mitra, S. W., Parmar, R. M., Cheng, K., Wu, T. J., Butler, B. S., Foor, F., Pasternak, A., Pan, Y., Silva, M., Freidinger, R. M., Smith, R. G., Chapman, K., Schaeffer, J. M. and Patchett, A. A. (1998) Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc Natl Acad Sci U S A, 95: 10836-10841. [PMID:9724791]
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[125I]Tyr11-SRIF-14, [125I]LTT-SRIF-28, [125I]CGP 23996 and [125I]Tyr10-CST14 may be used to label somatostatin receptors nonselectively; BIM 23052 is said to be selective in rat but not human receptor [12]. A number of nonpeptide subtype-selective agonists have been synthesised [13].