Somatostatin Receptor
Somatostatin is a naturally occurring inhibitory polypeptide hormone first isolated from the sheep hypothalamus, two biological forms of somatostatin exist: somatostatin-14 and -28, which are derived from a 92-amino acid pro-somatostatin precursor. Somatostatin and its analogs bind to receptors belonging to the seven transmembrane G protein coupled receptor superfamily. Native somatostatin-14 binds to somatostatin receptor (SSTR) 1–4 with higher affinity, while somatostatin-28 is more SSTR5 selective. Octreotide and lanreotide, on the other hand, bind preferentially to SSTR2, with moderate affinity for SSTR5 and SSTR3. All SSTRs associate with the pertussis toxin-sensitive Gi protein and are coupled to adenylate cyclase. Ligand binding triggers the recruitment of membrane adaptors/enzymes and the activation/inhibition of cytoplasmic targets, leading to multiple intracellular signaling pathways, some but not all of which are pertussis toxin sensitive (Gi dependent). While SSTR signal transduction pathways share certain similarities, differences between the SSTRs ensure that each receptor is responsible for a range of different actions. SSTR1, 2, and 3 transduce their antiproliferative action by stimulating one or more PTPs, which in turn affects the mitogenic MAPK and the survival PI3K pathways. In contrast, SSTR5 mediates its antiproliferative action through PTP-independent pathways. Increased understanding of SSTR signaling and function has highlighted the antiproliferative role of somatostatin and provided the rationale for the design of novel somatostatin analogs and therapeutics.
References
1.Theodoropoulou M, et al. Front Neuroendocrinol. 2013;34(3):228–252.
References
1.Theodoropoulou M, et al. Front Neuroendocrinol. 2013;34(3):228–252.
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Somatostatin Receptor
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CH 275
catalog no : M30709
cas no: 174688-78-9
Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens. -
CYN 154806
catalog no : M30575
cas no: 183658-72-2
CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist, The pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively. -
Somatostatin-28 1-14
catalog no : M30521
cas no: 79243-10-0
Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28. Somatostatin 28 arises from the posttranslational cleavage of prosomatostatin, which in turn is derived from a large precursor, preprosomatostatin. -
Cortistatin-14
catalog no : M30269
cas no: 186901-48-4
Cortistatin 14 is a neuropeptide expressed in inhibitory neurons of the cerebral cortex. Depresses neuronal activity, and induces slow-wave sleep, likely through antagonism of acetylcholine. It is structurally and functionally similar to somatostatin 14. Competes with somatostatin 14 for binding of somatostatin receptors (IC50s=5, 0.09, 0.3, 0.2, and 0.3nM for receptors sst1-5, respectively). -
CYN 154806 TFA(183658-72-2 free base)
catalog no : M30045
cas no: ——
CYN 154806 (TFA) is a cyclic octapeptide and an effective selective somatostatin sst2 receptor antagonist. For the recombinant sst2, sst1, sst3, sst4 and sst5 receptors, the pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48, respectively.