Somatostatin Receptor Agonist

Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.

CH 275 is a peptidic somatostatin analog that acts as an agonist of SST1 (IC₅₀ = 30.9 nM, K_i = 52 nM). The IC₅₀ values of CH 275 for sst3, sst4, sst2, and sst5 are 345 nM, >1 μM, >10 μM, and >10 μM, respectively. CH 275 binds to SSTR1 via the IAmp9-Asp137 ion pair interaction and the hydrophobic interaction between the isopropyl group of IAmp9 and Leu107, and reduces the extracellular acidification rate. CH 275 induces weak sst1 internalization, exerts immunosuppressive effects on macrophages, and decreases macrophage viability, MCP-1 expression/secretion, and IL-8 secretion, but does not alter proMMP-9 secretion or IL-8 mRNA levels. CH 275 reduces hippocampal β-amyloid levels and alleviates plaque pathology without inducing hippocampal microglial activation. CH 275 is used in research on Alzheimer's disease, Parkinson's disease, and depression.

L-797591 hydrochloride is a selective sst₁ agonist. L-797591 hydrochloride mimicks the effects of SRIF-14 and SRIF-28 by potently inhibiting either Forskolin (HY-15371)-stimulated or CRH-stimulated cAMP accumulation.

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST₄ receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST₄ receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.

Mazisotine (CNTX-0290) is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC₅₀ of 4.7 nM. Mazisotine exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine can be used for pain research.

Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.

TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.

Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity.

BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits K_i values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.

L-796778 acetate is a selective agonist of the sst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 acetate is a partial agonist that inhibits Forskolin (HY-15371)-stimulated cAMP production with an IC₅₀ value of 18 nM. L-796778 acetate has anticonvulsant effect.

L-803087 is a potent and selective somatostatin sst4 receptor agonist with a K_i of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent

Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR₂) agonist, and also a competitive antagonist of SSTR₁₄, SSTR₂₅, and SSTR₂₈. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes.

Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28.

Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.

Alkyne-βAG-TOCA, an octreotide derivative, targets somatostatin receptor type 2 (SST2). Alkyne-βAG-TOCA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst₂/sst₅ receptor partial agonist with IC₅₀ values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.