somatostatin receptor agonist

Octreotide (SMS 201-995) is a potent inhibitor of growth hormone, glucagon, and insulin.

The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5

Branosotine (compound 1-1) acts as a potent agonist for the somatostatin receptor (SSTR2), exhibiting an EC50 of less than 0.1 nM.

SSTR4agonist-1 (Compound 47) is a selective agonist of the somatostatin receptor 4 (SSTR4), with an EC50 of 4.7 nM. It has a half-life of over 130 minutes in human liver microsomes.

SSTR4 agonist5 (Compound 5) is an orally active agonist of the somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. It demonstrates good stability in human/rat liver microsomes and can inhibit mechanical hyperalgesia in rat models.

somatostatin sst2 receptor agonist

somatostatin sst5 receptor agonist

Somatostatin sst4 receptor agonist

TC-G1003 is an effective agonist of the somatostatin sst2 receptor.

L-779,976 is an agonist of somatostatin receptor.

L-797,591 is a selective agonist of somatostatin receptor subtype 1.

Seglitide acetate (MK-678) is a selective agonist of sst2 somatostatin receptor.

L-796,778 acetate is a slective somatostatin receptor agonist with IC50 of 24nM for sst3, for sst1, sst2, sst4 and sst5, IC50 is >1000nM.

Neuromedin C is a bombesin-like neuropeptide that stimulates uterine smooth muscle contraction and the release of gastrin , somatostatin, and amylase in rats. Neuromedin C is a truncated form of gastrin-releasing peptide corresponding to the GRP amino acids 18-27. It inhibits GRP and bombesin binding to rat pancreatic membranes (IC50s = 0.4 and 2.2 nM, respectively), which can be reduced by sodium chloride and guanylyl imidodiphosphate . Neuromedin C induces scratching and mast cell degranulation in mice when administered intradermally at doses ranging from 1 to 300 nmol/site, which is inhibited by the BB2 bombesin receptor agonist RC-3095 and reduced in mast cell-deficient mice. Neuromedin C (3.2 nmol/kg, i.p.) reduces rat glucose consumption by approximately 50% for up to one hour.

Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across isolated goby posterior intestine in 5% seawater-adapted solution.3In vivo, urotensin II (1.5-150 nmol/kg) decreases diastolic blood pressure and increases heart rate in anesthetized rats.4It also reduces the pressor responses to sympathetic nerve stimulation, norepinephrine , and vasopressin in pithed rats when administered at a dose of 150 nmol/kg. 1.Ames, R.S., Sarau, H.M., Chambers, J.K., et al.Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14Nature401(6750)282-286(1999) 2.Loretz, C.A., and Assad, J.A.Urotensin II lowers cytoplasmic free calcium concentration in goby enterocytes: Measurements using quin2Gen. Comp. Endocrinol.64(3)355-361(1986) 3.Loretz, C.A., Freel, R.W., and Bern, H.A.Specificity of response of intestinal ion transport systems to a pair of natural peptide hormone analogs: Somatostatin and urotensin IIGen. Comp. Endocrinol.52(2)198-206(1983) 4.Gibson, A., Wallace, P., and Bern, H.A.Cardiovascular effects of urotensin II in anesthetized and pithed ratsGen. Comp. Endocrinol.64(3)435-439(1986)

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

SSTR4 agonist 2 is a potent somatostatin receptor subtype 4 (SSTR4) agonist with potential applications in research on SSTR4-related medical disorders. The SSTR4 pathway inhibits nociceptive and inflammatory processes [1].

J-2156 TFA is a selective SST4 receptor (somatostatin receptor type 4) agonist with IC50 values of 0.05 nM and 0.07 nM for human and rat SST4 receptors respectively. It exhibits anti-inflammatory and analgesic effects while reducing pERK levels.

Paltusotine, also known as CRN00808, is a somatostatin receptor agonist.

Pasireotide diaspartate (SOM230), a long-acting cyclohexapeptide and somatostatin analog, enhances agonist activity across somatostatin receptor subtypes (sst1/2/3/4/5, with pK i values of 8.2, 9.0, 9.1, <7.0, and 9.9, respectively). This compound demonstrates antisecretory, antiproliferative, and proapoptotic activities [1] [2].

Octreotide, a cyclic SSTR agonist, serves as the cyclic Somatostatin Receptor SSTR agonist [1].

BIM-23027 is a selective sst 2 receptor agonist (EC 50 = 0.32 nM) with effects analogous to the cyclic tetradecapeptide somatostatin (SRIF). It promotes dopamine release through a Glu-dependent mechanism [1] [2].

Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients

DSPE-PEG1000-Octreotide, a PEG compound formed from DSPE and Octreotide, acts as a somatostatin receptor agonist. Octreotide exhibits antitumor properties and induces apoptosis, making it useful in researching acromegaly. Additionally, DSPE-PEG1000-Octreotide is applicable in drug delivery.