somatostatin release

FK962 是抑制生长抑素释放的增强剂，具有增强认知效果。

Somatostatin RC 102 is a peptide hormone. It regulates the endocrine system and affects neurotransmission and cell proliferation via interaction with G protein-coupled somatostatin receptors and inhibition of the release of numerous secondary hormones.

SRA880 is a non-peptide somatostatin sst(1) receptor antagonist which displays a significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d)= 6.0) or a wide range of neurotransmitter receptors, except for the human dopamine

AC-178335 is a pure somatostatin (SRIF) antagonist with an affinity constant (Ki) of 172 + - 12 nM. AC-178335 blocks SRIF inhibition of adenylate cyclase in vitro (IC50 = 5.1 + - 1.4 microM). It induces GH release when given alone (50 micrograms intraveno

FK962 is an enhancer of somatostatin release, which exerts cognitive-enhancing actions in rats. FK960 increases synaptic density in the hippocampal CA3 region of aged rats.

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

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.

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

Angiopeptin TFA，一种生长抑素的环状八肽类似物，作为sst2 sst5受体部分激动剂，其IC50值为0.26 nM和6.92 nM。该化合物能够抑制生长激素释放及IGF-1(胰岛素样生长因子-1)的产生，同时抑制腺苷酸环化酶活性或刺激细胞外酸化。Angiopeptin TFA在冠状动脉粥样硬化的研究中显示出潜力。

Gastric Inhibitory Polypeptide (1-30), porcine 缺乏天然胃抑制多肽 (GIP) C 端 12 个氨基酸残基，能够增强胰岛素和生长抑素的释放而发挥生物活性。

[Nle8] Somatostatin (1-28)为生长抑素(1-28)的衍生物，其特征在于第8位的甲硫氨酸被正亮氨酸所替代。该化合物能够促使淀粉酶的释放，并增加胰腺腺泡中的环AMP水平。

Sucrose octasulfate为硫糖铝组分，能直接刺激胃粘膜D细胞以促进生长抑素样免疫反应(SLI)的释放，进而发挥内源性胃生长抑素的溃疡愈合功能，适用于抗胃溃疡研究。

PACAP (1-38) free acid TFA，一种内源性神经肽，能有效促进胃窦运动，增强体液蛋白分泌，同时抑制胃泌素释放。此外，它刺激血管活性肠肽、胃泌素释放肽和P物质的释放，并通过RACK1增强N-甲基-D-天门冬氨酸受体功能及脑源性神经营养因子表达。

PACAP (1-38) free acid 是一种具有多重生物功能的内源性神经肽，主要作用包括刺激胃窦运动、增进体液蛋白分泌、抑制胃泌素分泌，以及促进血管活性肠肽、胃泌素释放肽和P 物质的释放。此外，PACAP (1-38) free acid 通过与RACK1互作，可以增强N-甲基-D-天门冬氨酸受体的功能并促进脑源性神经营养因子的表达。

BIM-23027为高选择性sst2受体激动剂（EC50=0.32 nM），其功能效果类似生长抑素（SRIF，环状十四肽）。该化合物可促进多巴胺的释放，此过程通过Glu依赖的机制进行调控。

PACAP (1-38), a novel neuropeptide isolated from the bovine hypothalamus is more active than vasoactive intestinal peptide (VIP) in stimulating adenylate cyclase (EC50=7 nM). PACAP 1-38 (10-9 M) increased substance P (SP), gastrin releasing peptide (GRP),

Somatostatin, also known as growth hormone-inhibiting hormone, is a naturally-occurring peptide hormone of 14 or 28 amino acid residues that regulates the endocrine system. It is secreted by the D cells of the islets to inhibit the release of insulin and

Galanin (1-30), human, is a 30-amino acid neuropeptide that acts as an agonist of GalR1 and GalR2 receptors with Kis of 1 nM. This endogenous peptide exhibits multiple endocrine, metabolic, and behavioral effects and has demonstrated activity on the intestinal system.

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