CYN 154806是一种环状八肽，是一种强效的、选择性的生长抑素sst2受体（pIC50=8.58）拮抗剂。
Cas No.:183658-72-2
Sample solution is provided at 25 µL, 10mM.
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CYN 154806 is a cyclic octapeptide and a potent, selective somatostatin sst2 receptor antagonist (pIC₅₀=8.58). CYN 154806 also inhibits sst1, sst3, sst4, and sst5 receptors[1-2]. CYN 154806 is applicable in research areas such as neuroscience, endocrinology, and pharmacology[3-4].
In vitro, pretreatment of rat pituitary GC cells with CYN 154806 (1nM to 1µM) for 30 minutes, followed by stimulation with somatostatin (10nM) or octreotide (10nM). CYN 154806 completely abolished the sst2 receptor-mediated decrease in intracellular free calcium concentration ([Ca²⁺]i) and the inhibition of Ca²⁺ transients[5]. Pretreatment of rat pituitary tumor GC cells with CYN 154806 (0.1µM) for 30 minutes, prior to stimulation with somatostatin or the sst2 receptor-selective agonist octreotide (1nM to 1µM). CYN 154806 significantly antagonized the following sst2 receptor-mediated inhibitory effects[6].
In vivo, bilateral microinjection of CYN 154806 (60-240ng/0.5µl/side) into the rat ventral pallidum/substantia innominata (VP/SI) reversed the somatostatin- and sst2 receptor agonist MK678-induced decrease in locomotor activity[7]. Intrathecal pretreatment of Slick-/- knockout mice, Lbx1-Slick-/- conditional knockout mice, and their respective wild-type controls with CYN 154806 (500ng in 5µl of 0.9% NaCl) 30 minutes before injecting capsaicin (5µg) into the hind paw. CYN 154806 prevented the capsaicin-induced prolonged licking behavior in Slick-/- and Lbx1-Slick-/- mice[8].
References:
[1] Nunn C, Schoeffter P, Langenegger D, et al. Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806. Naunyn Schmiedebergs Arch Pharmacol. 2003 Jan;367(1):1-9.
[2] Feniuk W, Jarvie E, Luo J, et al. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39(8):1443-50.
[3] Hannon JP, Nunn C, Stolz B, et al. Drug design at peptide receptors: somatostatin receptor ligands. J Mol Neurosci. 2002 Feb-Apr;18(1-2):15-27.
[4] Foong JP, Parry LJ, Gwynne RM, et al. 5-HT(1A), SST(1), and SST(2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum. Am J Physiol Gastrointest Liver Physiol. 2010 Mar;298(3):G384-94.
[5] Cervia D, Petrucci C, Bluet-Pajot MT, et al. Inhibitory control of growth hormone secretion by somatostatin in rat pituitary GC cells: sst(2) but not sst(1) receptors are coupled to inhibition of single-cell intracellular free calcium concentrations. Neuroendocrinology. 2002 Aug;76(2):99-110.
[6] Cervia D, Fiorini S, Pavan B, et al. Somatostatin (SRIF) modulates distinct signaling pathways in rat pituitary tumor cells; negative coupling of SRIF receptor subtypes 1 and 2 to arachidonic acid release. Naunyn Schmiedebergs Arch Pharmacol. 2002 Mar;365(3):200-9.
[7] Flauaus C, Engel P, Zhou F, et al. Slick Potassium Channels Control Pain and Itch in Distinct Populations of Sensory and Spinal Neurons in Mice. Anesthesiology. 2022 May 1;136(5):802-822.
[8] Marazioti A, Kastellakis A, Antoniou K, et al. Somatostatin receptors in the ventral pallidum/substantia innominata modulate rat locomotor activity. Psychopharmacology (Berl). 2005 Sep;181(2):319-26.
CYN 154806是一种环状八肽，是一种强效的、选择性的生长抑素sst2受体（pIC50=8.58）拮抗剂。CYN 154806对sst1、sst3、sst4和sst5受体均有抑制作用[1-2]。CYN 154806可用于神经科学、内分泌学和药理学等相关研究[3-4]。
在体外，CYN 154806（1nM至1µM）预处理大鼠垂体GC细胞30分钟，随后以生长抑素（10nM）或奥曲肽（10nM）进行刺激，CYN 154806可完全拮抗由sst2受体介导的细胞内游离钙浓度（[Ca²⁺]i）降低及钙瞬变抑制作用[5]。CYN 154806（0.1µM）预处理大鼠垂体肿瘤细胞（GC cells）30min，随后以生长抑素或sst2受体选择性激动剂奥曲肽（1nM至1µM），CYN 154806可显著拮抗通过sst2受体介导的下列抑制作用[6]。
在体内，CYN 154806（60-240ng/0.5μl/side）双侧注射到大鼠腹侧苍白球/无名质（VP/SI）。CYN 154806逆转了生长抑素和sst2受体激动剂MK678诱导的运动活动减少[7]。CYN 154806（500ng in 5μl 0.9%NaCl）鞘内注射预处理Slick-/-基因敲除小鼠、Lbx1-Slick-/-条件性基因敲除小鼠及其各自的野生型对照小鼠30min，随后将辣椒素（5μg）注射到小鼠后足掌。CYN 154806预处理阻止了Slick-/-小鼠和Lbx1-Slick-/-小鼠中由辣椒素诱导的延长舔爪行为[8]。
| Cell experiment [1]: | |
Cell lines | Rat pituitary tumor GC cells |
Preparation Method | GC cells were maintained in Dulbecco's modified Eagle's medium nutrient mixture F-12 Ham (DME-F12) supplemented with 15% heat-inactivated horse serum and 2.5% bovine calf serum at 37°C, 5% CO₂. Cells were pretreated with the sst2 receptor antagonist CYN 154806 (1nM-1µM). |
Reaction Conditions | 1nM-1µM; 30 minutes. |
Applications | CYN 154806 (100nM) pretreatment for 30 minutes abolished the inhibition of intracellular free calcium concentration ([Ca²⁺]i) and Ca²⁺ transients induced by somatostatin (SRIH; 10nM) or the sst2 receptor agonist octreotide (10nM), demonstrating its antagonistic property at sst2 receptors concerning Ca²⁺ signaling. Furthermore, CYN 154806 alone potently and concentration-dependently inhibited basal growth hormone (GH) secretion. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Rats were bilaterally microinjected with the selective sst2 receptor antagonist CYN 154806 (60-240ng/0.5μl/side), alone or in combination with somatostatin (SRIF) or the sst2 agonist MK678, into the ventral pallidum/substantia innominata (VP/SI) brain region. Locomotor activity was measured for 60 minutes post-injection. |
Dosage form | 60-240ng/0.5μl/side; intracerebral microinjection; single injections. |
Applications | CYN 154806 (120ng/0.5μl/side) partially reversed the somatostatin (60ng/0.5μl/side)-induced decrease in locomotor activity. Furthermore, CYN 154806 (240ng/0.5μl/side) completely blocked the locomotor activity attenuation caused by the sst2 agonist MK678 (240ng/0.5μl/side). When administered alone at doses of 60, 120, and 240ng/0.5μl/side, CYN 154806 had no significant effect on spontaneous locomotor activity. |
References: | |
| Cas No. | 183658-72-2 | SDF | |
| 化学名 | (4R,4Z,5Z,7S,8Z,10S,11Z,13R,14Z,16S,17Z,19S)-13-((1H-indol-3-yl)methyl)-10-(4-aminobutyl)-6,9,12,15,18-pentahydroxy-19-((Z)-((S)-1-hydroxy-2-((Z)-(1-hydroxyethylidene)amino)-3-(4-nitrophenyl)propylidene)amino)-N-((R)-1-hydroxy-3-(4-hydroxyphenyl)-1-iminop | ||
| Canonical SMILES | C[C@](O)([H])[C@@]1([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC2=CC=C(O)C=C2)([H])CSSC[C@](/N=C(O)/[C@](/N=C(O)/C)([H])CC3=CC=C(N(=O)=O)C=C3)([H])/C(O)=N/[C@@](/C(O)=N/[C@](/C(O)=N/[C@@](/C(O)=N/1)([H])CCCCN)([H])CC4=CNC5=CC=CC=C45)([H])CC6=CC=C(O)C=C6 | ||
| 分子式 | C56H68N12O14S2 | 分子量 | 1197.35 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Desiccate at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 835.2 μL | 4.1759 mL | 8.3518 mL |
| 5 mM | 167 μL | 835.2 μL | 1.6704 mL |
| 10 mM | 83.5 μL | 417.6 μL | 835.2 μL |
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