| Chemical Properties | Back Directory | [form ]
Solid | [color ]
White to light yellow | [Sequence]
Ac-{L-4-NO2-Phe}{D-CYS}-Tyr-{D-TRP}-Lys-Thr-Cys{D-TYR}-NH2 (Disulfidebridge:Cys2-Cys7) |
| Hazard Information | Back Directory | [Uses]
CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively[1][2]. | [in vivo]
CYN 154806 TFA (0.1 mg/kg; i.p.; 20 min before the administration of carbachol (CCh) (30 μg/kg) in M4 KO mice) dose-dependently and significantly reverses the decreases acid response to CCh in M4 but not M3 KO mice[3]. | [IC 50]
SSTR2 | [References]
[1] Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50(4):709-15. PMID:8863814
[2] Feniuk W, et al. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39(8):1443-50. DOI:10.1016/s0028-3908(00)00035-6
[3] Takeuchi K, et al. Activation of Muscarinic Acetylcholine Receptor Subtype 4 Is Essential for Cholinergic Stimulation of Gastric Acid Secretion: Relation to D Cell/Somatostatin. Front Pharmacol. 2016 Aug 30;7:278. DOI:10.3389/fphar.2016.00278 |
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