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Submit ReviewAstressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist (IC50 values are 1.3 and > 500 nM for CRF2 and CRF1 respectively). Antagonizes CRF2-mediated inhibition of gastric emptying.
分子量 | 4041.69 |
公式 | C183H307N49O53 |
序列 |
DLSFHLLRKXIEIEKQEKEKQQAENNKLLLDLI (Modifications: Asp-1 = N-terminal Ac, Phe-4 = D-Phe, Leu-6 = α-methyl-Leu, X = Nle, Glu-24 = γ-Glu, Lys-27 = ε-Lys, Leu-32 = α-methyl-Leu, Ile-33 = C-terminal amide, Lactam Bridge: Glu-24 - L |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 681260-70-8 |
PubChem ID | 90488758 |
InChI Key | IVIBPRHVUKMKSX-YJHXGIRISA-N |
Smiles | CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@](C)(CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H](CC1=CC=CC=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(C)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@](C)(CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
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溶解性 | Soluble to 1 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Rivier et al (2002) Potent and long-acting cortico. releasing factor (CRF) receptor 2 selective peptide competitive antagonists. J.Med.Chem. 45 4737 PMID: 12361401
Hoare et al (2005) Peptide ligand binding properties of the corticotropin-releasing factor (CRF) type 2 receptor: pharmacology of endogenously expressed receptors, G-protein-coupled sensitivity and determinants of CRF2 receptor selectivity. Peptides 26 457 PMID: 15652653
Henry et al (2006) The effect of lateral septum corticotropin-releasing factor receptor 2 activation on anxiety is modulated by stress. J.Neurosci. 26 9142 PMID: 16957071
If you know of a relevant reference for Astressin 2B, please let us know.
关键词: Astressin 2B, Astressin 2B supplier, Selective, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, Astressin2B, 2391, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Astressin 2B 的部分引用包括:
Boyson et al (2014) Social stress and CRF-DA interactions in the VTA: role in long-term escalation of cocaine self-administration. J Neurosci 34 6659 PMID: 24806691
Rodriguez et al (2015) Diminished expression of CRHR2 in human colon cancer promotes tumor growth and EMT via persistent IL-6/Stat3 signaling. Cell Mol Gastroenterol Hepatol 1 610 PMID: 26495412
Martinon and Dabrowska (2018) Corticotropin-Releasing Factor Receptors Modulate OXT Release in the Dorsolateral Bed Nucleus of the Stria Terminalis (BNST) in Male Rats. Front Neurosci 12 183 PMID: 29618970
Li et al (2018) Ablation of somatostatin cells leads to impaired pancreatic islet function and neonatal death in rodents. Cell Death Dis 9 682 PMID: 29880854
Kash et al (2008) DA enhances fast excitatory synaptic transmission in the extended amygdala by a CRF-R1-dependent process. Invest Ophthalmol Vis Sci 28 13856 PMID: 19091975
Abdelhamid et al (2013) Forced swim-induced musculoskeletal hyperalgesia is mediated by CRF2 receptors but not by TRPV1 receptors. Neuropharmacology 72 29 PMID: 23624287
Silberman and Winder (2013) Corticotropin releasing factor and catecholamines enhance glutamatergic neurotransmission in the lateral subdivision of the central amygdala. Neuropharmacology 70 316 PMID: 23470280
Tran et al (2014) Importance of CRF receptor-mediated mechanisms of the bed nucleus of the stria terminalis in the processing of anxiety and pain. Neuropsychopharmacology 39 2633 PMID: 24853772
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.