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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.
M. Wt | 4041.69 |
Formula | C183H307N49O53 |
Sequence |
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 |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility | Soluble to 1 mg/ml in water |
References are publications that support the biological activity of the product.
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.
Keywords: Astressin 2B, Astressin 2B supplier, Selective, CRF2, antagonists, Corticotropin-Releasing, Factor2, Receptors, Astressin2B, 2391, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Astressin 2B include:
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
Do you know of a great paper that uses Astressin 2B from Tocris? Please let us know.
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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.