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Submit ReviewNBI 27914 hydrochloride is a selective, non-peptide corticotropin-releasing factor1 (CRF1) receptor antagonist (Ki = 1.7 nM); has no activity at CRF2 receptors. Blocks behavioral seizures in vivo.
NBI 27914 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 470.66 |
公式 | C18H20Cl4N4.HCl |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 1215766-76-9 |
PubChem ID | 45073446 |
InChI Key | CPMGENCTAWBLNW-UHFFFAOYSA-N |
Smiles | Cl.CCCN(CC1CC1)C1=C(Cl)C(NC2=C(Cl)C=C(Cl)C=C2Cl)=NC(C)=N1 |
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。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 43.42 | 100 | |
DMSO | 43.42 | 100 |
以下数据基于产品分子量 470.66。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.12 mL | 10.62 mL | 21.25 mL |
5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Baram et al (1997) The CRF1 receptor mediates the excitatory actions of cortico. releasing factor (CRF) in the developing rat brain: in vivo evidence using a novel, selective, non-peptide CRF receptor antagonist. Brain Res. 770 89 PMID: 9372207
Chen et al (1996) Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J.Med.Chem. 39 4358 PMID: 8893829
McCarthy et al (1999) Recent advances with the CRF1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications. Curr.Pharm.Des. 5 289 PMID: 10213797
If you know of a relevant reference for NBI 27914 hydrochloride, please let us know.
关键词: NBI 27914 hydrochloride, NBI 27914 hydrochloride supplier, Selective, non-peptide, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, NBI27914, hydrochloride, 1591, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NBI 27914 hydrochloride 的部分引用包括:
Navarro et al (2015) Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. Stroke 35 6639 PMID: 25926444
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
Lowery-Gionta et al (2012) Corticotropin releasing factor signaling in the central amygdala is recruited during binge-like ethanol consumption in C57BL/6J mice. J Neurosci 32 3405 PMID: 22399763
Gallopin et al (2006) Cortical sources of CRF, NKB, and CCK and their effects on pyramidal cells in the neocortex. J Neurosci 16 1440 PMID: 16339088
Jia et al (2013) Role of nesfatin-1 in a rat model of visceral hypersensitivity. Cereb Cortex 19 3487 PMID: 23801843
Wang et al (2011) CRF receptor antagonist astressin-B reverses and prevents alopecia in CRF over-expressing mice. PLoS One 6 e16377 PMID: 21359208
Gutknecht et al (2008) Expression, binding, and signaling properties of CRF2(a) receptors endogenously expressed in human retinoblastoma Y79 cells: passage-dependent regulation of functional receptors. J Neurochem 104 926 PMID: 17976162
Rajbhandari et al (2015) Predator Stress-Induced CRF Release Causes Enduring Sensitization of Basolateral Amygdala NE Systems that Promote PTSD-Like Startle Abnormalities. J Neurosci 35 14270 PMID: 26490866
Ji et al (2013) Non-pain-related CRF1 activation in the amygdala facilitates synaptic transmission and pain responses. Mol Pain 9 2 PMID: 23410057
Liu et al (2010) Differential actions of urocortins on neurons of the myenteric division of the enteric nervous system in guinea pig distal colon. Br J Pharmacol 159 222 PMID: 20002096
Delawary et al (2010) NMDAR2B tyrosine phosphorylation regulates anxiety-like behavior and CRF expression in the amygdala. Mol Brain 3 37 PMID: 21118530
Nakamura and Sapru (2009) Cardiovascular responses to microinjections of urocortins into the NTS: role of inotropic glutamate receptors. Am J Physiol Heart Circ Physiol 296 H2022 PMID: 19395554
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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.