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Submit ReviewNBI 35965 hydrochloride is a potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.
NBI 35965 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 | 437.79 |
公式 | C21H22Cl2N4.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1782228-59-4 |
PubChem ID | 71433630 |
InChI Key | LNYUWBPFYXPUIO-RSAXXLAASA-N |
Smiles | CC[C@@H]3N(CC5CC5)C1=C2C(C(C4=CC=C(Cl)C=C4Cl)=NN2C3)=NC(C)=C1.Cl |
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 | |||
water | 43.78 | 100 | |
DMSO | 43.78 | 100 |
以下数据基于产品分子量 437.79。 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 | 2.28 mL | 11.42 mL | 22.84 mL |
5 mM | 0.46 mL | 2.28 mL | 4.57 mL |
10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
参考文献是支持产品生物活性的出版物。
Million et al (2003) A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 985 32 PMID: 12957366
Hoare et al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751 PMID: 12606786
Gross et al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780 PMID: 16134945
If you know of a relevant reference for NBI 35965 hydrochloride, please let us know.
关键词: NBI 35965 hydrochloride, NBI 35965 hydrochloride supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, antagonists, CRF1, Receptors, 3100, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NBI 35965 hydrochloride 的部分引用包括:
Abdelhamid et al (2013) Forced swim-induced musculoskeletal hyperalgesia is mediated by CRF2 receptors but not by TRPV1 receptors. Neuropharmacology 72 29 PMID: 23624287
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
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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.