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Submit ReviewJNJ 5207852 dihydrochloride
说明： High affinity H3 antagonist
化学名： 1-[3-[4-(1-Piperidinylmethyl)phenoxy]propyl]piperidine hydrochloride
纯度： ≥99% (HPLC)
生物活性 for JNJ 5207852 dihydrochloride
JNJ 5207852 dihydrochloride is a high affinity histamine H3 receptor neutral antagonist (pKi values are 8.9 and 9.2 in rat and human respectively). Brain penetrant and orally active. Has 3- and 100-fold higher affinity than thioperamide (Cat. No. 0644) for rat and human H3 receptors respectively. Suppresses slow-wave sleep; exhibits wake-promoting effects in rodent arousal models.
许可信息
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
技术数据 for JNJ 5207852 dihydrochloride
| 分子量 | 389.4 |
| 公式 | C20H32N2O.2HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1782228-76-5 |
| PubChem ID | 90488903 |
| InChI Key | RLLXSVVZCGBIJR-UHFFFAOYSA-N |
| Smiles | C1(CN2CCCCC2)=CC=C(OCCCN3CCCCC3)C=C1.Cl.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.
溶解性数据 for JNJ 5207852 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 19.47 | 50 | |
| DMSO | 7.79 | 20 温和加热 |
制备储备液 for JNJ 5207852 dihydrochloride
以下数据基于产品分子量 389.4。 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 |
|---|---|---|---|
| 0.5 mM | 5.14 mL | 25.68 mL | 51.36 mL |
| 2.5 mM | 1.03 mL | 5.14 mL | 10.27 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 25 mM | 0.1 mL | 0.51 mL | 1.03 mL |
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产品说明书 for JNJ 5207852 dihydrochloride
参考文献 for JNJ 5207852 dihydrochloride
参考文献是支持产品生物活性的出版物。
Barbier et al (2004) Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br.J.Pharmacol. 143 649 PMID: 15466448
Jia et al (2005) Effects of histamine H3 antagonists and donep. on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology 50 404 PMID: 16310812
Le et al (2008) Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J.Pharmacol.Exp.Ther. 325 902 PMID: 18305012
If you know of a relevant reference for JNJ 5207852 dihydrochloride, please let us know.
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关键词: JNJ 5207852 dihydrochloride, JNJ 5207852 dihydrochloride supplier, JNJ5207852, histamine, receptor, H3, neutral, antagonist, antagonists, Histamine, Receptors, 4020, Tocris Bioscience
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