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Submit ReviewR-96544 hydrochloride
说明： Potent, selective 5-HT2A antagonist
化学名： (2R,4R)-5-[2-[2-[2-(3-Methoxyphenyl)ethyl]phenoxy]ethyl]-1-methyl-3-pyrrolidinol hydrochloride
纯度： ≥99% (HPLC)
生物活性 for R-96544 hydrochloride
R-96544 hydrochloride is a potent, selective 5-HT2 receptor antagonist; displays some selectivity for 5-HT2A receptors (Ki = 1.6 nM). IC50 values are 2.2, 310, 2400, 3700, > 5000 and > 5000 nM for 5-HT2, α1-adrenergic, D2 dopamine, 5-HT1, 5-HT3 and β-adrenergic receptors respectively. Inhibits 5-HT-induced platelet aggregation and pressor responses in vivo.
化合物库 for R-96544 hydrochloride
R-96544 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for R-96544 hydrochloride
| 分子量 | 391.94 |
| 公式 | C22H29NO3.HCl |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 167144-80-1 |
| PubChem ID | 10668210 |
| InChI Key | OUKRSTJUAQEATQ-GZJHNZOKSA-N |
| Smiles | Cl[H].COC1=CC=CC(CCC2=C(OCC[C@@H]3C[C@@H](O)CN3C)C=CC=C2)=C1 |
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 R-96544 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 39.19 | 100 | |
| DMSO | 39.19 | 100 |
制备储备液 for R-96544 hydrochloride
以下数据基于产品分子量 391.94。 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 | 2.55 mL | 12.76 mL | 25.51 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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产品说明书 for R-96544 hydrochloride
参考文献 for R-96544 hydrochloride
参考文献是支持产品生物活性的出版物。
Tanaka et al (2000) [2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding. Chem.Pharm.Bull. 48 1729 PMID: 11086903
Ogawa et al (2002) Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444. Eur.J.Pharmacol. 457 107 PMID: 12464356
Ogawa et al (2005) Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: additional evidence for possible involvement of 5-HT2A receptors in the development of expe Eur.J.Pharmacol. 521 156 PMID: 16183055
If you know of a relevant reference for R-96544 hydrochloride, please let us know.
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关键词: R-96544 hydrochloride, R-96544 hydrochloride supplier, Potent, selective, 5-HT2A, antagonists, serotonin, receptors, 5-HT2, antagonist, Receptors, 1742, Tocris Bioscience
3 篇 R-96544 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 R-96544 hydrochloride 的部分引用包括：
Xu et al (2012) Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome. J Pharmacol Exp Ther 7 e48741 PMID: 23119095
Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000
Chien and Su (2015) 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts. PLoS One 22 42 PMID: 26076928
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
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.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.