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Submit ReviewMDL 11,939
说明： 5-HT2A antagonist
化学名： α-Phenyl-1-(2-phenylethyl)-4-piperidinemethanol
纯度： ≥99% (HPLC)
生物活性 for MDL 11,939
MDL 11,939 is an orally active 5-HT2A receptor antagonist; displays selectivity for 5-HT2A receptors over 5-HT2C receptors (Ki values are 0.54, 2.5, 81.6 and ~10,000 nM at rabbit 5-HT2A, human 5-HT2A, rabbit 5-HT2C and human 5-HT2C receptors respectively).
技术数据 for MDL 11,939
| 分子量 | 295.42 |
| 公式 | C20H25NO |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 107703-78-6 |
| PubChem ID | 71781 |
| InChI Key | AXNGJCOYCMDPQG-UHFFFAOYSA-N |
| Smiles | OC(C1CCN(CCC2=CC=CC=C2)CC1)C1=CC=CC=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 MDL 11,939
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 14.77 | 50 | |
| DMSO | 14.77 | 50 |
制备储备液 for MDL 11,939
以下数据基于产品分子量 295.42。 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 | 6.77 mL | 33.85 mL | 67.7 mL |
| 2.5 mM | 1.35 mL | 6.77 mL | 13.54 mL |
| 5 mM | 0.68 mL | 3.39 mL | 6.77 mL |
| 25 mM | 0.14 mL | 0.68 mL | 1.35 mL |
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产品说明书 for MDL 11,939
参考文献 for MDL 11,939
参考文献是支持产品生物活性的出版物。
Aloyo and Harvey (2000) Antagonist binding at 5-HT2A and 5-HT2C receptors in the rabbit: high correlation with the profile for the human receptors. Eur.J.Pharmacol. 406 163 PMID: 11020478
Dudley et al (1988) Pharmacological effects of MDL 11,939: a selective, centrally acting antagonist of 5-HT2 receptors. Drug Dev.Res. 13 29
Jensen et al (2013) Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-dazepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive J.Med.Chem. 56 1211 PMID: 23301527
If you know of a relevant reference for MDL 11,939, please let us know.
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关键词: MDL 11,939, MDL 11,939 supplier, 5-HT2A, antagonist, Serotonin, Receptors, MDL11939, 0870, Tocris Bioscience
8 篇 MDL 11,939 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MDL 11,939 的部分引用包括：
Nagata et al (2019) Blockade of multiple monoamines receptors reduce insulin secretion from pancreatic β-cells. Sci Rep 9 16438 PMID: 31712714
Williams et al (2012) Reduced levels of serotonin 2A receptors underlie resistance of Egr3-deficient mice to locomotor suppression by cloz. Neuropsychopharmacology 37 2285 PMID: 22692564
Halberstadt and Geyer (2010) LSD but not lisuride disrupts prepulse inhibition in rats by activating the 5-HT(2A) receptor. Psychopharmacology (Berl) 208 179 PMID: 19937319
Goda et al (2013) Serotonergic hallucinogens differentially modify gamma and high frequency oscillations in the rat nucleus accumbens. Psychopharmacology (Berl) 228 271 PMID: 23525524
Ptak et al (2009) Raphé neurons stimulate respiratory circuit activity by multiple mechanisms via endogenously released serotonin and substance P. Biomol Ther (Seoul) 29 3720 PMID: 19321769
Corcoran et al (2014) Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice. J Neurosci 34 51 PMID: 24381267
Yu and Yamaguchi (2009) 5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations. J Neurophysiol 102 752 PMID: 19474172
Hodges et al (2009) Transgenic mice lacking serotonin neurons have severe apnea and high mortality during development. J Neurosci 29 10341 PMID: 19692608
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MDL 11,939 的评论
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we used it for in vivo infusions.
By
noelia weisstaub on 01/04/2018
分析类型： In Vivo
种属： Rat
We used MDL for in vivo infusion at different regions of the brain. It works very well. It is very stable and easy to dissolve and not sticky which make it easy to infuse.
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.
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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.
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