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Submit ReviewMDL 100907
说明： Potent and selective 5-HT2A antagonist
别名： Volinanserin
化学名： (R)-(+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperinemethanol
纯度： ≥98% (HPLC)
生物活性 for MDL 100907
MDL 100907 is a potent and selective 5-HT2A receptor antagonist (Ki = 0.36 nM, IC50 = 3.3-5.1 nM). MDL 100907 exhibits > 80-fold selectivity for 5-HT2A receptors over other serotonergic receptor subtypes. MDL 100907 is neuroprotective; protects cultured dopaminergic neurons from MPP+ induced toxicity. Antipsychotic agent in vivo.
技术数据 for MDL 100907
| 分子量 | 373.46 |
| 公式 | C22H28FNO3 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 139290-65-6 |
| PubChem ID | 5311271 |
| InChI Key | HXTGXYRHXAGCFP-OAQYLSRUSA-N |
| Smiles | FC(C=C3)=CC=C3CCN(CC2)CCC2[C@@H](O)C1=C(OC)C(OC)=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 100907
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. HCl | 18.67 | 50 | |
| DMSO | 37.35 | 100 |
制备储备液 for MDL 100907
以下数据基于产品分子量 373.46。 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 | 2.68 mL | 13.39 mL | 26.78 mL |
| 5 mM | 0.54 mL | 2.68 mL | 5.36 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.68 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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产品说明书 for MDL 100907
参考文献 for MDL 100907
参考文献是支持产品生物活性的出版物。
Kehne et al (1996) Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile. J.Pharmacol. 277 968 PMID: 8627580
Sorensen et al (1993) Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies. J.Pharmacol.Exp.Ther. 266 684 PMID: 8102646
Ardayfio et al (2008) The 5-hydroxytryptamine2A receptor antagonist R-(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant dr J.Pharmacol.Exp.Ther. 327 891 PMID: 18772320
If you know of a relevant reference for MDL 100907, please let us know.
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关键词: MDL 100907, MDL 100907 supplier, MDL100907, potent, selective, 5-HT2A, receptors, antagonists, 5HT2A, antipsychotic, dopaminergic, neuroprotective, neuroprotection, volinanserin, M100907, Volinanserin, Receptors, 4173, Tocris Bioscience
11 篇 MDL 100907 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MDL 100907 的部分引用包括：
Grønli et al (2016) Sleep Homeostatic and Waking Behavioral Phenotypes in Egr3-Deficient Mice Associated with Serotonin Receptor 5-HT2 Deficits. Sleep 39 2189 PMID: 28057087
Daftary et al (2012) Essential role of brain-derived neurotrophic factor in the regulation of serotonin transmission in the basolateral amygdala. Neuroscience 224 125 PMID: 22917617
Athilingam et al (2017) Serotonin enhances excitability and gamma frequency temporal integration in mouse prefrontal fast-spiking interneurons. Elife 6 PMID: 29206101
Kara R et al (2022) Targeting 5-HT2A receptors and Kv7 channels in PFC to attenuate chronic neuropathic pain in rats using a spared nerve injury model. Neurosci Lett 789 136864 PMID: 36063980
Alharris et al (2019) Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget 10 45 PMID: 30713602
Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217
Bocchio et al (2015) Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala. Neuropsychopharmacology 40 3015 PMID: 26052039
Zhou et al (2019) A neural circuit for comorbid depressive symptoms in chronic pain. Nat Neurosci 22 1649 PMID: 31451801
Andrew et al (2019) A Discrete Dorsal Raphe to Basal Amygdala 5-HT Circuit Calibrates Aversive Memory. Neuron 103 489-505.e7 PMID: 31204082
Rui et al (2021) Dorsal raphe nucleus to anterior cingulate cortex 5-HTergic neural circuit modulates consolation and sociability. Elife 10 PMID: 34080539
Yuede et al (2021) Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease. J.Neurochem. 156 658 PMID: 33278025
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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.