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Submit ReviewAF-DX 116
说明： Selective M2 antagonist
别名： Otenzepad
化学名： 11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
纯度： ≥98% (HPLC)
生物活性 for AF-DX 116
AF-DX 116 is a selective M2 muscarinic receptor antagonist. Ki values are 64, 417, 786, 211 and 5130 nM for human recombinant M2, M1, M3, M4 and M5 muscarinic receptors, respectively.
许可信息
Sold with the permission of Boehringer Ingelheim GmbH
技术数据 for AF-DX 116
| 分子量 | 421.54 |
| 公式 | C24H31N5O2 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 102394-31-0 |
| PubChem ID | 107867 |
| InChI Key | UBRKDAVQCKZSPO-UHFFFAOYSA-N |
| Smiles | CCN(CC)CC1CCCCN1CC(=O)N1C2=C(C=CC=C2)C(=O)NC2=CC=CN=C12 |
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 AF-DX 116
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 10.54 | 25 温和加热 |
制备储备液 for AF-DX 116
以下数据基于产品分子量 421.54。 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 |
|---|---|---|---|
| 0.25 mM | 9.49 mL | 47.45 mL | 94.89 mL |
| 1.25 mM | 1.9 mL | 9.49 mL | 18.98 mL |
| 2.5 mM | 0.95 mL | 4.74 mL | 9.49 mL |
| 12.5 mM | 0.19 mL | 0.95 mL | 1.9 mL |
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产品说明书 for AF-DX 116
参考文献 for AF-DX 116
参考文献是支持产品生物活性的出版物。
Billard et al (1995) Identification of the primary muscarinic autoreceptor subtype in rat striatum as M2 through a correlation of in vivo microdialysis and in vitro receptor binding data. J.Pharmacol.Exp.Ther. 273 273 PMID: 7714776
Eglen et al (1996) Muscarinic receptor subtypes and smooth muscle function. Pharmacol.Rev. 48 531 PMID: 8981565
Hammer et al (1986) Binding profile of a novel cardioselective muscarinic receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat. Life Sci. 38 1653 PMID: 3754610
Mansfield et al (2005) Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing. Br.J.Pharmacol. 114 1089 PMID: 15723094
If you know of a relevant reference for AF-DX 116, please let us know.
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关键词: AF-DX 116, AF-DX 116 supplier, Selective, M2, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, AFDX116, Otenzepad, 1105, Tocris Bioscience
9 篇 AF-DX 116 的引用文献
引用文献是使用了 Tocris 产品的出版物。 AF-DX 116 的部分引用包括：
Gigout et al (2012) Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex. BMC Neurosci 13 42 PMID: 22540185
Bragança et al (2016) Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol 7 45 PMID: 27014060
Bell et al (2015) Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation. J Neurosci 9 115 PMID: 25918499
Placeres-Uray et al (2014) M2 Muscarinic acetylcholine receptor modulates rat airway smooth muscle cell proliferation. World Allergy Organ J 6 22 PMID: 24377382
Kitazawa et al (2009) M3 muscarinic receptors mediate positive inotropic responses in mouse atria: a study with muscarinic receptor knockout mice. Front Cell Neurosci 330 487 PMID: 19429792
Ross et al (2019) Olfactory Bulb Muscarinic Acetylcholine Type 1 Receptors Are Required for Acquisition of Olfactory Fear Learning. Front Behav Neurosci 13 164 PMID: 31379534
Clancy et al (2007) Coregulation of natively expressed pertussis toxin-sensitive muscarinic receptors with G-protein-activated potassium channels. Proc Natl Acad Sci U S A 27 6388 PMID: 17567799
Solanki et al (2007) Cholinergic innervation of the guinea-pig isolated vas deferens. Naunyn Schmiedebergs Arch Pharmacol 376 265 PMID: 17992517
Makara et al (2007) Involvement of nitric oxide in depolarization-induced suppression of inhibition in hippocampal pyramidal cells during activation of cholinergic receptors. J Neurosci 27 10211 PMID: 17881527
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