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Submit ReviewPHA 543613 hydrochloride
说明： Potent and selective α7 nAChR agonist
化学名： N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for PHA 543613 hydrochloride
PHA 543613 hydrochloride is a potent α7 nAChR agonist that displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for PHA 543613 hydrochloride
PHA 543613 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 PHA 543613 hydrochloride
| 分子量 | 307.78 |
| 公式 | C15H17N3O2.HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1586767-92-1 |
| PubChem ID | 56972222 |
| InChI Key | YMTPSZUBRSEWNY-ZOWNYOTGSA-N |
| Smiles | O=C(C2=NC=C(OC=C3)C3=C2)N[C@@H]1C4CCN(CC4)C1.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 PHA 543613 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 30.78 | 100 | |
| DMSO | 7.69 | 25 |
制备储备液 for PHA 543613 hydrochloride
以下数据基于产品分子量 307.78。 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 | 3.25 mL | 16.25 mL | 32.49 mL |
| 5 mM | 0.65 mL | 3.25 mL | 6.5 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.25 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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产品说明书 for PHA 543613 hydrochloride
参考文献 for PHA 543613 hydrochloride
参考文献是支持产品生物活性的出版物。
Wishka et al (2006) Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia; synthesis and st J.Med.Chem. 49 4425 PMID: 16821801
Faghih et al (2008) Allosteric modulators of the α7 nicotinic acetylcholine receptor. J.Med.Chem. 51 701 PMID: 18198823
Acker et al (2008) Discovery of N-[3R,5R)-1-azabicyclo[3.2.1]ocy-3-yl]furo-[2,3-c]pyridine-5-carboxamide as an agonist of the α7 nicotinic acetylcholine receptor: in vitro and in vivo activity. Bioorg.Med.Chem.Letts. 18 3611 PMID: 1849016
If you know of a relevant reference for PHA 543613 hydrochloride, please let us know.
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关键词: PHA 543613 hydrochloride, PHA 543613 hydrochloride supplier, Potent, selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PHA543613, hydrochloride, Pfizer, 478149-53-0, (a7), 3092, Tocris Bioscience
7 篇 PHA 543613 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PHA 543613 hydrochloride 的部分引用包括：
Foucault-Fruchard (2017) Neuroprotective effect of the alpha 7 nicotinic receptor agonist PHA 543613 in an in vivo excitotoxic adult rat model. Neuroscience 356 52 PMID: 28527955
Bali et al (2015) Differential effects of α7 nicotinic receptor agonist PHA-543613 on spatial memory performance of rats in two distinct pharmacological dementia models. Behav Brain Res 278 404 PMID: 25447295
Wang et al (2012) Electroacupuncture pretreatment attenuates cerebral ischemic injury through α7 nicotinic acetylcholine receptor-mediated inhibition of high-mobility group box 1 release in rats. J Neuroinflammation 9 24 PMID: 22277256
Bali et al (2019) Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep 9 9324 PMID: 31249369
Sérriàre et al (2015) Assessment of the Protection of DArgic Neurons by an α7 Nicotinic Receptor Agonist, PHA 543613 Using [(18)F]LBT-999 in a Parkinson's Disease Rat Model. Cell Death Differ 2 61 PMID: 26389120
Macpherson et al (2014) The α7 nicotinic receptor agonist PHA-543613 hydrochloride inhibits Porphyromonas gingivalis-induced expression of interleukin-8 by oral keratinocytes. Front Med (Lausanne) 63 557 PMID: 24609617
Bali et al (2019) Cognitive enhancer effects of low Mem. doses are facilitated by an alpha7 nicotinic acetylcholine receptor agonist in scopolamine-induced amnesia in rats. Front Pharmacol 10 73 PMID: 30804787
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Cognitive enhancer effect of PHA 543613 in rat behavioral tests.
By
Zsolt Bali on 02/14/2018
分析类型： In Vivo
种属： Rat
We used PHA 543613 in behavioral pharmacology experiments and tested its cognitive enhancer effect. PHA 543613 was found effective in different behavioral paradigms, and in different models of cognitive impairment. For instance, PHA 543613 dose-dependently reversed scopolamine induced transient amnesia in the spontaneous alternation (t-maze) task of rats.
Sometimes we experienced poor solubility in physiological saline. Slight warming and ultrasonics might help.
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。
Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.