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Submit ReviewPNU 282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). Found to be inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).
PNU 282987 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 264.75 |
公式 | C14H17ClN2O |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 711085-63-1 |
PubChem ID | 9795278 |
InChI Key | WECKJONDRAUFDD-ZDUSSCGKSA-N |
Smiles | O=C(C2=CC=C(Cl)C=C2)N[C@@H]1C3CCN(CC3)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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
1eq. HCl | 26.48 | 100 | |
DMSO | 26.48 | 100 |
以下数据基于产品分子量 264.75。 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 | 3.78 mL | 18.89 mL | 37.77 mL |
5 mM | 0.76 mL | 3.78 mL | 7.55 mL |
10 mM | 0.38 mL | 1.89 mL | 3.78 mL |
50 mM | 0.08 mL | 0.38 mL | 0.76 mL |
参考文献是支持产品生物活性的出版物。
Bodnar et al (2005) Discovery and structure-activity relationship of quinuclidine benzamides as agonists of α7 nicotinic acetylcholine receptors. J.Med.Chem. 48 905 PMID: 15715459
Hajós et al (2005) The selective α7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride] enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthe J.Pharmacol.Exp.Ther. 312 1213 PMID: 15523001
If you know of a relevant reference for PNU 282987, please let us know.
关键词: PNU 282987, PNU 282987 supplier, Selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PNU282987, (a7), 2303, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PNU 282987 的部分引用包括:
Zhong et al (2013) Nicotine elicits prolonged calcium signaling along ventral hippocampal axons. Elife 8 e82719 PMID: 24349346
Pandya and Yakel (2013) Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT?a receptor antagonist. Neuropharmacology 70 35 PMID: 23321689
Wang et al (2012) Reducing amyloid-related Alzheimer's disease pathogenesis by a small molecule targeting filamin A. J Neurosci 32 9773 PMID: 22815492
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