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).
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 264.75. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the products' biological activity.
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.
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Keywords: PNU 282987, supplier, Selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PNU282987, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
2 Citations for PNU 282987
Citations are publications that use Tocris products. Selected citations for PNU 282987 include:
Zhong et al (2013) Nicotine elicits prolonged calcium signaling along ventral hippocampal axons. Elife 8 e82719 PMID: 24349346
Wang et al (2012) Reducing amyloid-related Alzheimer's disease pathogenesis by a small molecule targeting filamin A. J Neurosci 32 9773 PMID: 22815492
Do you know of a great paper that uses PNU 282987 from Tocris? If so please let us know.
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