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Description: Selective α7 nAChR agonist
Chemical Name: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide
Purity: ≥98% (HPLC)
Biological Activity for PNU 282987
PNU 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).
Compound Libraries for PNU 282987
PNU 282987 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PNU 282987
| M. Wt | 264.75 |
| Formula | C14H17ClN2O |
| Storage | Store at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PNU 282987
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 26.48 | 100 | |
| DMSO | 26.48 | 100 |
Preparing Stock Solutions for PNU 282987
The following data is based on the product molecular weight 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.
| 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 |
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Product Datasheets for PNU 282987
References for PNU 282987
References are publications that support the biological activity of the product.
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, PNU 282987 supplier, Selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PNU282987, (a7), 2303, Tocris Bioscience
3 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
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.