Biological Activity
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
PNU 282987 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 264.75 |
| Formula | C14H17ClN2O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 123464-89-1 |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 26.48 | 100 | |
| DMSO | 26.48 | 100 |
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 |
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References
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
Keywords: PNU 282987, supplier, Selective, α7, alpha7, a7, nAChR, agonists, Nicotinic, Receptors, Acetylcholine, PNU282987, Nicotinic, (a7), Receptors, Nicotinic, (a7), Receptors, Tocris Bioscience
