| Bioactivity | PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems[1]. |
| Target | IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA) |
| Invitro | PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM[1].PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM[1].PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM[1]. |
| In Vivo | PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit[1].PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner[1]. Animal Model: |
| Name | PNU-282987 |
| CAS | 123464-89-1 |
| Formula | C14H18Cl2N2O |
| Molar Mass | 301.21 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Alice L Bodnar, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem |
PNU-282987
CAS: 123464-89-1 F: C14H18Cl2N2O W: 301.21
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a
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