Bioactivity | PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems[1]. |
Invitro | PNU-282987 (free base) (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 (free base) (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 free base |
CAS | 711085-63-1 |
Formula | C14H17ClN2O |
Molar Mass | 264.75 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Bodnar AL, Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem. 2005 Feb 24;48(4):905-8. |