PNU-282987 free base

SKU: orb2900875

Description

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.

Key Properties

• CAS Number: 711085-63-1
• MW: 264.75
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₇ClN₂O
• SMILES: Clc1ccc(cc1)C(=O)N[C@H]1CN2CCC1CC2
• Target: AChR

Bioactivity

• In Vivo:
  PNU-282987 (free base) (Compound C7) (i. v. ; 1, 3 mg/kg) leads to a reversal of the gating deficit. PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner. Animal model: Rats. Dosage: 1, 3 mg/kg. Administration: i. v. Result: Significantly reversed amphetamine-induced gating deficit.
• In Vitro:
  PNU-282987 (free base) (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM. PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM. PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

AChR