PNU 282987

SKU: orb1222797

Description

PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).

Key Properties

• CAS Number: 123464-89-1
• MW: 301.21
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₈Cl₂N₂O
• SMILES: Cl.C1CN2CCC1[C@H](C2)NC(=O)c1ccc(cc1)Cl
• Target: AChR
• Solubility: DMSO : ≥ 61 mg/mL 202.52 mM; H2O : 50 mg/mL 166.00 mM

Bioactivity

• In Vivo:
  PNU-282987 (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 (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

Alternative Names

PNU-282987 | PNU 282987

Quick Database Links

Gene Symbol

AChR