PNU-282987 free base

CAS No. 711085-63-1

PNU-282987 free base( —— )

Catalog No. M35418 CAS No. 711085-63-1

PNU-282987 (free base) is a potent agonist of α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 154 nM and a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PNU-282987 free base
  • Note
    Research use only, not for human use.
  • Brief Description
    PNU-282987 (free base) is a potent agonist of α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 154 nM and a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM.
  • 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.
  • 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 4541nM.
  • 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.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    AChR
  • Recptor
    AChR | 5-HT Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    711085-63-1
  • Formula Weight
    264.75
  • Molecular Formula
    C14H17ClN2O
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Clc1ccc(cc1)C(=O)N[C@H]1CN2CCC1CC2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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. ?
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