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PNU-282987

CAS No. 123464-89-1

PNU-282987 ( ——— )

Catalog No. M38006 CAS No. 123464-89-1

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.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PNU-282987
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM.
  • 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 4541nM.
  • 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.
  • Synonyms
    ———
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    5-HT Receptor
  • Research Area
    ———
  • Indication
    ———

Chemical Information

  • CAS Number
    123464-89-1
  • Formula Weight
    301.21
  • Molecular Formula
    C14H18Cl2N2O
  • Purity
    >98% (HPLC)
  • Solubility
    ?H2O : 50 mg/mL (166.00 mM; ultraphonic) DMSO : 10 mg/mL (33.20 mM; ultraphonic (<60°C)
  • SMILES
    Cl.C1CN2CCC1[C@H](C2)NC(=O)c1ccc(cc1)Cl
  • Chemical Name
    ——

Shipping & Storage Information

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

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?
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