2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. PNU-282987 free base

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.

For research use only. We do not sell to patients.

PNU-282987 free base Chemical Structure

PNU-282987 free base Chemical Structure

CAS No. : 711085-63-1

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PNU-282987 free base Related Antibodies

Top Publications Citing Use of Products

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Mar 13.  [Abstract]

    PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.

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    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[1].

    IC50 & Target

    5-HT3 Receptor

     

    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[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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PNU-282987 free base Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Rats[1]
    Dosage: 1, 3 mg/kg
    Administration: i.v.
    Result: Significantly reversed amphetamine-induced gating deficit.
    Molecular Weight

    264.75

    Formula

    C14H17ClN2O
    CAS No.
    SMILES

    O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    PNU-282987 free base Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PNU-282987711085-63-1PNU282987PNU 282987nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptornicotinic acetylcholine receptors (nAChRs)5-HT3nervous systemsα7Inhibitorinhibitorinhibit

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