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.

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CAS 番号 : 711085-63-1

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Other 在庫あり Forms of PNU-282987 free base:

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PNU-282987 free base 関連抗体

Top Publications Citing Use of Products

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) reduced Nlrp3 mRNA level in the oxygen-glucose deprivation/reperfusion (OGD/R) model performed in BV2 cells.

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) diminished the upregulation of NLRP3 expression induced by LPS + ATP in BV2 cells.

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) blocked conspicuous nucleus translocation by LPS + ATP stimulation in BV2 cells.

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) reduced the release of IL-1β in the conditioned medium collected from BV2 cells.

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) significantly ameliorated the apoptosis of PC12 cells induced by the LPS + ATP-containing conditioned medium.

    PNU-282987 free base purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Apr;72(4):879-892.  [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.

    5-HT Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    SH-SY5Y IC50
    >60 μM
    Compound: 2 PNU-282987
    Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
    Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
    		[PMID: 16821801]
    TE-671 IC50
    >60 μM
    Compound: 2 PNU-282987
    Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
    Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
    		[PMID: 16821801]
    体外実験

    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 関連抗体
    体内実験

    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.
    分子量

    264.75

    分子式

    C14H17ClN2O
    CAS 番号
    SMILES

    O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    Please store the product under the recommended conditions in the Certificate of Analysis.
    純度とドキュメンテーション
    参考文献
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    PNU-282987 free base Related Classifications

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    Keywords:

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

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    製品名:
    PNU-282987 free base
    製品番号:
    HY-12560
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