PNU-282987 free base
Based on 16 publication(s) in Google Scholar
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 No.: 711085-63-1
- Formule: C14H17ClN2O
- Masse moléculaire:264.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) PNU-282987 free base
More- Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365. [Abstract]
- Cell Death Discov. 2022 Mar 30;8(1):141. [Abstract]
- Int J Biol Macromol. 2026 Mar:349:150933. [Abstract]
- Mol Med. 2022 Sep 4;28(1):104. [Abstract]
- Free Radic Biol Med. 2025 Apr 3:S0891-5849(25)00207-2. [Abstract]
- PLoS Biol. 2026 Aug 3;24(8):e3003923.
- Biochem Pharmacol. 2025 Aug 29;242(Pt 1):117290. [Abstract]
- Inflamm Res. 2023 Apr;72(4):879-892. [Abstract]
- Respir Res. 2026 Apr 1;27(1):206. [Abstract]
- Eur J Pharmacol. 2021 Jun 5:900:174067. [Abstract]
- Int Immunopharmacol. 2025 Feb 6:147:113941. [Abstract]
- Cell Signal. 2024 Sep:121:111275. [Abstract]
- J Pain Res. 2021 Feb 15:14:441-452. [Abstract]
- J Cell Biochem. 2024 Sep;125(9):e30630. [Abstract]
- Biomed Res. 2017; Special Issue: ISSN 0970.
- Biomed Res-India. 2019 Apr.
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Voir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
Description
IC50 & Target
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5-HT3 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
>60 μM
Compound: 2 PNU-282987
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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
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[PMID: 16821801] |
| TE-671 | IC50 |
>60 μM
Compound: 2 PNU-282987
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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
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[PMID: 16821801] |
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.
In Vivo
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.
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Animal Model:Rats[1]
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Dosage:1, 3 mg/kg
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Administration:i.v.
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Result:Significantly reversed amphetamine-induced gating deficit.
Chemical Information
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CAS No. 711085-63-1
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Masse moléculaire 264.75
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Formule C14H17ClN2O
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SMILES
O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via α7nAchR-dependent inactivation of microglial NLRP3 inflammasome. [Abstract]2024 Jul;45(7):1349-1365. PMID: 38504011
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.
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Cell Death Discov
Alpha-7 nicotinic acetylcholine receptor agonist alleviates psoriasis-like inflammation through inhibition of the STAT3 and NF-κB signaling pathway. [Abstract]2022 Mar 30;8(1):141. PMID: 35351863 -
Int J Biol Macromol
α-Conotoxin LvID, an antagonist of α7 nicotinic acetylcholine receptor, mitigates Alzheimer-associated phenotypes by inhibiting Aβ deposition and reactive astrogliosis. [Abstract]2026 Mar:349:150933. PMID: 41692211 -
Mol Med
Protective effect of α7 nicotinic acetylcholine receptor activation on experimental colitis and its mechanism. [Abstract]2022 Sep 4;28(1):104. PMID: 36058917 -
Free Radic Biol Med
Ultrasound-responsive taurine lipid nanoparticles attenuate oxidative stress and promote macrophage polarization for diabetic wound healing. [Abstract]2025 Apr 3:S0891-5849(25)00207-2. PMID: 40187503 -
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Biochem Pharmacol
α7nAChR activation promotes the generation of Treg cells by enhancing the dephosphorylation of Foxo1 via the IP3R/Ca2+/calcineurin pathway. [Abstract]2025 Aug 29;242(Pt 1):117290. PMID: 40886855 -
Inflamm Res
Activating α7nAChR helps post-myocardial infarction healing by regulating macrophage polarization via the STAT3 signaling pathway. [Abstract]2023 Apr;72(4):879-892. PMID: 36912917
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.
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Respir Res
Activation of α7nAChR prevents maladaptive right ventricular remodeling via inhibiting the recruitment of CCR2+ macrophages in experimental pulmonary arterial hypertension. [Abstract]2026 Apr 1;27(1):206. PMID: 41923075 -
Eur J Pharmacol
Activation of alpha7 nicotinic acetylcholine receptor protects bovine endometrial tissue against LPS-induced inflammatory injury via JAK2/STAT3 pathway and COX-2 derived prostaglandin E2. [Abstract]2021 Jun 5:900:174067. PMID: 33811838 -
Int Immunopharmacol
Electroacupuncture promotes resolution of inflammation by modulating SPMs via vagus nerve activation in LPS-induced ALI. [Abstract]2025 Feb 6:147:113941. PMID: 39746272 -
Cell Signal
2024 Sep:121:111275. PMID: 38942343 -
J Pain Res
The Spinal α7-Nicotinic Acetylcholine Receptor Contributes to the Maintenance of Cancer-Induced Bone Pain. [Abstract]2021 Feb 15:14:441-452. PMID: 33623426 -
J Cell Biochem
Activation of α7 Nicotinic Acetylcholine Receptor Improves Muscle Endurance by Upregulating Orosomucoid Expression and Glycogen Content in Mice. [Abstract]2024 Sep;125(9):e30630. PMID: 39014907 -
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Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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