PNU-282987 free base
Based on 15 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.
For research use only. We do not sell to patients.
- CAS No.: 711085-63-1
- Formula: C14H17ClN2O
- Molecular Weight:264.75
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Storage:
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]
- 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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RT-PCR
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All 5-HT Receptor Isoforms
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Biological Activity
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. Further protocols information, click here.
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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Molecular Weight 264.75
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Formula C14H17ClN2O
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SMILES
O=C(N[C@H]1CN2CCC1CC2)C3=CC=C(Cl)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (15)
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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 -
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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Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PNU-282987 free base Related Classifications
HY-12560 Related Classifications
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