PNU 282987

Catalog No.S5930

PNU 282987 Chemical Structure

Molecular Weight(MW): 301.21

PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.

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Biological Activity

Description PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor.
Targets
rat α7 nAChR [1]
()
5-HT3 receptor [1]
()
26 nM(Ki) 930 nM(Ki)
In vitro

PNU282987 shows high affinity for the rat α7 nAChR (Ki = 26 nM) and activity at the α7-5-HT3 chimera (EC50 = 128 nM) and showed a negligible block of α1β1γδ and α3β4 nAChRs (≥60 μM). It is inactive at all tested monoamine, muscarine, glutamate, and GABA receptors at 1 μM concentration, except 5-HT3 receptors (Ki = 930 nM). PNU-282987 enhances GABAergic synaptic activity in the hippocampus in vitro[1].

In vivo PNU-282987 reverses amphetamine-induced gating deficit in amphetamine-treated rats[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Sprague-Dawley rats
  • Formulation: PBS
  • Dosages: 1 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (152.71 mM)
Water 11 mg/mL (36.51 mM)
Ethanol 4 mg/mL (13.27 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 301.21
Formula

C14H18Cl2N2O

CAS No. 123464-89-1
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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AChR Signaling Pathway Map

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