Home Metabolism AChR agonist PNU 282987 HCl For research use only.

PNU 282987 HCl

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

PNU 282987 HCl Chemical Structure

PNU 282987 HCl Chemical Structure

CAS No. 123464-89-1

Purity & Quality Control

Batch: S593001 DMSO]46 mg/mL]false]Water]11 mg/mL]false]Ethanol]4 mg/mL]false Purity: 99.82%
99.82

PNU 282987 HCl Related Products

Signaling Pathway

AChR Signaling Pathways

AChR Signaling Pathway

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
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
In vivo PNU-282987 reverses amphetamine-induced gating deficit in amphetamine-treated rats[1].
Animal Research Animal Models Sprague-Dawley rats
Dosages 1 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 301.21 Formula

C14H18Cl2N2O
CAS No. 123464-89-1 SDF --
Smiles C1CN2CCC1C(C2)NC(=O)C3=CC=C(C=C3)Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 46 mg/mL ( (152.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 11 mg/mL

Ethanol : 4 mg/mL


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In vivo
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