PNU 282987( PNU-282987 | PNU 282987 )

Catalog No. M17898 CAS No. 123464-89-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PNU 282987
Note

Research use only, not for human use.
Brief Description

PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
Description

PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM).
In Vitro

PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM.PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM. PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM.
In Vivo

PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit.PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner. Animal Model:Rats Dosage:1, 3 mg/kg Administration:i.v.Result:Significantly reversed amphetamine-induced gating deficit.
Synonyms

PNU-282987 | PNU 282987
Pathway

Endocrinology/Hormones
Target

AChR
Recptor

α7 nAChR
Research Area

Neurological Disease
Indication

——

CAS Number

123464-89-1
Formula Weight

301.21
Molecular Formula

C14H18Cl2N2O
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 61 mg/mL 202.52 mM; H2O : 50 mg/mL 166.00 mM
SMILES

Cl.C1CN2CCC1[C@H](C2)NC(=O)c1ccc(cc1)Cl
Chemical Name

Benzamide, N-(3R)-1-azabicyclo(2.2.2)oct-3-yl-4-chloro-, hydrochloride (1:1)

1. Bodnar AL, et al. J Med Chem. 2005 Feb 24;48(4):905-8.

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