PNU-282987 ( ——— )

Catalog No. M38006 CAS No. 123464-89-1

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.

Purity : >98% (HPLC)

COA

Datasheet

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Biological Information

Product Name

PNU-282987
Note

Research use only, not for human use.
Brief Description

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.
Description

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 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

———
Pathway

Others
Target

Other Targets
Recptor

5-HT Receptor
Research Area

———
Indication

———

Chemical Information

CAS Number

123464-89-1
Formula Weight

301.21
Molecular Formula

C14H18Cl2N2O
Purity

>98% (HPLC)
Solubility

?H2O : 50 mg/mL (166.00 mM; ultraphonic) DMSO : 10 mg/mL (33.20 mM; ultraphonic (<60°C)
SMILES

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

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Alice L Bodnar, et al. Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem?

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