Loading... Please wait...

Our Newsletter


PNU-282987 | nAChR agonist

  • PNU-282987.jpg
  • PNU-282987 | nAChR agonist, 400x400px, png
Price:
$79.00
Catalog #:
C7282-5
Quantity:


Product Description

PNU-282987 is an α7 nAChR agonist with an EC50 of 154 nM against the a7-5HT3 chimera. Up to concentrations of 100 uM, PNU-282987 displayed no agonist activity and negligible antagonistic activity (60 uM) toward the neuromuscular junction form of the receptor and the ganglionic nAChR (a3b4). PNU-282987 is a functional antagonist of the 5-HT3 receptor at an IC50 of 4.5 uM. (1)

Cotreatment of PC12 cells with nAChR modulator PNU120596 and PNU-282987 significantly induces ERK1/2 phosphorylation. (2) In a chloral hydrate-anesthetized rat model, PNU-282987 was shown to restore amphetamine-induced sensory gating deficit and may have implications in the treatment of schizophrenia. (3)


Technical information:

Chemical Formula:   C14H17ClN2O
CAS #:   123464-89-1
Molecular Weight:   264.75
Purity:   > 98%
Appearance:   white
Chemical Name:   N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   PNU-282987, PNU 282987, PNU282987

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Bodnar et al., Discovery and Structure-Activity Relationship of Quinuclidine Benzamides as Agonists of a7 Nicotinic Acetylcholine Receptors. J. Med. Chem. 2005, 48, 905-908. Pubmed ID: 15715459
2. El Kouhen et al., Pharmacology of a7 nicotinic acetylcholine receptor mediated extracellular signal-regulated kinase signalling in PC12 cells. Br. J. Pharmacology, 2009, 156, 638-648. Pubmed ID: 19226255
3. Hajos et al., The Selective a7 Nicotinic Acetylcholine Receptor Agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide Hydrochloride] Enhances GABAergic Synaptic Activity in Brain Slices and Restores Auditory Gating Deficits in Anesthetized Rats. J. Pharmcol. Exp. Ther. 2005, 312(3), 1213-1222. Pubmed ID: 15523001

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the PNU-282987 | nAChR agonist to your wish list.

You Recently Viewed...