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PNU-282987 | nAChR agonist

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Price:
$79.00
SKU:
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.

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