Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C14H17ClN2O |
| Molecular Weight | 264.751 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C(C=C1)C(=O)N[C@H]2CN3CCC2CC3
InChI
InChIKey=WECKJONDRAUFDD-ZDUSSCGKSA-N
InChI=1S/C14H17ClN2O/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17/h1-4,10,13H,5-9H2,(H,16,18)/t13-/m0/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20630711 | https://www.ncbi.nlm.nih.gov/pubmed/15523001Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27729414
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20630711 | https://www.ncbi.nlm.nih.gov/pubmed/15523001
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27729414
PNU-282987 is a potent and selective a7 nAChR agonist. This compound showed high affinity for the rat a7 nAChR (Ki = 26 nM) and activity at the a7–5-HT3 chimera (EC50 = 128 nM). In addition, PNU-282987 was found to be inactive at all tested monoamine, muscarine, glutamate, and GABA receptors at 1 uM concentration, except 5-HT3 receptors (Ki = 930 nM). The highly selective and potent a7 nAChR agonist PNU-282987 enhances GABAergic synaptic activity in the hippocampus in vitro, and reverses amphetamine induced auditory gating deficit in anesthetized rats. In addition, PNU-282987 improves the inherent gating deficit observed in a subset of rats and enhances amphetamine induced hippocampal activity. These results support the concept that a7 nAChR agonists represent a novel, potential pharmacotherapy in treatment of schizophrenia. It also has being shown that acute lung injury is reduced by PNU-282987 through changes in the macrophage profile.
CNS Activity
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The selective alpha7 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. | 2005 Mar |
|
| Alpha7 nicotinic acetylcholine receptor activation ameliorates scopolamine-induced behavioural changes in a modified continuous Y-maze task in mice. | 2009 Jan 5 |
|
| Human platelets express functional alpha7-nicotinic acetylcholine receptors. | 2011 Apr |
|
| Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation. | 2011 Sep |
|
| Interaction of bispyridinium compounds with the orthosteric binding site of human α7 and Torpedo californica nicotinic acetylcholine receptors (nAChRs). | 2011 Sep 25 |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Can also be used i.p. (0.3mg/kg and 1.0mg/kg) https://www.ncbi.nlm.nih.gov/pubmed/24833065
or s.c. (10mg/kg)
https://www.ncbi.nlm.nih.gov/pubmed/20630711
Rats: eye drops of PNU-282987 resulted in neuroprotection against etinal ganglion cells (RGCs) loss in a dose-dependent manner using concentrations between 100 uM and 2 mM PNU-282987
Route of Administration:
Topical
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9795278
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DTXSID701018122
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711085-63-1
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ACTIVE MOIETY
