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
| Molecular Formula | C14H17ClN2O |
| Molecular Weight | 264.751 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:53:32 GMT 2023
by
admin
on
Sat Dec 16 09:53:32 GMT 2023
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| Record UNII |
27M563MU5U
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| Record Status |
Validated (UNII)
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| Record Version |
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27M563MU5U
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9795278
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DTXSID701018122
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711085-63-1
Created by
admin on Sat Dec 16 09:53:32 GMT 2023 , Edited by admin on Sat Dec 16 09:53:32 GMT 2023
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TARGET -> AGONIST |
PNU-282,987: A SELECTIVE AND POTENT AGONIST, BUT MAY CAUSE LONG QT SYNDROME.
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ACTIVE MOIETY |
