Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H22N2O3S2 |
| Molecular Weight | 390.52 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)S(=O)(=O)N[C@H]1CCOC[C@@H]1C2=CC=C(C=C2)C3=CC=C(S3)C#N
InChI
InChIKey=FFAGHPLLBXWCSF-MSOLQXFVSA-N
InChI=1S/C19H22N2O3S2/c1-13(2)26(22,23)21-18-9-10-24-12-17(18)14-3-5-15(6-4-14)19-8-7-16(11-20)25-19/h3-8,13,17-18,21H,9-10,12H2,1-2H3/t17-,18+/m1/s1
| Molecular Formula | C19H22N2O3S2 |
| Molecular Weight | 390.52 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/20347881
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/20347881
PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.Displacement studies using [3
H]PF-04725379 in rat cortical
tissue determined a Ki of 85 nM for PF-4778574. The AMPAR potentiator PF-4778574 was characterized in
a series of in vitro assays and acute-dose animal studies
evaluating AMPAR-mediated mechanism, safety, and nootropism.
Potentiator-induced animal effects were likely
purely AMPAR-dependent since PF-4778574 (10 uM) only
affected the dopamine transporter (IC50 of 910 nM) in a broad
human-based receptor/enzyme selectivity panel.
CNS Activity
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| American Chemical Society-239th national meeting--Investigating new therapeutic candidates: part 1. 21-25 March 2010, San Francisco, CA, USA. | 2010 May |
|
| Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574. | 2013 Oct |
Sample Use Guides
Mice: A single dose (0.178 mg/kg) of PF-4778574 in 5:5:90 (v/v/v) DMSO:Cremophor EL:deionized H2O (0.0178 mg/ml) was administered (10 ml/kg s.c.) to CD-1 or C57BL/6J mice.
Rats: Intravenous Dose. From jugular vein–cannulated Sprague-Dawley rats receiving a single bolus (1 ml/kg i.v.) of PF-4778574 (0.2 mg/kg) in 2:98 (v/v) DMSO:20% hydroxypropyl-b-cyclodextrin (0.2 mg/ml).
Dogs: 0.1 mg/kg PO
Route of Administration:
Other
PF-4778574
concentration-dependently increased S-AMPA–evoked responses
in HEK293 cells expressing human GluA2i or
GluA2o, mouse neuronal precursors, and rat primary neurons.
Depending on the cell type, PF-4778574 EC50 ranged
from 45 to 919 nM. PF-4778574 (10 uM) only
affected the dopamine transporter (IC50 of 910 nM) in a broad
human-based receptor/enzyme selectivity panel
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:53:31 GMT 2023
by
admin
on
Sat Dec 16 09:53:31 GMT 2023
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| Record UNII |
TI55D82Z4B
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| Record Status |
Validated (UNII)
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| Record Version |
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TARGET->POSITIVE ALLOSTERIC MODULATOR (PAM) |
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ACTIVE MOIETY |
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