Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H21N5O3 |
Molecular Weight | 403.4338 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC2=NC=NC(N3CC[C@H](C3)OC4=NC5=CC=CC=C5N=C4)=C2C=C1OC
InChI
InChIKey=UBIIFKJMNRPNMT-CQSZACIVSA-N
InChI=1S/C22H21N5O3/c1-28-19-9-15-18(10-20(19)29-2)24-13-25-22(15)27-8-7-14(12-27)30-21-11-23-16-5-3-4-6-17(16)26-21/h3-6,9-11,13-14H,7-8,12H2,1-2H3/t14-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/24729456Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800025212
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24729456
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800025212
PQ-10 belongs to the same class as the PDE10 inhibitor papaverine, but IC50 literature suggests that is about 5 times more potent then papaverine, yet still about 10 times less potent the known PDE10 inhibitors TP- 10 and MP-10. Preclinical development is ongoing in USA for the treatment of psychotic disorders.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22951181
Curator's Comment: PQ-10 is clearly brain penetrant and CNS active
Originator
Sources: http://adisinsight.springer.com/drugs/800025212
Curator's Comment: # Pfizer
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22951181
Rats: PQ-10 was tested at doses of 0.1-1mg/kg (p.o.) in the scopolamine model and 0.3-3mg/kg in the MK-801 model.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24729456
PQ-10 inhibited PDE10A in cell-free assay with IC50 8nM
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927691-21-2
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11955614
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DTXSID10470891
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63643I762J
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DB08391
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ACTIVE MOIETY