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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
Structure of PQ-10

SMILES

COC1=CC2=NC=NC(N3CC[C@H](C3)OC4=CN=C5C=CC=CC5=N4)=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

HIDE SMILES / InChI

Molecular Formula C22H21N5O3
Molecular Weight 403.4338
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

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

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
8.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
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
PQ-10 inhibited PDE10A in cell-free assay with IC50 8nM
Substance Class Chemical
Record UNII
63643I762J
Record Status Validated (UNII)
Record Version