PQ-10

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 Search

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

HIDE SMILES / InChI

Description
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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Phosphodiesterase 10A 12 Target ID: CHEMBL4409 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24729456 \| https://www.ncbi.nlm.nih.gov/pubmed/17228859	Inhibitor 8297		8.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Psychotic disorder 26 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22951181 http://adisinsight.springer.com/drugs/800025212	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Fluorine-containing 6,7-dialkoxybiaryl-based inhibitors for phosphodiesterase 10 A: synthesis and in vitro evaluation of inhibitory potency, selectivity, and metabolism.	2014 Jul	24729456

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

Name

Type

Language

PQ-10

Common Name

English

QUINAZOLINE, 6,7-DIMETHOXY-4-((3R)-3-(2-QUINOXALINYLOXY)-1-PYRROLIDINYL)-

Systematic Name

English

Code System Code Type Description

CAS

927691-21-2