| Identification | Back Directory | [Name]
(R)-6,7-dimethoxy-4-(3-(quinoxalin-2-yloxy)pyrrolidin-1-yl)quinazoline | [CAS]
927691-21-2 | [Synonyms]
A844337
A-844337
A 844337
6,7-dimethoxy-4-[3-(2-quinoxalinyloxy)-1-pyrrolidinyl]quinazoline
6,7-dimethoxy-4-[(3R)-3-quinoxalin-2-yloxypyrrolidin-1-yl]quinazoline
6,7-Dimethoxy-4-[(3R)-3-(2-quinoxalinyloxy)-1-pyrrolidinyl]quinazoline
(R)-6,7-dimethoxy-4-(3-(quinoxalin-2-yloxy)pyrrolidin-1-yl)quinazoline
Quinazoline, 6,7-dimethoxy-4-[(3R)-3-(2-quinoxalinyloxy)-1-pyrrolidinyl]-
inhibit,Phosphodiesterase (PDE),PQ-10,Phosphodiesterase 10A,translational biomarker,schizophrenia,PQ10,PDE10A,glucose metabolism,Inhibitor,psychiatric disorders | [Molecular Formula]
C22H21N5O3 | [MDL Number]
MFCD12828216 | [MOL File]
927691-21-2.mol | [Molecular Weight]
403.43 |
| Hazard Information | Back Directory | [Description]
PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; Ki = 4 nM). It has >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro. Subcutaneous injection of PQ-10 (32 mg/kg) leads to increases in striatal cGMP and phosphorylation of cAMP response element binding protein (CREB) in murine striatum, known markers of in vivo PDE10 inhibition. PQ-10 at a dose of 0.3 mg/kg, p.o., reduces scopolamine- and MK-801-induced memory deficits in rats. PQ-10 also inhibits tumor cell growth with IC50 values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively. | [Uses]
PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia[1]. | [Biochem/physiol Actions]
PQ-10 is a potent and selective inhibitor of phosphodiesterase 10A (PDE10). Apparently, PQ-10 enhances basic auditory information processing in rats. PQ-10 as other PED10 inhibitors suppresses a growth of human non-small cell lung cancer (NSCLC) cell lines. | [in vivo]
PQ-10 shows region-specific increases in 2-DG uptake in the globus pallidus (equivalent to the external segment of the globus pallidus in primates) and the lateral habenula in mice[1]. | Animal Model: | 24 –28 g male C57BL/6 mice, PDE10A WT and KO mice[1] | | Dosage: | 0.16, 0.63, 2.5, and 10 mg/kg | | Administration: | s.c. | | Result: | Showed region-specific increases in 2-DG uptake in the globus pallidus (equivalent to the external segment of the globus pallidus in primates) and the lateral habenula in mice. |
| [IC 50]
PDE10A: 4.6 nM (IC50) | [References]
[1] Dedeurwaerdere S, et al. Patterns of brain glucose metabolism induced by phosphodiesterase 10A inhibitors in the mouse: a potential translational biomarker. J Pharmacol Exp Ther. 2011;339(1):210-217. DOI:10.1124/jpet.111.182766 |
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