A PDE2A inhibitor (IC50 = 1.6 nM); >2000-fold selective for PDE2A over a panel of ten additional PDEs; increases striatal

PF-05180999 – 1 mg

Brand:
Cayman
CAS:
1394033-54-5
Storage:
-20
UN-No:
Non-Hazardous - /

PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).{54068} It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.  

 

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Description

A PDE2A inhibitor (IC50 = 1.6 nM); >2000-fold selective for PDE2A over a panel of ten additional PDEs; increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner; inhibits MK-801-induced disruption of low frequency cortical δ oscillation in rat brain at 0.03 mg/kg; inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats at 0.1 and 0.32 mg/kg

Formal name: 4-(1-azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine

Synonyms: 

Molecular weight: 414.4

CAS: 1394033-54-5

Purity: ≥98%

Formulation: A crystalline solid

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