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PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM. The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitive medium spiny neurons in the striatum which are known to be targets of conventional antipsychotic agents. n the conditioned avoidance response assay (CAR), PF-2545920 was active with an ED50 of 1 mg/kg. Administration of PF-2545920 to mice caused a dose dependent increase in striatal cGMP.
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| Animal models | Jugular vein-cannulated male Sprague-Dawley rats |
| Formulation | 5:5:90 DMSO:1N HCl:saline |
| Dosages | 0.1 mg/kg |
| Administration | Inject intravenous through jugular vein catheter in a single dose 4 hours before feed |
| Molecular Weight | 392.45 |
| Formula | C25H20N4O |
| CAS Number | 1292799-56-4 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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BAY-60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). |
| Roflumilast
Roflumilast (APTA-2217; BYK 20869; B9302-107) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4). |
| Piclamilast
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| Apremilast
Apremilast is a novel, orally available small molecule inhibitor of PDE4 with IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM. |
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