Propentofylline

Propentofylline (HWA 285) is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders^[1][2][3][4]. In Vitro:Propentofylline (50 μM) significantly reduces Concanavalin A (HY-P2149)-stimulated reactive oxygen intermediate release from rat peritoneal macrophages and rat microglial cells^[1].
Propentofylline dose-dependently inhibits proliferation of cultured neonatal rat brain microglial cells^[1].
Propentofylline (0.1-3 mM) increases nerve growth factor synthesis and secretion by cultured mouse astroglial cells by more than 10-fold relative to controls^[1].
Propentofylline significantly reduces the release of proinflammatory cytokines from activated human blood mononuclear cells and activated microglial cells^[1].
Propentofylline completely inhibits adenosine transport via the es nucleoside transport system in cultured mouse leukemic L1210/B23.1 cells with an IC₅₀ of 9 μM^[2].
Propentofylline completely inhibits adenosine transport via the ei nucleoside transport system in cultured mouse leukemic L1210/C2 cells and rat carcinosarcoma Walker 256 cells with an IC₅₀ of 170 μM^[2].
Propentofylline completely inhibits adenosine transport via the N1 (cif) nucleoside transport system in cultured mouse leukemic L1210/MA27.1 cells with an IC₅₀ of 6 mM^[2].
Propentofylline (10 μM - 1 mM) inhibits [³H] Nitrobenzylthioinosine (HY-W010936) binding to nucleoside transporters in heart and brain tissue^[2]. In Vivo:Propentofylline (10 mg/kg; i.p.; daily; 14 days) enhances survival of CA1 pyramidal neurons and reduces ischemia-induced neuronal damage, Ca²⁺ accumulation, and reactive gliosis in gerbils with global forebrain ischemia^[2].
Propentofylline (40 mg/kg/day; p.o.; 4 weeks) does not alter adenosine receptor or es nucleoside transporter binding densities in the brains of normal gerbils^[2].
Propentofylline (25 mg/kg; p.o.; daily; 15 days) significantly improves impaired active avoidance learning in aged male SHR rats, without altering blood pressure^[3].
Propentofylline (25 mg/kg; p.o.; daily; 14 days) does not alter intact active avoidance learning in aged male WKY rats, and does not affect blood pressure^[3].
Propentofylline (3.8-30 mg/kg; i.p.; single dose) significantly improves Cycloheximide (HY-12320)-induced amnesia in male ICR mice, with a dose-related effect^[3].
Propentofylline (15-30 mg/kg; i.p.; single dose) significantly prevents Cycloheximide-induced amnesia in male ICR mice^[3].
Propentofylline (30 mg/kg; i.p.; single dose) does not alter step-down latency in naive male ICR mice^[3].