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Yonkenafil HCl is a PDE5 inhibitor potentially for the treatment of erectile dysfunction. | [Uses]
Yonkenafil (Tunodafil) hydrochloride, a novel phosphodiesterase 5 (PDE5) inhibitor, is effective in reducing cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area. Yonkenafil (Tunodafil) hydrochloride may improve cognitive function by modulating neurogenesis and has a potential therapeutic effect on Alzheimer's disease[1]. | [in vivo]
Yonkenafil (Tunodafil) hydrochloride (4-32 mg/kg, i.v. daily for 7?days) improves behavioral outcomes after stroke and reduces cerebral infarct volume, inhibits neuronal apoptosis, and significantly enhances synaptic function in ischemic brain by modulating the expression of BDNF/TrkB and NGF/TrkA[1].
Animal Model: | Male Sprague-Dawley (SD) Rat[1] | Dosage: | 4, 8, 16 and 32??mg/kg | Administration: | i.v. daily for 7?days | Result: | Induced a dose-dependent decrease in infarct volume, with an ED50 of 12.27 mg/kg.
Increased hsp70 expression, decreased apaf-1 expression, and inhibited caspase-3 and caspase-9 cleavage.
Significantly prevented neuronal damage and increases the number of surviving neurons after stroke.
Prevented decrease in synaptophysin levels and increase in PSD-95 and nNOS levels. |
| [IC 50]
PDE5 | [References]
[1] Xuemei Chen, et al. Yonkenafil: a novel phosphodiesterase type 5 inhibitor induces neuronal network potentiation by a cGMP-dependent Nogo-R axis in acute experimental stroke. Exp Neurol. 2014 Nov;261:267-77. DOI:10.1016/j.expneurol.2014.07.007 |
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