| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T92138 | ||||
| Target Name | Phosphodiesterase | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | NM-702 | Drug Info | IC50 = 0.179~0.26 nM | [552736] | |
| Action against Disease Model | NM-702 | We investigated the effects of NT-702, a selective phosphodiesterase (PDE) 3 inhibitor, on arterioles isolated from rabbit l uMbar spinal cords. NT-702 caused a dose-dependent dilation of the isolated spinal arterioles. The disruption of endotheli uM produced a significant reduction of higher concentrations (10(-7) and 10(-6) M), but not lower concentrations (less than 10(-8) M), of NT-702-induced vasodilation. The NT-702-induced vasodilation of the arterioles with endotheli uM was not affected by pretreatment with an inhibitor of nitric oxide, cyclooxygenase, or cytochrome P-450 monooxygenase. In contrast, catalase reduced significantly the higher concentrations of NT-702-induced vasodilation only. Tetraethylammoni uM (TEA) completely reduced the lower concentrations of NT-702-induced vasodilation, but decreased only partially the higher concentrations of NT-702-induced vasodilation of the arterioles with endotheli uM. Hydrogen peroxide dilated significantly theisolated arterioles with endotheli uM, the response of which was reduced significantly by TEA. KT5720 (a selective protein kinase inhibitor) significantly decreased both the lower and higher concentrations of NT-702-induced vasodilation of the arterioles with endotheli uM. | [552830] | Drug Info | |
| References | |||||
| Ref 552830 | NT-702, a selective phosphodiesterase 3 inhibitor, dilates rabbit spinal arterioles via endothelium-dependent and endothelium-independent mechanisms. J Physiol Sci. 2008 Aug;58(4):229-37. doi: 10.2170/physiolsci.RP003808. Epub 2008 Jun 18. | ||||
| Ref 552736 | NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase inhibitor, improves reduced walking distance and lowered hindlimb plantar surface temperature in a rat experimental intermittent claudication model. Life Sci. 2007 Sep 1;81(12):970-8. Epub 2007 Aug 8. | ||||
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