التفاصيل البيبلوغرافية
| العنوان: |
A new pyrazolo pyrimidine derivative inhibitor of cyclooxygenase-2 with anti-angiogenic activity |
| المؤلفون: |
Devesa, Isabel1, Alcaraz, M. José1, Riguera, Ricardo2, Ferrándiz, M. Luisa1 Luisa.ferrandiz@uv.es |
| المصدر: |
European Journal of Pharmacology. Mar2004, Vol. 488 Issue 1-3, p225. 6p. |
| مصطلحات موضوعية: |
*CYCLOOXYGENASES, *PROSTAGLANDINS, *NEOVASCULARIZATION, *EDEMA |
| مستخلص: |
In a previous study, we reported a new pyrazolo pyrimidine derivative, N4-benzyl-N6,N6-dimethyl-1-1(tert-butyl)-1H-pyrazolo[3,4-d]pyrimidine-6,4-diamine (DPP), which inhibited potently cyclooxygenase-2 activity in intact cell assays with minor activity against cyclooxygenase-1 (IC50=0.9 nM for cyclooxygenase-2 versus IC50=59.6 nM for cyclooxygenase-1). In the present work, this behaviour was confirmed in vivo by using the 24-h zymosan-injected mouse air pouch model (ID50=1.36 nmol/pouch for prostaglandin E2 level). We also studied the possible beneficial effect of DPP in the angiogenesis-dependent murine air pouch granuloma and rat paw carrageenan-induced hyperalgesia models. DPP exerted analgesic and anti-angiogenic (52% reduction in angiogenesis at 10 mg/kg, i.p.) effects that may be associated with inhibition of cyclooxygenase-2 activity. [Copyright &y& Elsevier] |
| قاعدة البيانات: |
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