Anagrelide-13C3 is intended for use as an internal standard for the quantification of anagrelide by GC- or LC-MS. Anagrelide is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 36 nM for the human platelet enzyme).1 It inhibits thrombopoietin-induced megakaryocytopoiesis of isolated human CD34+ progenitor cells (IC50 = 26 nM).2 Anagrelide reduces platelet aggregation induced by ADP, collagen, thrombin, or arachidonic acid in isolated rabbit platelet rich-plasma (EC50s = 0.31, 0.08, 0.18, and 0.1 µg/ml, respectively).3 It inhibits platelet thrombus formation in a dog model of electrically induced carotid artery thrombosis when administered at doses ranging from 0.5 to 5 mg/kg.4 Formulations containing anagrelide have been used in the treatment of thrombocythemia.
1.Wang, G., Franklin, R., Hong, Y., et al.Comparison of the biological activities of anagrelide and its major metabolites in haematopoietic cell culturesBr. J. Pharmacol.146(3)324-332(2005) 2.Hong, Y., Wang, G., Gutierrez del Arroyo, A., et al.Comparison between anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: Selectivity of anagrelide for the megakaryocytic lineageLeukemia20(6)1117-1122(2006) 3.Fleming, J.S., and Buyniski, J.P.A potent new inhibitor of platelet aggregation and experimental thrombosis, anagrelide (BL-4162A)Thromb. Res.15(3-4)373-388(1979) 4.Fleming, J.S., and Buyniski, J.P.AnagrelideNew drugs annual: Cardiovascular drugs277-294(1983)