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Primaquine diphosphate

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Chemical Structure| 63-45-6 同义名 : 磷酸伯安喹 ;Primaquine phosphate;Primaquine bisphosphate;Phosphate, Primaquine;Diphosphate, Primaquine;Boucher and Muir Brand of Primaquine Phosphate;Primaquine bis(phosphate);Primaquine (Diphosphate);NSC 149765;Primaquine (phosphate)
CAS号 : 63-45-6
货号 : A273278
分子式 : C15H27N3O9P2
纯度 : 98%
分子量 : 455.337
MDL号 : MFCD00013166
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(549.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(54.9 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 Primaquine (Diphosphate) is the only generally available anti-malarial that prevents relapse in vivax and ovale malaria, and the only potent gametocytocide in falciparum malaria. The currently recommended WHO single low dose (0.25 mg base/kg) to block falciparum malaria transmission confers a very low risk of haemolytic toxicity[3]. Primaquine (PQ) prevents relapses of vivax malaria but may induce severe haemolysis in glucose-6-phosphate dehydrogenase (G6PD) deficient patients. The risks of using primaquine in infancy must be weighed against the risks of recurrent vivax malaria in early life[4]. Primaquine is also effective against all exoerythrocytic forms of the parasite and is used in conjunction with other anti-malarials for the treatment of vivax and ovale malaria. However, primaquine is often associated with serious adverse effects, in consequence of its toxic metabolites[5]. A regimen of 0.5 mg/kg primaquine daily for 14 days, on the basis of superior efficacy and good tolerability and safety in nonpregnant persons without glucose-6-phosphate dehydrogenase deficiency[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01659281 Plasmodium Falciparum Malaria Not Applicable Completed - Thailand ... 展开 >> Vector Borne Diseases Control Units (VBDC, malaria clinics) Borai, Khaosaming and Muang districts, Trat, Thailand, 23000 收起 <<
NCT02324738 Healthy Phase 4 Completed - Thailand ... 展开 >> Faculty of Tropical Medicine Bangkok, Thailand, 10400 收起 <<
NCT02192944 Healthy Phase 4 Completed - Thailand ... 展开 >> Faculty of Tropical Medicine, Mahidol University Bangkok, Thailand, 10400 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.96mL

4.39mL

2.20mL
参考文献

[1]Vale N, Moreira R, Gomes P. Primaquine revisited six decades after its discovery. Eur J Med Chem. 2009 Mar;44(3):937-53.

[2]Rubin JR, Swaminathan P, Sundaralingam M. Structure of the anti-malarial drug primaquine diphosphate. Acta Crystallogr C. 1992 Feb 15;48 ( Pt 2):379-82.

[3]Ashley EA, Recht J, White NJ. Primaquine: the risks and the benefits. Malar J. 2014;13:418. Published 2014 Nov 3

[4]Setyadi A, Arguni E, Kenangalem E, et al. Safety of primaquine in infants with Plasmodium vivax malaria in Papua, Indonesia. Malar J. 2019;18(1):111. Published 2019 Apr 2

[5]Vale N, Moreira R, Gomes P. Primaquine revisited six decades after its discovery. Eur J Med Chem. 2009;44(3):937‐953

[6]Baird JK, Hoffman SL. Primaquine therapy for malaria. Clin Infect Dis. 2004;39(9):1336‐1345