Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
279.158291553
InChI
InChI=1S/C14H21N3O3/c1-9(2)15-7-12-4-3-10-5-11(8-18)14(17(19)20)6-13(10)16-12/h5-6,9,12,15-16,18H,3-4,7-8H2,1-2H3
InChI Key
InChIKey=XCGYUJZMCCFSRP-UHFFFAOYSA-N
IUPAC Name
(7-nitro-2-{[(propan-2-yl)amino]methyl}-1,2,3,4-tetrahydroquinolin-6-yl)methanol
Traditional IUPAC Name
oxamniquine
SMILES
CC(C)NCC1CCC2=CC(CO)=C(C=C2N1)[N+]([O-])=O
pKa (strongest acidic)
14.55
pKa (Strongest Basic)
9.9
Refractivity
79.87 m3·mol-1
Dược Lực Học :
Oxamniquine is an anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release egg.
Cơ Chế Tác Dụng :
An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martidale, The Extra Pharmacopoeia, 31st ed, p121)
Oxamniquine may associate with an irreversible inhibition of the nucleic acid metabolism of the parasites. A hypothesis has been put forth that the drug is activated by a single step, in which a schistosome sulfotransferase enzyme converts oxamniquine into an ester (probably acetate, phosphate, or sulfate). Subsequently, the ester spontaneously dissociates, the resulting electrophilic reactant is capable of alkylation of schistosome DNA.
Dược Động Học :
▧ Absorption :
Well absorbed orally
▧ Metabolism :
Probably hepatic
▧ Half Life :
1-2.5 hours
Chỉ Định :
For treatment of Schistosomiasis caused by Schistosoma mansoni