キナクリン二塩酸水和物 化學(xué)特性,用途語,生産方法
外観
白色～黃褐色, 結(jié)晶性粉末～粉末
溶解性
水にやや溶けやすい。水、エタノールに可溶、アセトン、エーテル、ベンゼンに難溶。水溶液はケイ光を発する。熱水及び熱エタノールに溶け、アセトンにほとんど溶けない。
用途
抗マラリア剤、カルモジュリン阻害剤、ホスホリパーゼ阻害剤
効能
抗マラリア薬, 抗原蟲薬
化學(xué)的特性
yellow crystals or powder
使用
Quinacrine dihydrochloride has been used:
- in its uptake and accumulation studies in mouse lung slices using fluorescence microscope
- in the staining of ATP vesicles in mesenchymal stem cells (MSCs)
- in uptake-release assay for characterization of dense granule functionality of platelets
適応癥
Quinacrine is no longer used extensively as an antimalarial
drug and has been largely replaced by the 4-
aminoquinolines.
抗菌性
Mepacrine is active against the asexual erythrocytic stage of
all four Plasmodium spp. that infect humans and the gametocytes
of P. vivax and P. malariae. The enantiomers have equal
antimalarial activity. It exhibits broad activity
in experimental
models against T. cruzi, Leishmania spp., E. histolytica,
Trichomonas vaginalis, G. lamblia and Blastocystis hominis. It is
also active against tapeworms.
獲得抵抗性
The structural resemblance to chloroquine suggests the likelihood
of cross-resistance with that drug, but evidence for this
is equivocal.
一般的な説明
Bright yellowish needles or bright yellow powder. Odorless. pH of a 1% aqueous solution is about 4.5.. Used as an anti-malarial drug. Moderately toxic.
空気と水の反応
Water soluble.
反応プロフィール
QUINACRINE DIHYDROCHLORIDE is an acidic salt of an amine. React as a weak acid to neutralize bases.
火災(zāi)危険
Flash point data for QUINACRINE DIHYDROCHLORIDE are not available, but QUINACRINE DIHYDROCHLORIDE is probably combustible.
応用例（製薬）
A synthetic acridine derivative, formulated as the hydrochloride
for oral use.
薬物動(dòng)態(tài)學(xué)
Oral absorption: Good
C
max 100 mg oral: 50 μg/L after 1–3 h
Plasma half-life: 5 days
Plasma protein binding: 85%
There is extensive tissue binding and a six-fold concentration into
leukocytes from plasma. About 10% of the daily dose is excreted
in the urine. It is widely distributed throughout the body.
臨床応用
Giardiasis
Prophylaxis of malaria
Tapeworm infections
副作用
Dizziness, headache and gastric problems are common.
Toxic psychoses, bone marrow depression, yellow skin and
exfoliative dermatitis are described. Poor toleration is noted,
especially
in children. It should not be used in combination
with 8-aminoquinolines.
純化方法
It crystallises from H2O (solubility is 2.8% at room temperature) as yellow crystals. It is slightly soluble in MeOH and EtOH. The free base crystallises from Me2CO or pet ether with m 86-88o, or aqueous EtOH with 85-87.5o. The bismethiodide has m 224o (from MeOH/EtOAc/Et3N), and the picrate has m 207-208o(dec) when crystallised from Me2CO/EtOH. It is an antimalarial, antiprotozoal and intercalates DNA. [Wolfe Antibiot 3 (Springer-Verlag) 203 1975, Beilstein 22 III/IV 6247, 22/12 V 235.]
キナクリン二塩酸水和物 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品