69-44-3
基本信息
鹽酸阿莫他喹
鹽酸阿莫地喹
阿莫地喹鹽酸鹽
阿莫地喹二鹽酸鹽
阿莫他喹二鹽酸鹽
7-氯-4-(3'-二乙基氨基甲基-4'-羥基苯胺基)喹啉二鹽酸鹽
4-((7-氯喹啉-4-基)氨基)-2-((二乙胺基)甲基)苯酚二鹽酸鹽
camoquinhydrochloride
AMODIAQUIN HYDROCHLORIDE
Acrichin dihydrochloride
AMODIAQUINE HYDROCHLORIDE
AMODIAQUIN DIHYDROCHLORIDE
AMODIAQUINE DIHYDROCHLORIDE
BULK DRUG : AMODIAQUINE HYDROCHLORIDE (DMF GRADE)
4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-o-cresodihydrochloride
4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-o-cresoldihydrochloride
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
2. 與三硅酸鎂和白陶土同時(shí)服用,氯喹胃腸吸收下降,阿莫地喹可能同氯喹相同。
3. 皮下注射狂犬病疫苗的同時(shí)服用氯喹預(yù)防瘧疾時(shí),可能會(huì)干擾抗體的產(chǎn)生。在使用阿莫地喹時(shí)應(yīng)考慮。
阿莫地喹的臨床前研究就估計(jì)到了它的誘變和遺傳毒性效應(yīng)。細(xì)菌誘變的實(shí)驗(yàn)報(bào)告顯示,對(duì)沙門菌屬的誘變作用很弱,但對(duì)妊娠期服用阿莫地喹的劑量還沒(méi)有研究,也就沒(méi)有引起器官和結(jié)構(gòu)畸形的數(shù)據(jù)資料。有資料顯示,在妊娠期服用氯喹后出現(xiàn)了幾例先天畸形(法洛四聯(lián)癥、先天性甲狀腺功能減退、脈絡(luò)膜視網(wǎng)膜炎耳聾),氯喹能通過(guò)胎盤屏障,阿莫地喹可能也可以通過(guò),但在妊娠期使用阿莫地喹藥物沒(méi)有發(fā)現(xiàn)先天畸形。盡管這樣,有研究者認(rèn)為妊娠期應(yīng)禁用阿莫地喹。而其他的研究者認(rèn)為即使沒(méi)有足夠的資料顯示阿莫地喹的安全 性,但是在沒(méi)有找到可替代的藥物之前不應(yīng)該限制它的使用。WHO 也認(rèn)識(shí)到了阿莫地喹的毒性,但沒(méi)有在妊娠期禁用阿莫地喹的數(shù)據(jù),因此需要進(jìn)一步的研究。
EC50: ~20 μM (Nurr1-LBD (ligand binding domain))
Histamine N-methyltransferase
Amodiaquine (10-20 μM; 4 hours) treatment suppresses LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
Amodiaquine (5 μM; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primary dopamine cells as examined by the number of TH
+
neurons and dopamine uptake. The neuroprotective effect of Amodiaquine is also observed in rat PC12 cells.
RT-PCR
Cell Line: | Primary microglia |
Concentration: | 10 μM, 15 μM, 20 μM |
Incubation Time: | 4 hours |
Result: | Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner. |
Amodiaquine (40 mg/kg; intraperitoneal injection; daily; for 3 days; male ICR mice) treatment diminishes perihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppresses ICH-induced mRNA expression of IL-1β, CCL2 and CXCL2, and ameliorated motor dysfunction of mice.
Animal Model: | Male ICR mice (8-10?weeks of age) induced ntracerebral hemorrhage (ICH) |
Dosage: | 40 mg/kg |
Administration: | Intraperitoneal injection; daily; for 3 days |
Result: | Diminished perihematomal activation of microglia/macrophages and astrocytes. |