132866-11-6
132866-11-6 結構式
基本信息
鹽酸樂卡地平
CLAP
mE10
c-E10
CIPER
BCL10
CarMen
LerzaM
Zandip
Lercan
Zanicor
Corifeo
Renovia
Vasodip
Lercadip
Lercapin
Lercaton
LerkaMen
Cardiovasc
BCL-10 human
Lercaridipine
LERCANIDIPINE HCL
B-cell CLL/lymphoma 10
B-cell lymphoma/leukemia 10
LERCANIDIPINE HYDROCHLORIDE
LERCANIDIPINEHYDROCHLORIDE(FORR&DONLY)
Lercanidipine hydrochloride heMihydrate
CARD-containing molecule enhancing NF-κ-B
Lercanidipine hemihydrate hydrochloride
1,4-dihydro-2,6-diMethyl-4-(3-nitrophenyl)-3,5-
1,4-Dihydro-2,6-dimethyl-4-(3-nittrophenyl)-3,5-pyridinedicarboxylicAcid2-[(3,3-Diphenylpropyl)methylamino]-1,1-dimeth
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-[(3,3-diphenylpropyl)methylamino]-1,1-dimethylethyl methyl ester hydrochloride
1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-[(3,3-diphenylpropyl)methylamino]-1,1-dimethylethyl methyl ester hydrochloride
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-2-[(3,3-diphenylpropyl)methylamino]-1,1-dimethylethyl methyl ester 3,5-pyridinedicarboxylic acid hydrochloride
O3-[1-[3,3-diphenylpropyl(methyl)amino]-2-methyl-propan-2-yl] O5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride
1,4-Dihydro-2,6-dimethyl-4-(3-nittrophenyl)-3,5-pyridinedicarboxylic Acid 2-[(3,3-Diphenylpropyl)methylamino]-1,1-dimethylethyl Methyl Ester Hydrochloride
3-O-[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] 5-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride
3,5-Pyridinedicarboxylicacid, 1,4-dihydro-2,6-diMethyl-4-(3-nitrophenyl)-,3-[2-[(3,3-diphenylpropyl)MethylaMino]-1,1-diMethylethyl] 5-Methyl ester,hydrochloride (1:1)
2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O3-[2-[3,3-diphenylpropyl(methyl)amino]-1,1-dimethyl-ethyl] ester O5-methyl ester hydrochloride
物理化學性質
制備方法
![3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-[2-[(3,3-diphenylpropyl)methylamino]-1,1-dimethylethyl] 5-methyl ester, ethanedioate (1:1)](/CAS/20211123/GIF/957215-03-1.gif)
957215-03-1
132866-11-6
以化合物（CAS:957215-03-1）為原料合成3-(1-((3,3-二苯丙基)(甲基)氨基)-2-甲基丙-2-基)5-甲基2,6-二甲基-4-(3-硝基苯基)-1,4-二氫吡啶-3,5-二羧酸酯鹽酸鹽的一般步驟如下：將10 mmol草酸鹽（實施例4）溶解于100 mL二氯甲烷中，加入含有20 mmol碳酸鉀的20 mL水溶液。分離有機相，水相用2×10 mL二氯甲烷萃取。合并有機相，用20 mL 1N鹽酸溶液處理。分離有機相并濃縮。將殘余物溶于2,000 mL水中，加入2 mL 1N鹽酸和5 mL飽和氯化鈉水溶液，形成I鹽酸鹽半水合物，過濾收集產物。產量：6.2 g（95%）；純度：99.8%（HPLC）；熔點：118-122℃。HPLC條件：RP 16柱，125×3 mm ID，5 μm，檢測波長：233 nm；洗脫液組成：0.01 mol Na2HPO4/MeOH/乙腈=25/65/10；保留時間約15 min。
參考文獻：
[1] Patent: EP1860102, 2007, A1. Location in patent: Page/Page column 1; 8; 15
常見問題列表
鹽酸樂卡地平為第三代二氫吡啶類鈣通道阻滯劑，其作用機制與同類藥物相似，即可逆地阻滯血管平滑肌細胞膜L型鈣通道的鈣離子內流，擴張外周血管而降低血壓。
鹽酸樂卡地平為第三代二氫吡啶類鈣通道阻滯劑，其親脂性較高，起效時間較慢，作用時間較長，血漿達峰時間為2~3h，具有首過代謝的飽和性，食物可增加其吸收，吸收后迅速分布、積聚在細胞膜脂質雙層，蛋白結合率高于98%。鹽酸樂卡地平主要由CYP3A4代謝，具有廣泛的首過效應，無活性代謝產物。50%由糞便排出，44%由尿液排出。
長效鈣拮抗劑-鹽酸樂卡地平，其降壓療效肯定，同時具有腎臟保護作用，對血脂也有利。
| Target | Value |
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Calcium channel
() |
Lercanidipine在體外的鈣拮抗活性與通過L型鈣離子通道流入平滑肌細胞的鈣內流的逐漸阻滯相關。Lercanidipine抑制細胞膽甾醇酯的形成。在臨床使用劑量下，Lercanidipine在體外可抑制巨噬細胞在動脈粥樣硬化形成以及斑塊穩(wěn)定性中的功能。