Details
| Stereochemistry | RACEMIC |
| Molecular Formula | 2C36H41N3O6.2ClH.H2O |
| Molecular Weight | 1314.392 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.Cl.Cl.COC(=O)C1=C(C)NC(C)=C(C1C2=CC=CC(=C2)[N+]([O-])=O)C(=O)OC(C)(C)CN(C)CCC(C3=CC=CC=C3)C4=CC=CC=C4.COC(=O)C5=C(C)NC(C)=C(C5C6=CC=CC(=C6)[N+]([O-])=O)C(=O)OC(C)(C)CN(C)CCC(C7=CC=CC=C7)C8=CC=CC=C8
InChI
InChIKey=ZFZXJUJPHGPYAJ-UHFFFAOYSA-N
InChI=1S/2C36H41N3O6.2ClH.H2O/c2*1-24-31(34(40)44-6)33(28-18-13-19-29(22-28)39(42)43)32(25(2)37-24)35(41)45-36(3,4)23-38(5)21-20-30(26-14-9-7-10-15-26)27-16-11-8-12-17-27;;;/h2*7-19,22,30,33,37H,20-21,23H2,1-6H3;2*1H;1H2
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugs.com/history/lercanidipine.html | https://www.ncbi.nlm.nih.gov/pubmed/27794423
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/history/lercanidipine.html | https://www.ncbi.nlm.nih.gov/pubmed/27794423
Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. Lercanidipine exists as a racemate, with anti-hypertensive activity residing primarily in S-enantiomer. NDA for lercanidipine was submitted to FDA in 2002 by Forest Laboratories, but FDA refused to approve the drug, and lercanidipine is not marketed in USA. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2095229 |
2.2 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ZANIDIP Approved UseLercanidipine is indicated for the treatment of mild to moderate essential hypertension |
|||
| Primary | Unknown Approved UseUnknown |
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| Palliative | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [The effect of calcium channel blocker lercanidipine on lowgrade inflammation parameters in essential hypertension patients]. | 2006 Dec |
|
| Lercanidipine in the treatment of hypertension. | 2007 Mar |
|
| Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellular reactive oxygen species and inactivating Ras-ERK1/2 signaling. | 2009 Jan |
Sample Use Guides
The recommended dosage is 10 mg orally once a day at least 15 minutes before meals; the dose may be increased to 20 mg depending on the individual patient's response. In preclinical models lercanidipine is administered intraperitoneally.
Route of Administration:
Other
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100000159821
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ACTIVE MOIETY
SUBSTANCE RECORD
