Lercanidipine targets L-type calcium channels in the smooth muscle cells of blood vessels. By blocking these channels, it prevents calcium influx, leading to relaxation of vascular smooth muscle and vasodilation. This results in improved blood flow and lowered blood pressure. Unlike non-dihydropyridine calcium channel blockers such as verapamil and diltiazem, lercanidipine has no significant effect on calcium channels in the heart at usual therapeutic doses and therefore does not lower heart rate.

In vitro, lercanidipine acts as a selective L-type calcium channel blocker in vascular smooth muscle. Its activity has been characterized in various isolated tissue preparations and cell-based assays. The compound's high vascular selectivity and lack of cardiac effects distinguish it from other calcium channel blockers. It is used in research to study calcium channel function and vascular physiology.

In vivo, lercanidipine is an orally active antihypertensive agent. It is slowly but completely absorbed from the intestine. The antihypertensive effect lasts for at least 24 hours due to a mild depot effect. It is used primarily for the treatment of essential hypertension.

The activity of Lercanidipine can be assessed using radioligand binding assays with membranes prepared from tissues expressing L-type calcium channels. The displacement of a radiolabeled dihydropyridine ligand is measured to determine the binding affinity. Functional assays measuring calcium influx or smooth muscle contraction in isolated vascular tissues can also be used.

To evaluate the cellular effects of Lercanidipine, vascular smooth muscle cells are treated with the compound. Calcium influx is measured using fluorescent calcium indicators. The effects on cell contraction and proliferation are assessed. The compound's selectivity for vascular versus cardiac calcium channels is evaluated using appropriate cell types.

In vivo studies with Lercanidipine typically involve administration to animal models via oral routes. In models of hypertension, the compound's effects on blood pressure are assessed. Its effects on heart rate and cardiac function are monitored. Pharmacokinetic parameters, such as bioavailability and half-life, are also characterized.

Lercanidipine has a molecular formula of C36H41N3O6 and a molecular weight of 611.73 g/mol. Its CAS number is 100427-26-7. It is a solid with a melting point of 186-190°C. It is used in the form of the hydrochloride and is taken orally. It should be stored according to the manufacturer's instructions.

Lercanidipine is generally well tolerated. No adverse effect was observed in more than 1% of treated patients. Typical side effects include headache, dizziness, tachycardia, palpitations, flushing, and edema. Edema occurs much less frequently with lercanidipine compared with first-generation dihydropyridines such as nifedipine. It is contraindicated in unstable angina, uncontrolled heart failure, and during pregnancy.

[1]. Barrios,"nV., et al., Lercanidipine is an effective and well tolerated"nantihypertensive drug regardless the cardiovascular risk profile: The"nLAURA study. Int J Clin Pract, 2006. 60(11): p. 1364-70.

[2]. Burnier,"nM., M. Pruijm, and G. Wuerzner, Treatment of essential hypertension"nwith calcium channel blockers: what is the place of lercanidipine?"nExpert Opin Drug Metab Toxicol, 2009. 5(8): p. 981-7.

[3]. Grassi"nG, et, al. Lercanidipine in the Management of Hypertension: An Update. J"nPharmacol Pharmacother. Oct-Dec 2017;8(4):155-165.

[4]. Clinical efficacy of calcium channel blockers slow the third generation of lercanidipine in the treatment of patients with arterial hypertension and metabolic disorders (review). Georgian Med News. 2015 Feb;(239):51-6. Review. Russian.

Lercanidipine is a diarylmethane compound. It is a dihydropyridine calcium channel blocker. It is marketed under several brand names, including Zanidip. Indications: Used to treat hypertension, angina pectoris, and Raynaud's syndrome. Mechanism of Action: Lercanidipine inhibits the influx of extracellular calcium ions across the smooth muscle cell membranes of myocardium and vascular tissues by altering ion channels, inhibiting ion gating mechanisms, and/or interfering with the release of calcium ions from the sarcoplasmic reticulum. The decrease in intracellular calcium ion concentration inhibits the contractile process of myocardial smooth muscle cells, leading to dilation of coronary and systemic arteries, increased oxygen supply to myocardial tissue, reduced total peripheral resistance, decreased systemic blood pressure, and reduced afterload. Pharmacodynamics: Lercanidipine is a dihydropyridine calcium channel blocker that can be used alone or in combination with angiotensin-converting enzyme inhibitors. Lercanidipine hydrochloride is a medication used to treat hypertension, chronic stable angina, and prinzmetal angina. Its mechanism of action is similar to other peripheral vasodilators. It inhibits the influx of extracellular calcium ions across the membranes of cardiomyocytes and vascular smooth muscle cells by inhibiting calcium channel deformation, blocking ion-gating mechanisms, and/or interfering with calcium ion release from the sarcoplasmic reticulum. The decrease in intracellular calcium concentration inhibits the contraction of myocardial smooth muscle cells, leading to dilation of coronary and systemic arteries, increasing oxygen supply to myocardial tissue, reducing total peripheral resistance, lowering systemic blood pressure, and reducing afterload.
Lercanidipine is a dihydropyridine calcium channel blocker used for the treatment of essential hypertension. It is also used for angina pectoris symptoms and Raynaud's syndrome. Its high vascular selectivity and lack of cardiac effects make it a valuable antihypertensive agent. It is a research tool for studying calcium channel function and vascular physiology.

C36H41N3O6

611.72724

611.299

100427-26-7

Lercanidipine hydrochloride;132866-11-6;(R)-Lercanidipine;185197-70-0;(R)-Lercanidipine hydrochloride;187731-34-6;Lercanidipine-d3 hydrochloride;1189954-18-4;(S)-Lercanidipine hydrochloride;184866-29-3

65866

Light yellow to yellow solid powder

1.2±0.1 g/cm3

712.5±60.0 °C at 760 mmHg

118-120ºC

384.7±32.9 °C

0.0±2.3 mmHg at 25°C

1.580

8.04

1

8

13

45

1090

0

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC(C)(C)CN(CCC(C3=CC=CC=C3)C4=CC=CC=C4)C

ZDXUKAKRHYTAKV-UHFFFAOYSA-N

InChI=1S/C36H41N3O6/c1-24-31(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/h7-19,22,30,33,37H,20-21,23H2,1-6H3

5-O-[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ~100 mg/mL (~163.5 mM; with ultrasonication)

Solubility in Formulation 1: dissolve in 20% ethanol, 20% DMSO and 60% normal saline (Please use freshly prepared in vivo formulations for optimal results.)