Levamlodipine hydrobromide  (Synonyms: (S)-Amlodipine hydrobromide; Levoamlodipine hydrobromide)

Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrobromide is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine hydrobromide significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine hydrobromide not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine hydrobromide exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine hydrobromide may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine hydrobromide can be used in research related to hypertension and atherosclerosis^[1][2][3].

Levamlodipine hydrobromide-Sorbic acid (HY-N0626) ion pair patches (¹³-15% (w/w) LAM-SA, 10% (w/w) IPM; 72 h) maintain equivalent porcine skin permeability to free levamlodipine patches, and addition of 10% IPM significantly enhances permeability; the optimized 13% LAM-SA, 10% IPM, 70 μm patch achieves high, predictable transdermal delivery over 72 h^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Levamlodipine hydrobromide (2.5 mg/d; intragastric administration; once daily; for 8 consecutive weeks) exerts no significant inhibitory effect on intimal hyperplasia after balloon-induced endothelial injury of the abdominal aorta in rabbits, but it can improve plaque stability by reducing the expression of MMP-9 in plaques. Meanwhile, the serum LDL-C level shows a decreasing trend, while the serum TNF-α level increases significantly^[1].
Levamlodipine (1-4 mg/kg; intragastric administration; single dose; 1 mg/kg/day; p.o.; daily; 16 weeks) hydrobromide reduces blood pressure in male SHR in a dose-dependent manner^[2].
The ion-pair transdermal patch of Levamlodipine hydrobromide and sorbic acid (HY-N0626) (12-15% w/w; transdermal administration; single dose; 72 h) significantly reduces skin irritation in rabbits. Compared with non-ion-pair levamlodipine patches, it shows a lower erythema index, milder epidermal thickening, and faster skin recovery^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

489.79

C₂₀H₂₆BrClN₂O₅

865430-78-0

O=C(C1=C(COCCN)NC(C)=C(C(OC)=O)[C@@H]1C2=CC=CC=C2Cl)OCC.Br

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Aidong Z, et al. Levamlodipine besylate influence on intimal hyperplasia and plaque stability after balloon injury in rabbits[J]. J Clin Cardiol, 2015, 31(1): 101-105.

  [2]. Yang YL, et al. Synergic effects of levamlodipine and bisoprolol on blood pressure reduction and organ protection in spontaneously hypertensive rats. CNS Neurosci Ther. 2012;18(6):471-474.  [Content Brief]

  [3]. Wu J, et al. Development of levamlodipine long-acting patches based on an ion-pair strategy: Investigation of the mechanism for reducing skin irritation. Int J Pharm. 2024;665:124703.  [Content Brief]