Introduction of
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Levamlodipine ((S)-Amlodipine; Levoamlodipin) is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine 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 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 exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine 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 can be used in research related to hypertension and atherosclerosis[1][2][3].
IC50 & Target:Calcium channel
[1].
In Vitro:Levamlodipine-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].
In Vivo:Levamlodipine (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) reduces blood pressure in male SHR in a dose-dependent manner
[2].
The ion-pair transdermal patch of Levamlodipine 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].
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