Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of lacidipine analogues

Abstract

Six analogues of lacidipine, (E)-diethyl 4-(2-(3-amino)-3-oxoprop-1-enyl)phenyl-2, 6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates (compounds 1-6), were synthesized and their antihypertensive effects in spontaneously hypertensive rats were evaluated by ig administration. Amongst the tested compounds, compound 5 exhibited the highest antihypertensive effect. The lasting time and potency of compound 5 showed a dose-dependent manner. The results suggested that N-tert-butyl acrylamide moiety at 2 0 -position of 4-phenyl in the structure of analogues of lacidipine is necessary to keep antihypertensive effects.

Vasodilation and Hypotension of CZ454, an Analogue of Lacidipine through Inhibiting Extracellular Calcium Influx

“…The results showed that 1.0 mg/kg CZ454 lowered systolic and diastolic blood pressures by almost 20 %. Furthermore, in the previous study, it was confi rmed that antihypertension of CZ454 could last 24 h [ 16 ] . Calcium channel blockers can impede voltage-gated calcium channels, inhibit the entry of extracellular calcium, relax vascular smooth muscle, and lower blood pressure.…”