Лерканидипин

Описание

Lerdip was launched in the Netherlands for hypertension. It is prepared in four steps, the last of which is a Hantsch reaction of 1-[(3,3-diphenyl)-N-methylpropylamino]- 2-methyl-2-propyl-2-(3-nitrobenzylidene)acetoacetate with methyl 3-aminocrotonate. This compound was designed to be very lipophilic which imparts the drug with a gradual onset and a long duration of action as a result of prolonged exposure to receptors by partitioning into membranes. It is an antagonist of L-type calcium channels with no activity in smooth muscle cells, is tissue selective, lacks any myocardial contractility impairment, has no neuroendocrine activation, and has negligible affinity for neurotransmitter receptors such as α₁- and α₂-adrenergic receptors. While sold as a racemate, the calcium channel activity is found in the (S)- isomer with the (R)-isomer being 2-orders of magnitude less active. It has an increased cardiac contractility index which is much more than Nitrendipine or nifedipine. The good selectivity causes a reduction in blood pressure with no negative inotropic effects.

Использование

Antihypertensive compound; calcium channel blocker.