cicletanine

Cicletanine is a small molecule diuretic and antihypertensive agent, structurally classified as a furopyridine and dihydropyridine derivative. It is approved in France for the treatment of hypertension and has also been investigated for pulmonary arterial hypertension (PAH), diabetes, hypokalemia, and hyponatremia[1][2][5]. Cicletanine exerts thiazide-like diuretic activity primarily through inhibition of the apical Na+-dependent Cl-/HCO3− anion exchanger in the distal convoluted tubule via its sulfoconjugated metabolite[6][7]. Its vasodilatory effects are multifactorial, involving inhibition of protein kinase C (PKC), stimulation of vascular prostaglandin synthesis, inhibition of low Km cyclic GMP phosphodiesterases, blockade of Ca2+ channels (directly or indirectly via K+-channel opening), interaction with alpha-adrenergic, histamine, and muscarinic receptors, stimulation of nitric oxide synthesis, and inhibition of myosin light chain kinase[1][6][7][8]. Cicletanine was originally developed by Ipsen and marketed under the brand name Tenstaten. It is currently produced by several generic manufacturers.

Brand names

Tenstaten

Other names

cicletanina