Drug intelligence / Profile preview

cetiedil

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cetiedil is a small molecule vasodilator and anti-sickling agent belonging to the azepane class. It acts primarily as a potassium channel blocker, leading to vascular smooth muscle relaxation and peripheral vasodilation. Cetiedil has been used experimentally for the treatment of painful crises in sickle cell anemia and pain associated with arterial disease. Its pharmacological effects include inhibition of phosphodiesterase (increasing cyclic AMP), blockade of bradykinin and serotonin effects, analgesia, inhibition of platelet aggregation, reduction in plasma viscosity and fibrinogen levels, as well as modulation of erythrocyte membrane ATPases that contribute to its antisickling activity[1][3][4][5]. Mechanistically, it inhibits the Gardos phenomenon by preventing opening of potassium-specific gates in erythrocyte membranes[6], modulates cation permeability[8], and can inhibit acetylcholine release at cholinergic synapses[7].

Brand names
fusten
Other names
cetiedilum14176-10-4
02

Targets

Bradykinin B2 receptorKCNN4 (Intermediate conductance calcium-activated potassium channel protein 4)ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)5-HT (Serotonin receptors)PDE (Phosphodiesterase family)KCNQ1 (Potassium voltage-gated channel subfamily KQT member 1)

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