Cinaciguat (BAY 58-2667) is an experimental drug for the treatment of
acute decompensated heart failure
Acute decompensated heart failure (ADHF) is a sudden worsening of the signs and symptoms of heart failure, which typically includes difficulty breathing (dyspnea), edema, leg or feet swelling, and Fatigue (medical), fatigue. ADHF is a common and ...
.
Mechanism of action
Cinaciguat activates the
soluble guanylate cyclase
Soluble guanylyl cyclase (sGC) is the only known receptor for nitric oxide, NO. It is soluble, i.e. completely intracellular. Most notably, this enzyme is involved in vasodilation. In humans, it is encoded by the genes GUCY1A2, GUCY1A3, GUCY ...
(sGC) which is a receptor for
nitric oxide. This increases biosynthesis of
cyclic GMP
Cyclic guanosine monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate (GTP). cGMP acts as a second messenger much like cyclic AMP. Its most likely mechanism of action is activation of intracellular protein kinases in r ...
, resulting in
vasodilation
Vasodilation is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. The process is the opposite of vasoconstrictio ...
.
[Schubert-Zsilavecz, M, Wurglics, M, ''Neue Arzneimittel 2009'']
See also
*
Riociguat
Riociguat, sold under the brand name Adempas, is a medication by Bayer that is a stimulator of soluble guanylate cyclase (sGC). It is used to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH ...
, another drug stimulating sGC, but with a different mechanism
*
PDE5 inhibitor
A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a vasodilating drug that works by blocking the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplyi ...
s act further downstream in the nitric oxide signalling pathway, reducing cyclic GMP degradation.
References
Vasodilators
Benzoic acids
Phenol ethers
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