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Zamicastat
Zamicastat (; developmental code name BIA-5-1058) is a peripherally selective drug, peripherally selective dopamine β-hydroxylase (DBH) enzyme inhibitor, inhibitor which is under development for the treatment of pulmonary arterial hypertension (PAH) and heart failure. It is structural analog, structurally related to etamicastat and is said to be an improved version of this drug. As of July 2022, zamicastat is in Phases of clinical research#Phase II, phase 2 clinical trials for PAH and Phases of clinical research#Phase I, phase 1 clinical trials for heart failure. However, no recent development has been reported for heart failure. See also * Nepicastat References Secondary amines Chromanes Dopamine beta hydroxylase inhibitors Fluoroarenes Imidazoles Peripherally selective drugs Thioureas {{Antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine β-hydroxylase
Dopamine beta-hydroxylase (DBH), also known as dopamine beta-monooxygenase, is an enzyme () that in humans is encoded by the DBH gene. Dopamine beta-hydroxylase catalysis, catalyzes the conversion of dopamine to norepinephrine. The three substrate (biochemistry), substrates of the enzyme are dopamine, vitamin C (ascorbate), and oxygen, O2. The product (chemistry), products are norepinephrine, dehydroascorbate, and water, H2O. DBH is a 290 kDa copper-containing oxygenase consisting of four identical subunits, and its activity requires ascorbate as a Cofactor (biochemistry), cofactor. It is the only enzyme involved in the synthesis of small-molecule neurotransmitters that is membrane-bound, making norepinephrine the only known transmitter synthesized inside vesicles. It is expressed in noradrenergic neurons of the central nervous system (i.e. locus coeruleus) and peripheral nervous systems (i.e. sympathetic ganglia), as well as in chromaffin cells of the adrenal medulla. Mecha ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
