Etamicastat Explained

Class:Dopamine β-hydroxylase inhibitor
Cas Number:760173-05-5
Pubchem:10450387
Drugbank:DB15288
Chemspiderid:8625804
Unii:9X96V6DBU4
Chembl:1196088
Synonyms:BIA 5-453; BIA-5-453
Iupac Name:4-(2-aminoethyl)-3-[(3''R'')-6,8-difluoro-3,4-dihydro-2''H''-chromen-3-yl]-1H-imidazole-2-thione
C:14
H:15
F:2
N:3
O:1
S:1
Smiles:C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCN
Stdinchi:1S/C14H15F2N3OS/c15-9-3-8-4-11(7-20-13(8)12(16)5-9)19-10(1-2-17)6-18-14(19)21/h3,5-6,11H,1-2,4,7,17H2,(H,18,21)/t11-/m1/s1
Stdinchikey:CWWWTTYMUOYSQA-LLVKDONJSA-N

Etamicastat (; developmental code name BIA 5-453) is a peripherally selective dopamine β-hydroxylase (DBH) inhibitor which was under development for the treatment of hypertension (high blood pressure) and heart failure but was never marketed.[1] [2] The peripheral selectivity of etamicastat is in contrast to the earlier DBH inhibitor nepicastat, which is centrally active and produced associated side effects. Etamicastat was found to reduce blood pressure but not affect heart rate in clinical trials. The development of etamicastat was discontinued by August 2016.

See also

Notes and References

  1. Web site: Etamicastat . AdisInsight . 27 December 2019 . 21 October 2024.
  2. Dey SK, Saini M, Prabhakar P, Kundu S . Dopamine β hydroxylase as a potential drug target to combat hypertension . Expert Opin Investig Drugs . 29 . 9 . 1043–1057 . September 2020 . 32658551 . 10.1080/13543784.2020.1795830 .