Etamicastat

Etamicastat
Clinical data
Other names	BIA 5-453; BIA-5-453
Drug class	Dopamine β-hydroxylase inhibitor
Identifiers
	IUPAC name 4-(2-aminoethyl)-3-[(3R)-6,8-difluoro-3,4-dihydro-2H-chromen-3-yl]-1H-imidazole-2-thione;
CAS Number	760173-05-5;
PubChem CID	10450387;
DrugBank	DB15288;
ChemSpider	8625804;
UNII	9X96V6DBU4;
ChEMBL	ChEMBL1196088;
CompTox Dashboard (EPA)	DTXSID00226940 ;
Chemical and physical data
Formula	C14H15F2N3OS
Molar mass	311.35 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1[C@H](COC2=C1C=C(C=C2F)F)N3C(=CNC3=S)CCN;
	InChI InChI=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; Key:CWWWTTYMUOYSQA-LLVKDONJSA-N;

Etamicastat (INNTooltip International Nonproprietary Name; 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.^[2] Etamicastat was found to reduce blood pressure but not affect heart rate in clinical trials.^[2] The development of etamicastat was discontinued by August 2016.^[1]

References

^ ^a ^b "Etamicastat". AdisInsight. 27 December 2019. Retrieved 21 October 2024.
^ ^a ^b ^c Dey SK, Saini M, Prabhakar P, Kundu S (September 2020). "Dopamine β hydroxylase as a potential drug target to combat hypertension". Expert Opin Investig Drugs. 29 (9): 1043–1057. doi:10.1080/13543784.2020.1795830. PMID 32658551.

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