etamicastat
Description
etamicastat: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10450387 |
| CHEMBL ID | 1196088 |
| SCHEMBL ID | 1028587 |
| SCHEMBL ID | 1560760 |
| MeSH ID | M0561941 |
Synonyms (19)
| Synonym |
|---|
| CHEMBL1196088 |
| unii-9x96v6dbu4 |
| etamicastat [inn] |
| etamicastat |
| 9x96v6dbu4 , |
| 5-(2-aminoethyl)-1-((3r)-6,8-difluoro-3,4-dihydro-2h-chromen-3-yl)-1,3-dihydro-2h-imidazole-2-thione |
| 760173-05-5 |
| SCHEMBL1028587 |
| DTXSID00226940 |
| SCHEMBL1560760 |
| (r)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1h-imidazole-2(3h)-thione |
| CWWWTTYMUOYSQA-LLVKDONJSA-N |
| HY-14838 |
| CS-0003588 |
| DB15288 |
| 4-(2-aminoethyl)-3-[(3r)-6,8-difluoro-3,4-dihydro-2h-chromen-3-yl]-1h-imidazole-2-thione |
| bia 5-453 |
| Q27273344 |
| AKOS040733131 |
Research Excerpts
Overview
Etamicastat is a reversible dopamine-β-hydroxylase inhibitor that decreases noradrenaline levels in sympathetically innervated tissues and slows down sympathetic nervous system drive. It has been administered orally at doses up to 600 mg once daily for 10 days to male healthy volunteers.
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " There was no serious adverse event or clinically significant abnormality in clinical laboratory tests, vital signs, or ECG parameters." | ( Safety, tolerability, and pharmacokinetics of etamicastat, a novel dopamine-β-hydroxylase inhibitor, in a rising multiple-dose study in young healthy subjects. Almeida, L; Falcão, A; Igreja, B; Nunes, T; Rocha, JF; Soares-da-Silva, P; Vaz-da-Silva, M; Wright, LC, 2010) | 0.62 |
Pharmacokinetics
Etamicastat Tmax was 1 hour postdose, and mean t½ was 19 to 28 hours following repeated administration. Large interindividual variability dependent on the NAT2 acetylator status was found in the pharmacokinetic parameters of etamicast at and BIA 5-961.
Compound-Compound Interactions
| Excerpt | Reference | Relevance |
|---|---|---|
| " This study evaluated the efficacy of etamicastat, a dopamine-β-hydroxylase (DβH) inhibitor, in controlling high blood pressure in the spontaneously hypertensive rat (SHR), either alone or in combination with other classes of antihypertensives." | ( Blood pressure-decreasing effect of etamicastat alone and in combination with antihypertensive drugs in the spontaneously hypertensive rat. Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Pires, NM; Soares-da-Silva, P; Wright, LC, 2015) | 0.96 |
Bioavailability
The absolute oral bioavailability of etamicastat was 64% of the administered dose. Despite its lower bioavailability and higher clearance, as compared to nepicastat, etamicstat showed preferential distribution to peripheral tissues and high plasma free fraction (15%)
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " No deleterious effects, including ECG disturbance were observed in male and female dogs dosed by gavage with etamicastat (up to 20mg/kg/day) for 28 days." | ( Cardiovascular safety pharmacology profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor. Igreja, B; Lacroix, P; Loureiro, AI; Pires, NM; Soares-da-Silva, P, 2015) | 0.89 |
Research
Studies (18)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.56) | 29.6817 |
| 2010's | 16 (88.89) | 24.3611 |
| 2020's | 1 (5.56) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (33.33%) | 5.53% |
| Reviews | 1 (5.56%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 11 (61.11%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||