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metomidate
- Development stage
- Phase 1
- Lead developer
- Johnson & Johnson
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Immersion (for Fish And Aquatic Animals)
01
Overview
Metomidate is a non-barbiturate imidazole derivative used primarily as a sedative-hypnotic and anesthetic agent, mainly in veterinary medicine and in some countries for humans[1][2][5]. It acts by positive allosteric modulation of the GABAA receptor, enhancing inhibitory neurotransmission in the central nervous system. Metomidate also inhibits adrenal steroidogenesis by blocking the enzymes 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2); this property is exploited in nuclear medicine as radiolabeled metomidate derivatives are used for imaging adrenal cortical tumors[4].
- Brand names
- HypnodilNokemylAquacalm
- Other names
- Methoxymol5377-20-8
02
Targets
CYP11B2 (Cytochrome P450 11B2)GABRR (GABA-A receptor subunit rho)CYP11B1 (Cytochrome P450 11B1)
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