Drug intelligence / Profile preview

metomidate

Development stage: Unknown
Lead developer: Janssen Pharmaceutica
Modality: Small Molecules
Administration: Oral, Intravenous, Immersion (for Fish And Aquatic Animals)

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

Targets

CYP11B2 (Cytochrome P450 11B2)GABRR (GABA-A receptor subunit rho)

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