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Metharbital is a barbiturate anticonvulsant, similar to phenobarbital, marketed as Gemonil by Abbott Laboratories. It was patented in 1905 by Emil Fischer of Merck.
- Mechanism
- Curator reviewed
Metharbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
- Primary indication
- Metharbital is used for the treatment of epilepsy.Curator reviewed
- Formula / weight
- C9H14N2O3 · 198.2191 g/mol (avg)
Resolves to
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Which drugs share a target with Metharbital, and which of those have an active Phase 3 trial?