Aprobarbital
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Aprobarbital is a barbiturate derivative synthesized in the 1920s by Ernst Preiswerk. It was determined that the substance was capable of demonstrating sedative, hypnotic, and anticonvulsant effects. A primary treatment indicated for the use of aprobarbital was subsequently insomnia. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed.
Aprobarbital is a barbiturate derivative synthesized in the 1920s by Ernst Preiswerk. It was determined that the substance was capable of demonstrating sedative, hypnotic, and anticonvulsant effects. A primary treatment indicated for the use of aprobarbital was subsequently insomnia. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed.
Aprobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Aprobarbital also appears to bind neuronal nicotinic acetylcholine receptors.
用于镇静、催眠。
