| 药品名称 |
Metharbital
|
| 分子靶点 |
Gamma-aminobutyric acid receptor subunit alpha-1;Gamma-aminobutyric acid receptor subunit alpha-2;Gamma-aminobutyric acid receptor subunit alpha-3;Gamma-aminobutyric acid receptor subunit alpha-4;Gamma-aminobutyric acid receptor subunit alpha-5;Gamma-amin
|
| 药物类型 |
Small Molecule
|
| 研发阶段 |
Withdrawn
|
| 药物描述 |
Metharbital was patented in 1905 by Emil Fischer working for Merck. It was marketed as Gemonil by Abbott Laboratories. It is a barbiturate anticonvulsant, used in the treatment of epilepsy. It has similar properties to phenobarbital [Wikipedia].
|
| 结构式 |
 |
| 药物别名 |
Metarbital;Metharbital;Metharbitalum
|
| 治疗类别 |
Anticholinergic Agents;Anticonvulsants;Barbiturates and Derivatives;Central Nervous System Depressants;Nervous System;Nicotinic Antagonists;Pyrimidines;Pyrimidinones
|
| UNII号 |
02OS7K758T
|
| CAS号 |
50-11-3
|
| 分子量 |
198.2191
|
| 分子式 |
C9H14N2O3
|
| 适应症 |
Metharbital is used for the treatment of epilepsy.
|
| 药效学 |
Metharbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
|
| 作用机制 |
Metharbital binds at a distinct binding site associated with a Cl ionopore at the GABA 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.
|
| 毒理 |
Signs of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
|
| ATC代码 |
N03AA30
|
