The Sound of Evolution
Clorazepate
氯拉䓬酸
Mechanism of action:
Clorazepate 是一種苯二氮平類（benzodiazepine）衍生物。Clorazepate 為一種前驅藥，在腸胃道吸收後迅速被水解為其主要活性代謝物去甲西泮（nordazepam，N-desmethyldiazepam）。去甲西泮能結合於 GABA_A 受體上的苯二氮平結合位點（benzodiazepine-binding site），增強抑制性神經傳導物質 GABA 的作用，促進氯離子通道（chloride channel）開啟頻率，使氯離子進入神經元，導致膜電位超極化（hyperpolarization），減少神經元產生動作電位，降低中樞神經興奮性。
Reference(s):
1. Committee on the Review of Medicines. (1980). Systematic review of the benzodiazepines: Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Br Med J.
2. McElhatton PR et al. (1994). The effects of benzodiazepine use during pregnancy and lactation. Reprod Toxicol.
3. Ochs HR et al. (1982). Desmethyldiazepam kinetics after intravenous, intramuscular, and oral administration of clorazepate dipotassium. Klin Wochenschr.