Tallman J F, Paul S M, Skolnick P, Gallager D W
Science. 1980 Jan 18;207(4428):274-81. doi: 10.1126/science.6101294.
Investigation of the actions of the benzodiazepines has provided insights into the neurochemical mechanisms underlying anxiety, seizures, muscle relaxation, and sedation. Behavioral, electrophysical, pharmacological, and biochemical evidence indicates that the benzodiazepines exert their therapeutic effects by interacting with a high-affinity binding site (receptor) in the brain. The benzodiazepine receptor interacts with a receptor for gamma-aminobutyric acid, a major inhibitory neurotransmitter, and enhances its inhibitory effects. The benzodiazepine receptor may also interact with endogenous substances and several naturally occurring compounds, including the purines and nicotinamide, are candidates for this role. Both the purines and nicotinamide possess some benzodiazepine-like properties in vivo, although further work will be required to confirm their possible roles as endogenous benzodiazepines.
对苯二氮䓬类药物作用的研究为焦虑、癫痫、肌肉松弛和镇静背后的神经化学机制提供了见解。行为学、电生理学、药理学和生物化学证据表明,苯二氮䓬类药物通过与大脑中的高亲和力结合位点(受体)相互作用发挥其治疗作用。苯二氮䓬受体与γ-氨基丁酸(一种主要的抑制性神经递质)的受体相互作用,并增强其抑制作用。苯二氮䓬受体也可能与内源性物质相互作用,几种天然存在的化合物,包括嘌呤和烟酰胺,是这一作用的候选物质。嘌呤和烟酰胺在体内都具有一些苯二氮䓬样特性,尽管还需要进一步的研究来证实它们作为内源性苯二氮䓬的可能作用。