γ-Hydroxybutyric Acid and Its Analogs, γ-Butyrolactone and 1,4-Butanediol
γ-Hydroxybutyric Acid and Its Analogs, γ-Butyrolactone and 1,4-Butanediol
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γ-羟基丁酸及其类似物、γ-丁内酯和1,4-丁二醇
DOI：
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发表时间：
2001
期刊：
影响因子：
--
通讯作者：
L. Marinetti
中科院分区：
文献类型：
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作者：
L. Marinetti
γ-羟基丁酸（GHB）是哺乳动物中枢神经系统和外周组织中的一种内源性化合物，也是γ-氨基丁酸（GABA）的一种次要代谢物或前体，GABA是一种抑制性神经递质（图1）。它于1960年首次由Alfreit（1）及其同事合成，作为实验性GABA类似物，可能用于治疗癫痫发作。他们假设，由于GHB可以很容易地穿过血/脑屏障，也许它可以促进大脑中GABA的合成。虽然GHB没有产生GABA合成升高，但研究表明，GHB具有一些药理学特性，使其可用作麻醉剂佐剂。伽马--羟丁酸在人体中最早的药理学用途就是在这方面。Blumenfeld等人（2）列出了他们在人体麻醉中使用GHB的实验中观察到的九种品质：模仿自然睡眠，引起分钟呼吸量的可忽略的减少，具有强心作用，产生放松以便于插管，增强其它中枢神经系统（CNS）抑制剂，不改变氧消耗，允许容易地控制呼吸，提供非常稳定的生命体征，并允许缓慢的麻醉诱导。在这种情况下，Helrich等人（3）在16名成人患者中将GHB的血液浓度与意识状态相关联（表1）。
Gamma-hydroxybutyric acid (GHB) is an endogenous compound in mammalian central nervous system and peripheral tissues and a minor metabolite or precursor of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter (Fig. 1). It was first synthesized in 1960 by Laborit (1) and his associates as an experimental GABA analog for possible use in the treatment of seizure disorder. They hypothesized that since GHB could readily cross the blood/brain barrier perhaps it could facilitate the synthesis of GABA in the brain. Although GHB did not produce elevated GABA synthesis, the research revealed that GHB had some pharmacologic properties that rendered it useful as an anesthetic adjuvant. The earliest pharmacological use of GHB in humans was in this application. Blumenfeld et al. (2) listed nine qualities observed from their experiments with GHB used in human anesthesia: mimics natural sleep, causes negligible reduction in minute respiratory volume, has cardiotonic effects, produces relaxation for ease of intubation, potentiates other central nervous system (CNS) depressants, does not change oxygen consumption, permits easy control of respiration, provides very stable vital signs, and permits slow induction of anesthesia. In this context Helrich et al. (3) correlated blood concentrations of GHB with state of consciousness in 16 adult human patients (Table 1).
大鼠和人脑突触体膜中的γ-羟基丁酸结合位点。
影响因子：
5.8
作者：
Snead3rd,OC;Liu,CC
通讯作者：
Liu,CC
γ-羟基丁酸（GHB）与γ-氨基丁酸（GABA）关系的研究。
影响因子：
5.8
作者：
Snead3rd,OC;Liu,CC;Bearden,LJ
通讯作者：
Bearden,LJ
γ-羟基丁酸是一种 GABAB 受体激动剂，可增加大鼠腹侧被盖多巴胺神经元的钾电导。
DOI：
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发表时间：
1998
期刊：
The Journal of pharmacology and experimental therapeutics.
影响因子：
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作者：
Madden,TE;Johnson,SW
通讯作者：
Johnson,SW