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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Gamma butyrolactone (GBL) and gamma valerolactone (GVL): Similarities and differences in their effects on the acoustic startle reflex and the conditioned enhancement of startle in the rat
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Gamma butyrolactone (GBL) and gamma valerolactone (GVL): Similarities and differences in their effects on the acoustic startle reflex and the conditioned enhancement of startle in the rat

机译：γ丁内酯（GBL）和γ戊内酯（GVL）：它们对大鼠听觉惊吓反射和惊吓的条件增强的影响的异同

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Gamma butyrolactone (GBL) is metabolized to gamma hydroxybutyrate (GHB) in the body. GHB is a DEA Schedule 1 compound; GBL is a DEA List 1 chemical. Gamma valerolactone (GVL) is the 4-methyl analog of GBL; GVL is metabolized to 4-methyl-GHB; GVL is NOT metabolized to GBL or GHB. The effects of GBL (18.75-150 mg/kg), GVL (200-1600 mg/kg) or vehicle on the acoustic startle reflex (ASR), and the classically-conditioned enhancement of startle, the Startle Anticipated Potentiation of Startle (SAPS) response were studied in male rats. Both compounds produced a dose-dependent reduction of ASR, with GBL 5-7 times more potent than GVL. In contrast, GBL treatment significantly reduced SAPS at doses that exerted only moderate effects on ASR, whereas GVL exerted little or no effect on the SAPS, except at doses that produced pronounced reductions in Noise Alone ASR. In a second experiment, rats were tested for Noise Alone ASR behavior following treatment with a single mid-range dose of GBL (75 mg/kg), GVL (400 mg/kg) or vehicle; immediately following startle testing the animals were sacrificed and their brains and blood were collected for determination of GHB, 4-methyl-GHB, GBL and GVL. GHB was found in measurable concentrations in all of the blood specimens and 6 (of 8) of the brain specimens from the GBL-treated subjects. 4-Methyl-GHB was found in measurable concentrations in all of the blood and brain specimens of the GVL-treated subjects; the change in startle amplitude was inversely correlated to the brain concentrations of these compounds. These findings confirm the differences in the metabolic fate of GBL and GVL as pro-drugs for the formation of GHB and 4-methyl-GHB, respectively. Moreover, the dissimilarity in effect profile for GBL and GVL on ASR versus SAPS behaviors suggests that different receptor(s) may be involved in mediating these behavioral effects.
机译：γ丁内酯（GBL）在体内代谢为γ羟基丁酸酯（GHB）。 GHB是DEA附表1化合物; GBL是DEA清单1的化学品。丙戊内酯（GVL）是GBL的4-甲基类似物; GVL被代谢为4-甲基-GHB; GVL不会代谢为GBL或GHB。 GBL（18.75-150 mg / kg），GVL（200-1600 mg / kg）或赋形剂对听觉惊吓反射（ASR）和经典条件增强的惊吓，惊吓预期的惊吓增强（SAPS）的影响对雄性大鼠进行了研究。两种化合物均产生剂量依赖性的ASR降低，GBL的效力是GVL的5-7倍。相比之下，GBL处理在仅对ASR产生中度影响的剂量下可显着降低SAPS，而GVL对SAPS则几乎没有影响或无影响，除非在产生“单独噪声” ASR的作用下显着降低。在第二个实验中，对中剂量的GBL（75 mg / kg），GVL（400 mg / kg）或赋形剂进行单次治疗后，对大鼠进行了Alone Noise ASR行为测试;进行惊吓测试后，立即处死动物并收集其大脑和血液以测定GHB，4-甲基-GHB，GBL和GVL。在来自接受GBL治疗的受试者的所有血液样本和8个脑样本中，可测量的浓度都含有GHB。在接受GVL治疗的受试者的所有血液和脑部样本中，可测量的浓度都发现了4-甲基-GHB。惊吓幅度的变化与这些化合物的大脑浓度成反比。这些发现证实了GBL和GVL作为形成GHB和4-甲基-GHB的前药的代谢命运的差异。此外，GBL和GVL在ASR与SAPS行为上的作用谱上的差异表明，在这些行为作用的介导中可能涉及不同的受体。

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