Kinouchi K, Maeda S, Saito K, Inoki R, Fukumitsu K, Yoshiya I
Department of Anesthesiology, Osaka University Medical School, Japan.
Res Commun Chem Pathol Pharmacol. 1989 Feb;63(2):201-13.
Effects of d- and l-pentazocine on the release and uptake of norepinephrine and other neurotransmitters were examined in rat cerebral cortex. D- and l-pentazocine (10(-6)-10(-4) M) evoked the release of tritium from rat cortex slices preloaded with [3H]norepinephrine. Both isomers of pentazocine (3 x 10(-5) M) also evoked the release of tritium from slices preloaded with [3H]dopamine and [3H]5-hydroxytryptamine ([3H]5-HT) but did not from those preloaded with [3H] gamma-aminobutyric acid ([3H]GABA) and [3H]choline. The releasing effect of pentazocine was neither dependent on the extracellular calcium nor antagonized by naloxone. Both isomers inhibited the uptake of [3H]norepinephrine, [3H]dopamine and [3H]5-HT but not that of [3H]GABA and [3H]choline into synaptosomes prepared from the cortex. These results suggest that the effects of d- and l-pentazocine on release and uptake are relatively specific to monoamines and might explain some aspects of pharmacological actions of pentazocine.
研究了右旋和左旋喷他佐辛对大鼠大脑皮层去甲肾上腺素及其他神经递质释放和摄取的影响。右旋和左旋喷他佐辛（10⁻⁶ - 10⁻⁴ M）可使预先用[³H]去甲肾上腺素标记的大鼠皮层切片释放氚。喷他佐辛的两种异构体（3×10⁻⁵ M）也可使预先用[³H]多巴胺和[³H]5-羟色胺（[³H]5-HT）标记的切片释放氚，但不能使预先用[³H]γ-氨基丁酸（[³H]GABA）和[³H]胆碱标记的切片释放氚。喷他佐辛的释放作用既不依赖细胞外钙，也不受纳洛酮拮抗。两种异构体均抑制[³H]去甲肾上腺素、[³H]多巴胺和[³H]5-HT进入从皮层制备的突触体，但不抑制[³H]GABA和[³H]胆碱的摄取。这些结果表明，右旋和左旋喷他佐辛对释放和摄取的影响对单胺类物质具有相对特异性，这可能解释了喷他佐辛药理作用的某些方面。
