Silva I, Cortes H, Escartín E, Rangel C, Florán L, Erlij D, Aceves J, Florán B
Departamento de Fisiología, Biofísica y Neurociencias del CINVESTAV, México, México.
J Neural Transm (Vienna). 2006 Dec;113(12):1847-53. doi: 10.1007/s00702-006-0493-7. Epub 2006 Jun 1.
The effect of L-DOPA on [(3)H]GABA release in slices of globus pallidus from 6-OHDA-lesioned rats was studied. Release was evoked by high (15 mM) K(+). The lesion reduced dopamine content and dopamine synthesized from L-DOPA. The inhibition of DOPA decarboxylase blocked dopamine synthesis. Endogenous dopamine released by high K(+) inhibited [(3)H]GABA release in normal but not in lesioned slices. L-DOPA inhibited (IC(50) = 0.44 microM) evoked [(3)H]GABA release. The inhibition was via D2-like receptors but not mediated by dopamine. The turning behavior induced by L-DOPA methyl ester (25 mg/kg, i.p.) was not abolished by the DOPA decarboxylase inhibitor 3-hydroxybenzylhydrazine but in this condition it was abolished by sulpiride. Results suggest that L-DOPA acting as D2-like agonist inhibits GABA release in the rat globus pallidus and induces turning behavior in rats with unilateral lesions of the dopamine innervation. L-DOPA could control Parkinson's disease symptoms acting not only as dopamine precursor but also by itself.
研究了左旋多巴(L-DOPA)对6-羟基多巴胺(6-OHDA)损伤大鼠苍白球切片中[³H]γ-氨基丁酸(GABA)释放的影响。通过高浓度(15 mM)钾离子(K⁺)诱发释放。损伤降低了多巴胺含量以及由L-DOPA合成的多巴胺。多巴脱羧酶的抑制作用阻断了多巴胺的合成。高钾离子释放的内源性多巴胺抑制正常切片而非损伤切片中的[³H]GABA释放。L-DOPA抑制(半数抑制浓度(IC₅₀) = 0.44 μM)诱发的[³H]GABA释放。这种抑制作用是通过D2样受体介导,但不是由多巴胺介导。L-DOPA甲酯(25 mg/kg,腹腔注射)诱导的旋转行为不会被多巴脱羧酶抑制剂3-羟基苄基肼消除,但在这种情况下会被舒必利消除。结果表明,L-DOPA作为D2样激动剂抑制大鼠苍白球中的GABA释放,并在多巴胺神经支配单侧损伤的大鼠中诱导旋转行为。L-DOPA不仅作为多巴胺前体,而且自身也可控制帕金森病症状。