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目的:比较左旋千金藤立定((-)-stepholidine,(-)-SPD)和12-氯斯阔任(12-chloroscoulerine,CSL)对黑质(substantia nigra,SN)多巴胺(DA)神经元放电的影响。方法:麻痹大鼠上的胞外单单位记录。结果:在大鼠,(-)-SPD,(-)-,(±)-和(+)-CSL减弱iv 10μg·kg~(-1)阿朴吗啡引起的放电抑制。ED_(50)值分别为15.1(11.9—19.4),7.8(7.0—8.7),12.6(2.0—17.9)μg·kg~(-1)和2.9(2.6—3.3)mg·kg~(-1)。(-)-CSL比(-)-SPD强1倍,比(+)-CSL强371倍。在利血平化大鼠,(-)-SPD,(-)-,(±)-,和(+)-CSL减弱4mg·kg~(-1)SKF-38393引起的放电抑制。ED_(50)值为0.53(0.51—0.55),0.51(0.43—0.60),1.2(0.7—2.0)和5.9(4.9—7.1)mg·kg~(-1)。(-)-CSL的强度与(-)-SPD相似,比(+)-CSL强11倍。结论:(-)-SPD和CSL是D_1/D_2混合性阻滞剂。(-)-CSL最强,(+)-CSL最弱。
OBJECTIVE: To compare the substantia nigra (SN) dopamine (DA) neuronal discharges with 12-chloroscoulerine (CSL) and levascaline (SPSD) Impact. Methods: Extracellular single unit recordings on paralyzed rats. RESULTS: In rats, (-) - SPD, (-) -, (±) - and (+) - CSL attenuated the discharge inhibition induced by 10 μg · kg -1 apomorphine. ED 50 values were 15.1 (11.9-19.4), 7.8 (7.0-8.7), 12.6 (2.0-17.9) μg · kg -1 and 2.9 (2.6-3.3) mg · kg -1, respectively. . (-) - CSL is 1 time stronger than (-) - SPD and 371 times stronger than (+) - CSL. In reserpinetized rats, (-) - SPD, (-) -, (±) -, and (+) - CSL attenuated the discharge inhibition induced by 4 mg · kg -1 SKF-38393. The values of ED_ (50) were 0.53 (0.51-0.55), 0.51 (0.43-0.60), 1.2 (0.7-2.0) and 5.9 (4.9-7.1) mg · kg -1, respectively. (-) - The intensity of CSL is similar to (-) - SPD, 11-fold stronger than (+) - CSL. Conclusion: (-) - SPD and CSL are D_1 / D_2 mixed blockers. (-) - CSL strongest, (+) - CSL weakest.