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本文以[~3H]-spiperone为配基,证实ι-THP与脑内DA受体有亲和力(K_i=0.2μM),而d-THP无亲和力(K_i>0.1mM)。小剂量ι-THP(2.5—10mg/kg)能增加尾核内TH酶活力,加速ι-dopa生物合成,又能拮抗去水吗啡抑制ι-dopa的生物合成,表明它们在突触前DA受体水平相拮抗;大剂量d-THP(100mg/kg)略能增强TH酶活力,增加ι-dopa的含量,但ι-THP比它强20—50倍,并且此作用不可能由于d-THP阻滞DA受体所引起。应用DPV法和荧光测定法,证实小剂量ι-THP能使尾核内DOPAC和HVA增加数倍。上述资料均表明ι-THP是DA受体拮抗剂。d-THP(25mg/kg)明显减少DA含量,增为100mg/kg时,D减少80％。大剂量的d-THP能使脑内5-HT和NA约减少20％,仅为DA影响的1/4。所以,d-THP较专一地降低DA含量。大剂量的ι-THP对脑内5-HT和NA的含量无明显影响,虽稍减DA含量,可能由于阻滞突触前DA受体,反馈性增强释放DA的缘故。
In this paper, [~3H]-spiperone was used as a ligand to verify that I-THP has affinity with DA receptor in the brain (K_i = 0.2μM), while d-THP has no affinity (K_i> 0.1mM). Small doses of TT-THP (2.5–10 mg/kg) increase the activity of TH enzyme in the caudate nucleus, accelerate the biosynthesis of ι-dopa, and antagonize the dehydromorphine morphine to inhibit the biosynthesis of ι-dopa, indicating that they are affected by presynaptic DA. Antagonism at body level; large doses of d-THP (100 mg/kg) slightly enhances the activity of TH enzyme and increases the content of i-dopa, but i-THP is 20-50 times stronger than it, and this effect cannot be due to d-THP. Blocked by DA receptors. Using the DPV method and fluorescence assay, it was confirmed that small doses of ι-THP can increase DOPAC and HVA in the tail nucleus several times. The above data show that ι-THP is a DA receptor antagonist. d-THP (25mg/kg) significantly reduced the DA content, and increased to 100mg/kg, D decreased by 80%. High-dose of d-THP can reduce brain 5-HT and NA by about 20%, only 1/4 of DA effects. Therefore, d-THP specifically lowers the DA content. High-dose ι-THP had no significant effect on the content of 5-HT and NA in brain. Although the DA content was slightly decreased, it may be due to the blockade of presynaptic DA receptors and feedback enhanced release of DA.