首页> 外文期刊>Life sciences >Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.
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Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.

机译:口服氟哌啶醇,利培酮和奥氮平后大鼠脑神经递质受体的结合特征。

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摘要

The present study was conducted to characterize the binding of neurotransmitter receptors (dopamine D(2), serotonin 5-HT(2), histamine H(1), adrenaline alpha(1) and muscarine M(l) receptors) in the rat's brain after the oral administration of haloperidol, risperidone, and olanzapine. Haloperidol at 1 and 3 mg/kg displayed significant activity to bind the D(2) receptor (increase in the Kd value for [(3)H]raclopride binding) in the corpus striatum with little change in the activity toward the 5-HT(2) receptor (binding parameters for [(3)H]ketanserin). In contrast, risperidone (0.1-3 mg/kg) showed roughly 30 times more affinity for the 5-HT(2) receptor than D(2) receptor. Also, olanzapine (1-10 mg/kg) was most active toward the H(1) receptor in the cerebral cortex, corpus striatum, and hippocampus, was less active in binding 5-HT(2) and D(2) receptors, and showed the least affinity for alpha(1) and M(1) receptors. In conclusion, haloperidol and risperidone administered orally selectively bind D(2) and 5-HT(2) receptors, respectively, in the rat brain, while olanzapine binds H(1), 5-HT(2), and D(2) receptors more than alpha(1) and M(1) receptors.
机译:进行本研究以表征大鼠大脑中神经递质受体(多巴胺D(2),5-羟色胺5-HT(2),组胺H(1),肾上腺素α(1)和毒蕈碱M(l)受体)的结合情况口服氟哌啶醇,利培酮和奥氮平后。氟哌啶醇在1和3 mg / kg时显示在纹状体中结合D(2)受体的显着活性([(3)H] raclopride结合的Kd值增加),而对5-HT的活性变化很小(2)受体([(3)H] ketanserin的结合参数)。相反,利培酮(0.1-3 mg / kg)对5-HT(2)受体的亲和力比D(2)受体高出约30倍。此外,奥氮平(1-10 mg / kg)对大脑皮层,纹状体和海马中的H(1)受体活性最高,对结合5-HT(2)和D(2)受体的活性较低,并显示出对alpha(1)和M(1)受体的亲和力最低。总之,口服氟哌啶醇和利培酮分别选择性地在大鼠脑中结合D(2)和5-HT(2)受体,而奥氮平结合H(1),5-HT(2)和D(2)受体比alpha(1)和M(1)受体更多。

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