Supraspinal D2 receptor involved in antinociception induced by l-tetrahydropalmatine.

J Y Hu, G Z Jin
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Abstract

Aim: To study the role of dopamine (DA) receptors in l-tetrahydropalmatine (l-THP)-induced antinociception.

Methods: The intraperitoneal (i.p.) and intrathecal (ith) injections were used to give the drugs. The tail-flick test was used to assess the nociceptive threshold of rats.

Results: By i.p. injection, l-THP (10, 20, 40 mg.kg-1) as well as D2 receptor antagonist spiperone (1, 2, 3 mg.kg-1) produced dose-dependent antinociceptive effects on the nociception of rats, while D2 receptor agonist quinpirole, D1 receptor agonist SKF38393, and D1 receptor antagonist Sch-23390 showed no antinociception. Moreover, l-THP- or spiperone-induced antinociception was markedly attenuated by quinpirole (2, 3 mg.kg-1) but not SKF38393 or naloxone. On the other hand, ith quinpirole (20, 30, 40 micrograms.kg-1) also induced a dose-dependent antinociception, while ith l-THP, spiperone, SKF38393, and Sch-23390 did not exhibit any antinociception. Furthermore, ith spiperone (20, 30, 40 micrograms.kg-1) but not Sch-23390 dose-dependently antagonised the antinociception induced by quinpirole. l-THP (ith, 100, 200, 300 micrograms.kg-1) also dramatically attenuated the quinpirole-induced antinociception with a dose-dependent relationship.

Conclusion: Activating the spinal D2 receptor or blocking the supraspinal D2 receptor produces antinociception. D1 receptor might be not directly involved in the antinociception. l-THP (as a D2 antagonist) as well as spiperone produces antinociception via blocking the supraspinal D2 receptor.

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脊髓上D2受体参与l-四氢巴马汀诱导的抗痛觉作用。
目的:研究多巴胺(DA)受体在l-四氢巴马汀(l-THP)诱导的抗痛觉作用。方法:采用腹腔注射和鞘内注射两种方法给药。采用甩尾试验评估大鼠的伤害阈值。结果:通过腹腔注射,l-THP(10、20、40 mg.kg-1)和D2受体拮抗剂spiperone(1、2、3 mg.kg-1)对大鼠的伤害感受产生剂量依赖性的抗伤害感受作用,而D2受体激动剂quinpirole、D1受体激动剂SKF38393和D1受体拮抗剂sch23390对大鼠的伤害感受无抑制作用。此外,喹匹罗(2,3 mg.kg-1)明显减弱l-THP-或spiperone诱导的抗痛感,而SKF38393或纳洛酮则没有。另一方面,使用喹匹罗(20,30,40微克。kg-1)也诱导了剂量依赖性的抗伤性,而使用l-THP, spiperone, SKF38393和Sch-23390没有表现出任何抗伤性。此外,spiperone(20,30,40微克。kg-1)而不是Sch-23390可以剂量依赖性地拮抗喹匹罗诱导的抗痛反应。l-THP(分别为100、200、300 μ g .kg-1)也能显著减弱喹匹罗诱导的抗避孕作用,且呈剂量依赖关系。结论:激活脊髓D2受体或阻断棘上D2受体可产生抗感觉。D1受体可能不直接参与抗感觉作用。l-THP(作为D2拮抗剂)和spiperone通过阻断棘上D2受体产生抗感觉。
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