Hu J Y, Jin G Z
Department of Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1999 Aug;20(8):715-9.
To study the role of dopamine (DA) receptors in l-tetrahydropalmatine (l-THP)-induced antinociception.
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.
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.
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.
研究多巴胺(DA)受体在左旋四氢巴马汀(l-THP)诱导的镇痛作用中的作用。
采用腹腔注射(i.p.)和鞘内注射(ith)给药。用甩尾试验评估大鼠的痛阈。
腹腔注射时,l-THP(10、20、40mg·kg-1)以及D2受体拮抗剂螺哌隆(1、2、3mg·kg-1)对大鼠的疼痛产生剂量依赖性镇痛作用,而D2受体激动剂喹吡罗、D1受体激动剂SKF38393和D1受体拮抗剂Sch-23390未表现出镇痛作用。此外,喹吡罗(2、3mg·kg-1)可显著减弱l-THP或螺哌隆诱导的镇痛作用,但SKF38393或纳洛酮无此作用。另一方面,鞘内注射喹吡罗(20、30、40μg·kg-1)也诱导剂量依赖性镇痛作用,而鞘内注射l-THP、螺哌隆、SKF38393和Sch-23390未表现出任何镇痛作用。此外,鞘内注射螺哌隆(20、30、40μg·kg-1)而非Sch-23390剂量依赖性地拮抗喹吡罗诱导的镇痛作用。l-THP(鞘内注射,100、200、300μg·kg-1)也以剂量依赖关系显著减弱喹吡罗诱导的镇痛作用。
激活脊髓D2受体或阻断脊髓上D2受体可产生镇痛作用。D1受体可能不直接参与镇痛作用。l-THP(作为D2拮抗剂)以及螺哌隆通过阻断脊髓上D2受体产生镇痛作用。