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The cannabinoid CB1 receptor antagonist SR141716A selectively facilitates nociceptive responses of dorsal horn neurones in the rat

机译:大麻素CB1受体拮抗剂SR141716A可选择性促进大鼠背角神经元的伤害性反应

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摘要

The effect of spinal administration of the selective cannabinoid CB1 receptor antagonist, SR141716A, and the selective CB2 receptor antagonist, SR144528, on innocuous versus noxious evoked responses of dorsal horn neurones in the spinal cord of the anaesthetized rat was investigated. SR141716A (0.001–1 ng 50 μl−1) dose-relatedly facilitated the non-potentiated component of the electrical C-fibre mediated neuronal response (120±6, 156±13, 192±33 and 192±31% of control respectively; n=6). In contrast, SR144528 (0.001–1 ng 50 μl−1) did not influence the non-potentiated component of the C-fibre evoked neuronal response (n=5). The electrical evoked Aβ-fibre mediated neuronal responses were not influenced by SR141716A or SR144528. The results of this study provide evidence that tonic cannabinoid CB1 receptor activation, but not CB2 receptor activation, attenuates acute nociceptive transmission, at the level of the spinal cord. These results suggest a selective antinociceptive role of the endogenous cannabinoids at spinal CB1 receptors.
机译:研究了选择性大麻素CB1受体拮抗剂SR141716A和选择性CB2受体拮抗剂SR144528的脊髓给药对麻醉大鼠脊髓背角神经元的无毒和有害诱发反应的影响。 SR141716A(0.001–1 ng 50μl −1 )剂量相关地促进了C纤维介导的神经元反应的非增强成分(120±6、156±13、192±33和192)分别为对照的±31%; n = 6)。相反,SR144528(0.001–1 ng 50μl -1 )不会影响C纤维诱发的神经元反应的非增强成分(n = 5)。电诱发的Aβ-纤维介导的神经元反应不受SR141716A或SR144528的影响。这项研究的结果提供了证据,表明进补大麻素CB1受体激活而不是CB2受体激活在脊髓水平上减弱了急性伤害性传递。这些结果表明内源性大麻素对脊髓CB1受体具有选择性的镇痛作用。

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