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首页> 外文期刊>Life sciences >Tramadol reduces the 5-HTP-induced head-twitch response in mice via the activation of mu and kappa opioid receptors.
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Tramadol reduces the 5-HTP-induced head-twitch response in mice via the activation of mu and kappa opioid receptors.

机译：曲马多可通过激活mu和kappa阿片受体降低小鼠5-HTP诱导的头跳反应。

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摘要

Tramadol, an atypical opioid analgesic, stimulates both opiatergic and serotonergic systems. Here we have investigated the effect of tramadol in mice on 5-hydroxyptrytophan (5-HTP)-induced head twitch response (HTR), which is an animal model for the activation of the CNS 5-HT(2A) receptors in mice. Tramadol attenuated 5-HTP-induced HTR in a dose-dependent manner as morphine. Furthermore, the nonselective opioid receptor antagonists, naloxone and diprenorphine (M5050), reversed the effect of tramadol on 5-HTP-induced HTR dose-dependently. Interestingly, in contrast to the selective delta opioid receptor antagonist NTI, beta-FNA, a selective mu receptor antagonist, and nor-BNI, a selective kappa opioid receptor antagonist, antagonized the attenuation of 5-HTP-induced HTR by tramadol. In conclusion, administration of tramadol systemically inhibits 5-HTP-induced HTR in mice by activating opiatergic system in the CNS. Our findings show that mu and kappa opioid receptors, but not delta opioid receptor, play an important role in the regulation of serotonergic function in the CNS.
机译：曲马多是一种非典型的阿片类镇痛药，可刺激鸦片和5-羟色胺系统。在这里，我们研究了曲马多对小鼠5-羟色氨酸（5-HTP）诱导的头抽搐反应（HTR）的影响，后者是激活小鼠中枢神经系统5-HT（2A）受体的动物模型。曲马多作为吗啡以剂量依赖性方式减弱5-HTP诱导的HTR。此外，非选择性阿片受体拮抗剂纳洛酮和二肾上腺素（M5050）逆转了曲马多对5-HTP诱导的HTR的剂量依赖性作用。有趣的是，与选择性δ阿片受体拮抗剂NTI相反，β-FNA（选择性mu受体拮抗剂）和nor-BNI（选择性κ阿片受体拮抗剂）拮抗了曲马多对5-HTP诱导的HTR的抑制作用。总之，曲马多的给药通过激活中枢神经系统的鸦片剂能系统性地抑制小鼠的5-HTP诱导的HTR。我们的发现表明，μ和κ阿片受体而不是δ阿片受体在CNS的血清素能功能调节中起重要作用。

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