Differential involvement of mu-opioid receptor subtypes in endomorphin-1- and -2-induced antinociception.
Differential involvement of mu-opioid receptor subtypes in endomorphin-1- and -2-induced antinociception.
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DOI：
10.1016/s0014-2999(99)00181-8
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发表时间：
1999-05
影响因子：
5
通讯作者：
S. Sakurada;J. Zadina;A. Kastin;S. Katsuyama;Tsutomu Fujimura;Kimie Murayama;Masayuki Yuki;Hiroshi Ueda;T. Sakurada
中科院分区：
文献类型：
--
作者：
S. Sakurada;J. Zadina;A. Kastin;S. Katsuyama;Tsutomu Fujimura;Kimie Murayama;Masayuki Yuki;Hiroshi Ueda;T. Sakurada
本研究采用脊髓上介导的行为学方法，研究μ阿片受体亚型在内吗啡肽-1和内吗啡肽-2诱导的小鼠抗伤害感受中的作用。尾压作为机械伤害性刺激，脑室内（i. c. v.）和鞘内（i.t.）注射的内吗啡肽产生有效和显著的抗伤害感受活性。i.t.诱导的抗伤害感受。i. c. v.注射内吗啡肽-1不能被选择性μ1-阿片受体拮抗剂纳洛嗪（35 mg/kg，s.c.）预处理所逆转。相比之下，i.t.μ1-阿片受体拮抗剂可显著降低i. c. v.内吗啡肽-2（endomorphin-2）。两种i.t. i. c. v.内吗啡肽-1和-2可被β-funaleuramine（40 mg/kg，s.c.）预处理完全逆转。结果提示内吗啡肽可能通过μ阿片受体的μ 1和μ 2亚型产生抗伤害作用。
We investigated the role of μ-opioid receptor subtypes in both endomorphin-1 and endomorphin-2 induced antinociception in mice using supraspinally mediated behavior. With tail pressure as a mechanical noxious stimulus, both intracerebroventricularly (i.c.v.) and intrathecally (i.t.) injected-endomorphins produced potent and significant antinociceptive activity. Antinociception induced by i.t. and i.c.v. injection of endomorphin-1 was not reversed by pretreatment with a selective μ1-opioid receptor antagonist, naloxonazine (35 mg/kg, s.c.). By contrast, antinociception induced by i.t. and i.c.v. endomorphin-2 was significantly decreased by μ1-opioid receptor antagonist. Antinociception of both i.t. and i.c.v. endomorphin-1 and -2 was completely reversed by pretreatment with β-funaltrexamine (40 mg/kg, s.c.). The results indicate that endomorphins may produce antinociception through the distinct μ1and μ2subtypes of μ-opioid receptor.