Garzón J, Martínez-Peña Y, Sánchez-Blázquez P
Instituto Cajal, C.S.I.C., Madrid, Spain.
Life Sci. 1994;55(11):PL205-12. doi: 10.1016/0024-3205(94)90048-5.
Intracerebroventricular (i.c.v.) administration to mice of IgGs raised against alpha subunits of Gi2 or Gx/z transducer proteins lessened the activation of low Km GTPase induced by morphine, DAMGO and DADLE in P2 membranes from mouse periaqueductal grey matter (PAG). In mice injected with anti Gi2 alpha, DADLE, DPDPE and [D-Ala2] Deltorphin II, but not beta-endorphin-(1-31), antagonized the analgesic activity of morphine. Conversely, following anti Gx/z alpha, morphine antagonized the antinociceptive potency of DADLE. It is concluded that opioids display diverse efficacy at mu-Gi2 and mu-Gx/z complexes to produce supraspinal analgesia in mice.
给小鼠脑室内注射针对Gi2或Gx/z转导蛋白α亚基产生的IgG,可减弱吗啡、DAMGO和DADLE在小鼠导水管周围灰质(PAG)P2膜中诱导的低Km GTP酶的激活。在注射抗Gi2α的小鼠中,DADLE、DPDPE和[D-Ala2]强啡肽II可拮抗吗啡的镇痛活性,但β-内啡肽-(1-31)则不能。相反,注射抗Gx/zα后,吗啡可拮抗DADLE的抗伤害感受作用。得出的结论是,阿片类药物在μ-Gi2和μ-Gx/z复合物上表现出不同的效力,从而在小鼠中产生脊髓上镇痛作用。