Garzón J, Castro M A, Juarros J L, Sánchez-Blázquez P
Instituto Cajal, C.S.I.C., Madrid, Spain.
Life Sci. 1994;54(11):PL191-6. doi: 10.1016/0024-3205(94)90167-8.
A polyclonal antiserum directed against the first 16 amino acids of the N-terminal sequence of the murine delta opioid receptor was raised in rabbits. The intracerebroventricular (i.c.v.) injection to mice of the anti delta receptor IgGs impaired the antinociception produced by DPDPE, [D-Ala2]-Deltorphin II, DADLE and beta-endorphin-(1-31) when studied 24 h later in the tail-flick test. Antinociception produced by morphine and DAMGO was fully expressed in mice undergoing this treatment. The selective delta antagonist ICI 174864 (0.8 nmols/mouse, i.c.v.) significantly reduced the antinociceptive activity of opioids to the extent observed after giving the antibodies. ICI 174864 did not decrease further the antinociception that remained after the anti delta receptor serum. The specific binding displayed by 3 nM [3H]-DPDPE was reduced in membranes pre-incubated with the antiserum, whereas no change could be detected for 0.6 nM [3H]-DAMGO labelling mu receptors. This experimental approach revealed the delta component of opioid-evoked supraspinal antinociception in mice.
针对小鼠δ阿片受体N端序列前16个氨基酸制备了多克隆抗血清。给兔子注射该抗血清后获取抗δ受体IgG，将其脑室内（i.c.v.）注射到小鼠体内，24小时后在甩尾试验中研究发现，这会损害由DPDPE、[D - Ala2]-Deltorphin II、DADLE和β-内啡肽-（1 - 31）产生的镇痛作用。吗啡和DAMGO产生的镇痛作用在接受该处理的小鼠中能充分表现出来。选择性δ拮抗剂ICI 174864（0.8 nmol/小鼠，i.c.v.）显著降低了阿片类药物的镇痛活性，其程度与给予抗体后观察到的相似。ICI 174864并未进一步降低抗δ受体血清处理后仍残留的镇痛作用。用抗血清预孵育的膜中，3 nM [3H]-DPDPE显示的特异性结合减少，而0.6 nM [3H]-DAMGO标记μ受体未检测到变化。该实验方法揭示了小鼠中阿片类药物诱发的脊髓上镇痛作用中的δ成分。
