Jacob J, Michaud G, Nicola M A, Prudhomme N
Life Sci. 1983;33 Suppl 1:645-8. doi: 10.1016/0024-3205(83)90585-4.
The pattern of [3H]Nx and [3H]EKC binding by brain homogenates was different for each of the three studied strains of mice. CXBH was rich in [3H]Nx and relatively poor in [3H]EKC sites; CXBK poor in the two sites; C3H rich in the two sites (especially [3H]EKC). Using two antinociceptive tests (hot plate: paw lick and D'Amour and Smith's; tail flick) the activities of morphine paralleled the number of [3H]Nx sites (CXBH greater than C3H much greater than CXBK) indicating that the number of mu sites is one of the genetic factors of the amplitude of the response to Mo. The same was true for the activities of EKC when the hot plate test was used (C3H much greater than CXBH congruent to CXBK) an observation which favours the view of an involvement of kappa sites in the regulation of the paw lick reaction. However, when the tail flick test was used, C3H still remained much more reactive to EKC than CXBK but CXBH were unexpectedly also very reactive; we tentatively suggest that EKC might then be acting through mu like sites. In this hypothesis mu and kappa sites would be involved in the regulation of paw lick but essentially a mu type site in that of tail flick. Further experimental evidence is needed.
在所研究的三种小鼠品系中，脑匀浆对[3H]Nx和[3H]EKC的结合模式各不相同。CXBH富含[3H]Nx，而[3H]EKC位点相对较少；CXBK在这两个位点都较少；C3H在这两个位点都很丰富（尤其是[3H]EKC）。使用两种抗伤害感受测试（热板法：舔爪和达莫尔与史密斯法；甩尾法），吗啡的活性与[3H]Nx位点的数量平行（CXBH > C3H >> CXBK），这表明μ位点的数量是对吗啡反应幅度的遗传因素之一。当使用热板测试时，EKC的活性也是如此（C3H >> CXBH ≈ CXBK），这一观察结果支持κ位点参与舔爪反应调节的观点。然而，当使用甩尾测试时，C3H对EKC的反应仍然比CXBK强烈得多，但CXBH出乎意料地也非常敏感；我们初步认为，此时EKC可能是通过类μ位点起作用。在这个假设中，μ和κ位点参与舔爪的调节，但在甩尾调节中基本上是μ型位点。还需要进一步的实验证据。
