Ross D H, Lynn S C, Jones D J
Proc West Pharmacol Soc. 1976;19:66-70.
Tolerance to morphine proceeds with an adaptation in the nerve membrane causing an increase in endogenously bound calcium. Our data on calcium binding is compatible with Collier's hypothesis (10) for drug induced changes in number and/or types of receptors. The results demonstrating naloxone reversal of this membrane adaptation suggest that opiate antagonist action may be to maintain the opiate macromolecule portion of the membrane in a Ca++ associated homeostatic state. Lack of effects of Na+ on opiate treated SPM suggest that cellular adaptation to morphine proceeds in vivo through a change in membrane binding of calcium.
对吗啡的耐受性伴随着神经膜的适应性变化,导致内源性结合钙增加。我们关于钙结合的数据与科利尔关于药物诱导受体数量和/或类型变化的假说(10)相符。表明纳洛酮可逆转这种膜适应性变化的结果提示,阿片拮抗剂的作用可能是使膜的阿片大分子部分维持在与钙离子相关的稳态。钠离子对经阿片处理的突触小体膜无影响,这表明细胞对吗啡的适应性变化在体内是通过钙的膜结合变化来实现的。