Werz M A, Macdonald R L
J Pharmacol Exp Ther. 1985 Jul;234(1):49-56.
Opioid peptides decrease somatic calcium-dependent action potential duration of a subpopulation of mouse dorsal root ganglion (DRG) neurons grown in dissociated cell culture. Based on rank order of potency and naloxone sensitivity, both mu and delta opioid receptors were demonstrated on the somata of DRG neurons and were shown to have a heterogeneous distribution. The purpose of the present investigation was to determine the actions of dynorphin gene products, dynorphin A, dynorphin B, dynorphin A(1-8), dynorphin A(1-9), alpha-neoendorphin and beta-neoendorphin on DRG neuron somatic calcium-dependent action potentials and to compare the actions of dynorphin and neoendorphin peptides to the action of morphiceptin, a mu receptor-selective ligand, and Leu-enkephalin, a delta receptor-preferring ligand. We report that the dynorphin and neoendorphin peptides decreased DRG neuron somatic calcium-dependent action potential duration in a portion of DRG neurons, an action that was dose-dependent and was antagonized by naloxone. DRG neuron responses to the dynorphins and neoendorphins differed from responses to morphiceptin and Leu-enkephalin. First, many DRG neurons responded to dynorphin A but not to morphiceptin or Leu-enkephalin. Second, dynorphin A responses, unlike responses to morphiceptin or Leu-enkephalin, were present after intracellular injection of cesium, a potassium channel blocker. Dynorphin A effectiveness was decreased after deletions at the carboxy-terminus and Leu-enkephalin [dynorphin A(1-5)] was inactive at 10 microM. Thus, on DRG neurons in cell culture, dynorphins and neoendorphins act at opioid receptors distinct from mu and delta receptors, possibly kappa receptors.(ABSTRACT TRUNCATED AT 250 WORDS)
阿片肽可缩短在解离细胞培养中生长的小鼠背根神经节(DRG)神经元亚群的体细胞钙依赖性动作电位持续时间。根据效力等级顺序和纳洛酮敏感性,在DRG神经元的胞体上证实了μ和δ阿片受体,且显示其分布不均一。本研究的目的是确定强啡肽基因产物强啡肽A、强啡肽B、强啡肽A(1-8)、强啡肽A(1-9)、α-新内啡肽和β-新内啡肽对DRG神经元体细胞钙依赖性动作电位的作用,并将强啡肽和新内啡肽肽的作用与μ受体选择性配体吗啡肽和δ受体偏好性配体亮氨酸脑啡肽的作用进行比较。我们报告称,强啡肽和新内啡肽肽在一部分DRG神经元中缩短了体细胞钙依赖性动作电位持续时间,这一作用呈剂量依赖性且被纳洛酮拮抗。DRG神经元对强啡肽和新内啡肽的反应不同于对吗啡肽和亮氨酸脑啡肽的反应。首先,许多DRG神经元对强啡肽A有反应,但对吗啡肽或亮氨酸脑啡肽无反应。其次,与对吗啡肽或亮氨酸脑啡肽的反应不同,在细胞内注射钾通道阻滞剂铯后仍存在强啡肽A反应。强啡肽A在羧基末端缺失后效力降低,且亮氨酸脑啡肽[强啡肽A(1-5)]在10微摩尔时无活性。因此,在细胞培养中的DRG神经元上,强啡肽和新内啡肽作用于不同于μ和δ受体的阿片受体,可能是κ受体。(摘要截短于250字)