Severi C, Grider J R, Makhlouf G M
Department of Medicine, Medical College of Virginia, Richmond 23298.
Life Sci. 1988;42(23):2373-80. doi: 10.1016/0024-3205(88)90191-9.
Smooth muscle cells were isolated from the fundus of the canine gallbladder and examined for the presence of opioid receptors. The cells contracted in a concentration-dependent manner in response to three opioid peptides (Met-enkephalin, dynorphin1-13 and Leu-enkephalin), which are known derivatives of opioid precursors present in myenteric neurons of the gut. The order of potency was Met-enkephalin greater than dynorphin1-13 greater than Leu-enkephalin. The contractile response to opioid agonists was selectively inhibited by opioid antagonists (naloxone and Mr2266) but not by muscarinic, CCK/gastrin or tachykinin antagonists. Equivalent responses to the three opioid peptides exhibited differential sensitivity to preferential antagonists of mu (naloxone) and kappa (Mr2266) opioid receptors consistent with the presence of the three main types of opioid receptors (mu, delta and kappa) on canine gallbladder muscle cells.
从犬胆囊底部分离出平滑肌细胞,并检测阿片受体的存在。这些细胞对三种阿片肽(甲硫氨酸脑啡肽、强啡肽1 - 13和亮氨酸脑啡肽)呈浓度依赖性收缩,这三种肽是肠道肌间神经元中存在的阿片前体的已知衍生物。效力顺序为甲硫氨酸脑啡肽大于强啡肽1 - 13大于亮氨酸脑啡肽。阿片激动剂的收缩反应被阿片拮抗剂(纳洛酮和Mr2266)选择性抑制,但不受毒蕈碱、胆囊收缩素/胃泌素或速激肽拮抗剂抑制。对三种阿片肽的等效反应对μ(纳洛酮)和κ(Mr2266)阿片受体的选择性拮抗剂表现出不同的敏感性,这与犬胆囊肌细胞上存在三种主要类型的阿片受体(μ、δ和κ)一致。