A human neuroblastoma cell line expresses mu and delta opioid receptor sites.
A human neuroblastoma cell line expresses mu and delta opioid receptor sites.
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发表时间：
1986-01
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通讯作者：
V. Yu;M. Richards;W. Sadee
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作者：
V. Yu;M. Richards;W. Sadee
用示踪剂[~3H]双丙诺啡(u、β、kappa配体)和[~H]纳洛酮(u-选择性配体)筛选一系列神经母细胞瘤细胞系中阿片受体的存在。一种人神经母细胞瘤细胞系SK-N-SH对这两种示踪剂显示出强烈的结合。用多种示踪剂进行的结合实验表明，同时存在Mu和Delta位点。这些部位具有立体专一性、可饱和性和蛋白质性质。饱和结合实验估计为50,000亩和10,000个增量位点/细胞。氯化钠(100 MM)和鸟嘌呤核苷酸，鸟氨酰亚胺二磷酸(50微米)，减少阿片激动剂，但不拮抗剂结合到这些位置。依托啡在1 nM时抑制前列腺素E_1刺激的环磷酸腺苷的产生约20%，这可被纳洛酮逆转。SK-N-SH细胞上的阿片结合位点与先前报道的人脑和啮齿动物脑内的Mu和Delta位点非常相似。因此，SK-N-SH神经母细胞瘤细胞系是研究阿片受体分子功能的有用工具。
A series of neuroblastoma cell lines were screened for the presence of opioid receptor sites with the tracers [3H]diprenorphine (mu, delta, kappa ligand) and [3H]naloxone (mu-selective ligand). One human neuroblastoma cell line, SK-N-SH, displayed avid binding for both tracers. Binding experiments with multiple tracers revealed the presence of both mu and delta sites. These sites were stereospecific, saturable, and proteinaceous in character. Saturation binding experiments provided an estimate of 50,000 mu and 10,000 delta sites/cell. NaCl (100 mM) and guanine nucleotide, guanylyl imidodiphosphate (50 microM), reduced opioid agonist but not antagonist binding to these sites. Etorphine at 1 nM inhibited prostaglandin E1-stimulated cyclic AMP production by approximately 20%, which was reversible by naloxone. The opioid-binding sites on SK-N-SH cells closely resemble the previously reported mu and delta sites in human and rodent brain. Therefore, the SK-N-SH neuroblastoma cell line represents a useful tool to study the molecular functions of opioid receptors.