阿片受体配体对大鼠纹状体神经元细胞浆钙离子浓度的激动剂选择性作用。
Agonist-selective effects of opioid receptor ligands on cytosolic calcium concentration in rat striatal neurons.
机构信息
Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA.
出版信息
Drug Alcohol Depend. 2012 Jun 1;123(1-3):277-81. doi: 10.1016/j.drugalcdep.2011.11.021. Epub 2011 Dec 21.
BACKGROUND
Buprenorphine is an opioid receptor ligand whose mechanism of action is incompletely understood.
METHODS
Using Ca(2+) imaging, we assessed the effects of buprenorphine, β-endorphin, and morphine on cytosolic Ca(2+) concentration Ca(2+), in rat striatal neurons.
RESULTS
Buprenorphine (0.01-1 μM) increased Ca(2+) in a dose-dependent manner in a subpopulation of rat striatal neurons. The effect of buprenorphine was largely reduced by naloxone, a non-selective opioid receptor antagonist, but not by μ, κ, δ or NOP-selective antagonists. β-Endorphin (0.1 μM) increased Ca(2+) with a lower amplitude and slower time course than buprenorphine. Similar to buprenorphine, the effect of β-endorphin was markedly decreased by naloxone, but not by opioid-selective antagonists. Morphine (0.1-10 μM), did not affect Ca(2+) in striatal neurons.
CONCLUSIONS
Our results suggest that buprenorphine and β-endorphin act on a distinct type/subtype of plasmalemmal opioid receptors or activate intracellular opioid-like receptor(s) in rat striatal neurons.
背景
丁丙诺啡是一种阿片受体配体，其作用机制尚不完全清楚。
方法
我们使用 Ca(2+) 成像技术，评估了丁丙诺啡、β-内啡肽和吗啡对大鼠纹状体神经元细胞浆钙离子浓度(Ca(2+))的影响。
结果
丁丙诺啡（0.01-1 μM）以剂量依赖的方式增加大鼠纹状体神经元亚群中的Ca(2+)。丁丙诺啡的作用主要被纳洛酮（一种非选择性阿片受体拮抗剂）所削弱，但不受 μ、κ、δ 或 NOP 选择性拮抗剂的影响。β-内啡肽（0.1 μM）增加Ca(2+)的幅度和速度比丁丙诺啡低。与丁丙诺啡相似，β-内啡肽的作用也明显被纳洛酮削弱，但不受阿片类选择性拮抗剂的影响。吗啡（0.1-10 μM）对纹状体神经元中的Ca(2+)没有影响。
结论
我们的结果表明，丁丙诺啡和β-内啡肽作用于大鼠纹状体神经元上的一种独特类型/亚型的质膜阿片受体，或激活细胞内阿片样受体。
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