2-[125I]iodomelatonin and [3H]melatonin Binding Assays for Melatonin Receptors.

褪黑素受体的 2 - [125I] 碘褪黑素和 [3H] 褪黑素结合测定。

• 发表时间: 2022
• 来源期刊: Methods Mol Biol
• DOI: 10.1007/978-1-0716-2593-4_18
• PMID: 36180687
• 文章类型: Journal Article
• 作者列表: Gbahou F,Jockers R,Gbahou F,Jockers R,Gbahou F,Jockers R

关键词: 2-[125I]-iodomelatonin; Binding assay; Competition; Kinetic; Melatonin receptors; Radioligand; Saturation; [3H]-melatonin; 2-[125I]-iodomelatonin; Binding assay; Competition; Kinetic; Melatonin receptors; Radioligand; Saturation; [3H]-melatonin; 2-[125I]-iodomelatonin; Binding assay; Competition; Kinetic; Melatonin receptors; Radioligand; Saturation; [3H]-melatonin

Mesh: Binding Sites; Binding, Competitive; Iodine Radioisotopes; Kinetics; Ligands; Melatonin / metabolism; Receptors, Cell Surface / metabolism; Receptors, Melatonin; Binding Sites; Binding, Competitive; Iodine Radioisotopes; Kinetics; Ligands; Melatonin / metabolism; Receptors, Cell Surface / metabolism; Receptors, Melatonin; Binding Sites; Binding, Competitive; Iodine Radioisotopes; Kinetics; Ligands; Melatonin / metabolism; Receptors, Cell Surface / metabolism; Receptors, Melatonin

Abstract

The radioligand binding assay is a powerful method to study the interaction of a ligand with its target. This technique allows not only to determine different pharmacological key parameters such as the affinity and the association and dissociation constants but also to estimate the amount of target expressed in recombinant or endogenous cells or tissues. The current detailed protocols describe the different binding assays (saturation, kinetic, and competition) that can be performed on melatonin receptors using their most commonly used and validated radioligands 2-[125I]-iodomelatonin (2-[125I]-MLT) and [3H]-melatonin ([3H]-MLT).

摘要

放射性配体结合测定法是研究配体与其靶标相互作用的有力方法。该技术不仅允许确定不同的药理学关键参数,例如亲和力以及缔合和解离常数,而且允许估计在重组或内源性细胞或组织中表达的靶标的量。当前的详细方案描述了不同的结合测定(饱和，动力学,和竞争），可以使用其最常用和经过验证的放射性配体2-[125I]-碘褪黑素（2-[125I]-MLT）和[3H]-褪黑素（[3H]-MLT）对褪黑素受体进行。