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通过放射性配体结合研究对人和啮齿动物天然和重组的腺苷 A(2B)受体进行表征。

Characterization of human and rodent native and recombinant adenosine A(2B) receptors by radioligand binding studies.

机构信息

Pharmaceutical Institute, Pharmaceutical Sciences Bonn (PSB), Pharmaceutical Chemistry Poppelsdorf, University of Bonn, Bonn, Germany.

出版信息

Purinergic Signal. 2006 Sep;2(3):559-71. doi: 10.1007/s11302-006-9012-4. Epub 2006 Jul 8.

DOI:10.1007/s11302-006-9012-4
PMID:18404493
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2096648/
Abstract

Adenosine A(2B) receptors of native human and rodent cell lines were investigated using [(3)H]PSB-298 [(8-{4-[2-(2-hydroxyethylamino)-2-oxoethoxy]phenyl}-1-propylxanthine] in radioligand binding studies. [(3)H]PSB-298 showed saturable and reversible binding. It exhibited a K(D) value of 60 +/- 1 nM and limited capacity (B(max) = 3.511 fmol per milligram protein) at recombinant human adenosine A(2B) receptors expressed in human embryonic kidney cells (HEK-293). The addition of sodium chloride (100 mM) led to a threefold increase in the number of binding sites recognized by the radioligand. The curve of the agonist 5'-N-ethylcarboxamidoadenosine (NECA) was shifted to the right in the presence of NaCl, while the curve of the antagonist PSB-298 was shifted to the left, indicating that PSB-298 may be an inverse agonist at A(2B) receptors. Adenosine A(2B) receptors were shown to be the major adenosine A(2) receptor subtype on the mouse neuroblastoma x rat glioma hybrid cell line NG108-15 cells. Binding studies at rat INS-1 cells (insulin secreting cell line) demonstrated that [(3)H]PSB-298 is a selective radioligand for adenosine A(2B) binding sites in this cell line.

摘要

采用 [(3)H]PSB-298 [(8-{4-[2-(2-羟乙基氨基)-2-氧代乙氧基]苯基}-1-丙基黄嘌呤]，对天然人源和啮齿动物细胞系的腺苷 A(2B)受体进行了研究。 [(3)H]PSB-298 表现出可饱和和可还原的结合特性。它在表达于人胚肾细胞 (HEK-293) 的重组人腺苷 A(2B)受体上的 K(D) 值为 60 +/- 1 nM，最大结合容量 (B(max) = 3.511 皮摩尔/毫克蛋白)。加入氯化钠 (100 mM) 可使被放射性配体识别的结合位点数量增加三倍。激动剂 5'-N-乙基羧酰胺腺苷 (NECA) 的曲线在存在 NaCl 的情况下向右侧移位，而拮抗剂 PSB-298 的曲线向左侧移位，表明 PSB-298 可能是 A(2B)受体的反向激动剂。腺苷 A(2B)受体被证明是鼠神经母细胞瘤 x 大鼠神经胶质瘤杂交细胞系 NG108-15 上的主要腺苷 A(2)受体亚型。在大鼠 INS-1 细胞 (胰岛素分泌细胞系) 上的结合研究表明，[(3)H]PSB-298 是该细胞系中腺苷 A(2B)结合位点的选择性放射性配体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/bb1dac02d7fc/11302_2006_Article_9012_Fig12.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/bb1dac02d7fc/11302_2006_Article_9012_Fig12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/cd45f9654825/11302_2006_Article_9012_Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/13a57c2bc919/11302_2006_Article_9012_Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/a7d675dcb386/11302_2006_Article_9012_Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/07c07d38838c/11302_2006_Article_9012_Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/b0818a9b7a5f/11302_2006_Article_9012_Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/8b14d82b3fbe/11302_2006_Article_9012_Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/e05c61878ecd/11302_2006_Article_9012_Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/c6cd77735c08/11302_2006_Article_9012_Fig8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/92cb20563940/11302_2006_Article_9012_Fig9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/3a6deda07f35/11302_2006_Article_9012_Fig10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/fbf39b2f09eb/11302_2006_Article_9012_Fig11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/27b7/2096648/bb1dac02d7fc/11302_2006_Article_9012_Fig12.jpg

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