Tritium-Labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionylguanidine ([3H]UR-PI294), a High-Affinity Histamine H3 and H4 Receptor Radioligand

被引:32
作者
Igel, Patrick [1 ]
Schnell, David [2 ]
Bernhardt, Guenther [1 ]
Seifert, Roland [3 ]
Buschauer, Armin [1 ]
机构
[1] Univ Regensburg, Inst Pharm, D-93053 Regensburg, Germany
[2] Univ Regensburg, Inst Pharm Pharmakol & Toxikol, D-93053 Regensburg, Germany
[3] Hannover Med Sch, Inst Pharmacol, D-30625 Hannover, Germany
关键词
acylguanidines; histamine receptor ligands; imidazolylpropylguanidine; radiopharmaceuticals; receptors; PHARMACOLOGICAL CHARACTERIZATION; 1ST POTENT; CLONING; ANTAGONIST; CELLS; IDENTIFICATION; BENZIMIDAZOLE; H-2-RECEPTOR; INHIBITION; EXPRESSION;
D O I
10.1002/cmdc.200800349
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This study reports the synthesis and pharmacological characterization of tritium-labeled N-1-[3-(1H-imidazol-4-yl)propyl]-N-2-propionylguanidine ([H-3]UR-PI294), a novel and readily accessible radioligand for the human histamine H-3 receptor (hH(3)R) and H-4 receptor (hH(4)R). The radioligand displays high affinity for both histamine receptor subtypes (K-D (hH(3)R) = 1.1 nm, K-D (h H4R) = 5.1 nM) and is shown to be a valuable pharmacological tool for the determination of hH(3)R and hH(4)R affinities.
引用
收藏
页码:225 / 231
页数:7
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