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

来源：

CHEMMEDCHEM | 2009年 / 4卷 / 02期

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

页码：225 / 231

页数：7

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