Tritium-Labeled N-1-[3-(1H-imidazol-4-yl)propyl]-N-2-propionylguanidine ([H-3]UR-PI294), a High-Affinity Histamine H-3 and H-4 Receptor Radioligand

Igel, Patrick and Schnell, David and Bernhardt, Guenther and Seifert, Roland and Buschauer, Armin (2009) Tritium-Labeled N-1-[3-(1H-imidazol-4-yl)propyl]-N-2-propionylguanidine ([H-3]UR-PI294), a High-Affinity Histamine H-3 and H-4 Receptor Radioligand. CHEMMEDCHEM, 4 (2). pp. 225-231. ISSN 1860-7179, 1860-7187

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Abstract

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.

Item Type: Article
Uncontrolled Keywords: PHARMACOLOGICAL CHARACTERIZATION; 1ST POTENT; CLONING; ANTAGONIST; CELLS; IDENTIFICATION; BENZIMIDAZOLE; H-2-RECEPTOR; INHIBITION; EXPRESSION; acylguanidines; histamine receptor ligands; imidazolylpropylguanidine; radiopharmaceuticals; receptors
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Depositing User: Dr. Gernot Deinzer
Date Deposited: 06 Oct 2020 11:01
Last Modified: 06 Oct 2020 11:01
URI: https://pred.uni-regensburg.de/id/eprint/29494

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