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Tritium-labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionylguanidine ([3H]UR-PI294), a high affinity histamine H3 and H4 receptor radioligand

Igel, Patrick ; Schnell, David ; Bernhardt, Günther ; Seifert, Roland ; Buschauer, Armin



Abstract

This study reports the synthesis and pharmacological characterization of tritium-labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionyl¬guanidine ([3H]UR-PI294), a novel readily accessible radioligand for the human histamine H3 receptor (hH3R) and H4 receptor (hH4R). The radioligand displayed high affinity for both histamine receptor subtypes (KD (hH3R) = 1.1 nM, KD (hH4R) = 5.1 nM) and was shown to serve as a valuable pharmacological tool for the determination of hH3R and hH4R affinities.


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