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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 and Buschauer, Armin (2009) Tritium-labeled N1-[3-(1H-imidazol-4-yl)propyl]-N2-propionylguanidine ([3H]UR-PI294), a high affinity histamine H3 and H4 receptor radioligand. ChemMedChem 4 (2), pp. 225-231.

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Other URL: http://www3.interscience.wiley.com/cgi-bin/fulltext/121579667/PDFSTART, http://www.ncbi.nlm.nih.gov/pubmed/19101971?ordinalpos=1&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum


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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Item type:Article
Date:13 February 2009
Additional Information (public):Online publiziert am 19. Dezember 2008
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
19101971PubMed ID
Related URLs:
http://onlinelibrary.wiley.com/doi/10.1002/cmdc.200990005/epdfSupplementary Material
Keywords:histamine H3 receptor; histamine H4 receptor; radiolabeled H3 receptor ligand; radiolabeled H4 receptor ligand; acylguanidine; imidazolylpropylguanidine
Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:4682
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