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Tritium‐Labeled N 1 ‐[3‐(1 H ‐imidazol‐4‐yl)propyl]‐ N 2 ‐propionylguanidine ([ 3 H]UR‐PI294), a High‐Affinity Histamine H 3 and H 4 Receptor Radioligand
Author(s) -
Igel Patrick,
Schnell David,
Bernhardt Günther,
Seifert Roland,
Buschauer Armin
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800349
Subject(s) - radioligand , histamine , tritium , histamine receptor , chemistry , receptor , stereochemistry , affinities , radioligand assay , histamine h4 receptor , ligand (biochemistry) , radiochemistry , biochemistry , pharmacology , histamine h2 receptor , biology , antagonist , physics , nuclear physics
Histamine mediates its various functions through four histamine receptor subtypes. The H 3 subtype is mainly found in the central nervous system, where it modulates the release of histamine and other neurotransmitters, whereas the H 4 subtype plays a crucial role in inflammatory and immunological processes. Herein, the synthesis and characterization of a conveniently accessible tritiated radioligand is reported that proved to be a versatile pharmacological probe.This study reports the synthesis and pharmacological characterization of tritium‐labeled N 1 ‐[3‐(1 H ‐imidazol‐4‐yl)propyl]‐ N 2 ‐propionylguanidine ([ 3 H]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 n M , K D (hH 4 R)=5.1 n M ) and is shown to be a valuable pharmacological tool for the determination of hH 3 R and hH 4 R affinities.