Tritium-labeled N(1)-[3-(1H-imidazol-4-yl)propyl]-N(2)-propionylguanidine ([(3)H]UR-PI294), a high-affinity histamine H(3) and H(4) receptor radioligand.
This study reports the synthesis and pharmacological characterization of tritium-labeled N(1)-[3-(1H-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 nM, K(D) (hH(4)R)=5.1 nM) and is shown to be a valuable pharmacological tool for the determination of hH(3)R and hH(4)R affinities.
Igel
Patrick
P
Institut für Pharmazie, Universität Regensburg, Germany.
Schnell
David
D
Bernhardt
Günther
G
Seifert
Roland
R
Buschauer
Armin
A
D000818:Animals; D001667:Binding, Competitive; D002851:Chromatography, High Pressure Liquid; D006146:Guanidines / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D011869:Radioligand Assay; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D011968:Receptors, Histamine / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D000074040:Receptors, Histamine H4; D013056:Spectrophotometry, Ultraviolet; D018411:Spodoptera; D014316:Tritium
D006146:Guanidines; C418607:HRH4 protein, human; D007093:Imidazoles; C539896:N(1)-(3-(1H-imidazol-4-yl)propyl)-N(2)-propionylguanidine; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; D000074040:Receptors, Histamine H4; D014316:Tritium