Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
A series of imidazole-containing (non-)chiral carbamates were tested at human histamine H(3) receptor (H(3)R). All compounds displayed K(i) values below 100 nM. A trend for a stereoselectivity at human H(3)R was observed for the chiral alpha-branched ligands. Selected compounds were also tested at human histamine H(4) receptor and showed moderate to weak affinities (118-1460 nM).
Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, 30-688 Kraków, Poland.
Dorota
D
Łazewska
Małgorzata
M
Wiecek
Xavier
X
Ligneau
Tim
T
Kottke
Lilia
L
Weizel
Roland
R
Seifert
Walter
W
Schunack
Holger
H
Stark
Katarzyna
K
Kieć-Kononowicz
D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects*; D011968:Receptors, Histamine / Q000187:drug effects*; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D000074040:Receptors, Histamine H4; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D002219:Carbamates; C418607:HRH4 protein, human; D007093:Imidazoles; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D018100:Receptors, Histamine H3; D000074040:Receptors, Histamine H4; C029899:imidazole