N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.
New potent N alpha-alkylated histamine H1-receptor agonists have been prepared and functionally evaluated for partial agonist potency and selectivity. N alpha-Methyl-2-(3-trifluoromethylphenyl)histamine contracts ileal segments and aortic rings of guinea-pig with a relative potency of 174% (95% confid. lim. 161-188%) and 217% (164-287%), respectively (histamine: 100%) and is the most potent H1 receptor agonist described so far.
Kramer
K
K
Fachbereich Pharmazie, Freie Universität Berlin, Germany.
Elz
S
S
Pertz
H H
HH
Schunack
W
W
D000478:Alkylation; D000818:Animals; D001011:Aorta / Q000187:drug effects; D006168:Guinea Pigs; D006632:Histamine / Q000031:analogs & derivatives*; D017442:Histamine Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D011969:Receptors, Histamine H1 / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014661:Vasoconstriction / Q000187:drug effects
D017442:Histamine Agonists; D011969:Receptors, Histamine H1; D006632:Histamine