Evaluation of some aroxyethylamine derivatives for hypotensive properties and their affinities for adrenergic receptors.
A series of aroxyethylamines (1-10) was synthesized and evaluated for hypotensive activity in rats after intravenous and oral administration. The 4 compounds (4, 7, 8 and 10) containing a (2-methoxy)phenylpiperazine moiety displayed hypotensive activity and their affinities for alpha1-, alpha2- and beta1-adrenoreceptors were determined by radioligand binding assays. Compounds 4, 7, 8 and 10 were also tested for their effect on the pressor responses to epinephrine, norepinephrine, methoxamine, tyramine and DMPP. The results suggest that the hypotensive effect of these compounds is related to their alpha- and beta-adrenolytic properties.
Maciag
D
D
Department of Pharmacobiology, Faculty of Pharmacy, Medical College, Jagiellonian University, Kraków, Poland. dorota.m.farmbiol@interia.pl
Filipek
B
B
Czekaj
T
T
Marona
H
H
Nowak
G
G
D000284:Administration, Oral; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D002855:Chromatography, Thin Layer; D005021:Ethylamines / Q000737:chemistry* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007275:Injections, Intravenous; D007700:Kinetics; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011941:Receptors, Adrenergic / Q000187:drug effects / Q000378:metabolism*; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects / Q000378:metabolism; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects / Q000378:metabolism; D018342:Receptors, Adrenergic, beta-1 / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D014662:Vasoconstrictor Agents / Q000037:antagonists & inhibitors / Q000494:pharmacology
D000959:Antihypertensive Agents; D005021:Ethylamines; D007202:Indicators and Reagents; D011941:Receptors, Adrenergic; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; D018342:Receptors, Adrenergic, beta-1; D014662:Vasoconstrictor Agents