Effect of bufalin and pregnanes on vasoreactivity of human resistance arteries.
Endogenous Na/K ATPase inhibitory activity has been implicated in salt and water homeostasis in mammals and amphibians. Recent interest has focused on endogenous cardiac glycosides, some progesterone derivatives (pregnanes) and the amphibian bufodienolides. This study has examined the effects of non-planar and planar pregnanes and the bufodienolide bufalin on vasoreactivity of human resistance arteries. Bufalin and a non-planar pregnane caused concentration-dependent potentiation of the tone of submaximally pre-contracted arteries and inhibited endothelium-dependent relaxation, whereas a planar pregnane affected neither response. The relative potency of the compounds studied suggest the results do not simply reflect degrees of Na/K ATPase inhibition. The active compounds may be important in the regulation of vascular tone.
Woolfson
R G
RG
Division of Physiology, United Medical School, Guys Hospital, London, UK.
Graves
J
J
LaBella
F S
FS
Templeton
J F
JF
Poston
L
L
D000109:Acetylcholine / Q000494:pharmacology; D000328:Adult; D001160:Arterioles / Q000187:drug effects / Q000502:physiology*; D002018:Bufanolides / Q000494:pharmacology*; D002715:Chlormadinone Acetate / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000502:physiology*; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008419:Materia Medica / Q000494:pharmacology; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D009638:Norepinephrine / Q000494:pharmacology; D011278:Pregnanes / Q000494:pharmacology*; D012867:Skin / Q000098:blood supply; D014655:Vascular Resistance; D014661:Vasoconstriction / Q000187:drug effects*; D014664:Vasodilation / Q000187:drug effects*
D002018:Bufanolides; D008419:Materia Medica; D011278:Pregnanes; D002715:Chlormadinone Acetate; D000109:Acetylcholine; C022777:bufalin; D009638:Norepinephrine