Effect of the steroidal alkaloid buxaminol-E on blood pressure, acetylcholinesterase activity and (3H)quinuclidinyl benzilate binding in cerebral cortex.
Pharmacological properties of the steroidal alkaloid buxaminol-E isolated from Buxus sempervirens varietas bullata were studied in relation to the cholinergic nervous system. In anaesthetised cats buxaminol-E (1.25 mumol/kg) initially induced a small short-lasting increase in blood pressure followed by marked hypotension. Atropine (1.47 mumol/kg) inhibited the hypotensive effect almost completely and methylatropine (1.47 mumol/kg) partially. Buxaminol-E and the muscarinic agonists McN-A-343 and bethanechol inhibited the binding of the muscarinic antagonist (3H)quinuclidinyl benzilate in cat and rabbit cerebral cortex membranes in decreasing order of potency. In about 10-fold higher concentrations they also inhibited acetylcholinesterase activity in cat cerebral cortex in the same order of potency. The results suggest that the hypotensive effect of buxaminol-E could be due to both central and peripheral activation of muscarinic receptors, and to a lesser degree to inhibition of acetylcholinesterase activity.
Kvaltínová
Z
Z
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.
Lukovic
L
L
Machová
J
J
Fatranská
M
M
D008455:(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride / Q000494:pharmacology; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D001286:Atropine Derivatives / Q000494:pharmacology; D018723:Bethanechol; D001626:Bethanechol Compounds / Q000494:pharmacology; D001665:Binding Sites; D001794:Blood Pressure / Q000187:drug effects*; D002415:Cats; D002540:Cerebral Cortex / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D002800:Cholinesterase Inhibitors; D005260:Female; D008297:Male; D009649:Norpregnadienes / Q000494:pharmacology*; D011813:Quinuclidinyl Benzilate / Q000737:chemistry / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000502:physiology
D000470:Alkaloids; D001286:Atropine Derivatives; D001626:Bethanechol Compounds; D002800:Cholinesterase Inhibitors; D009649:Norpregnadienes; D011976:Receptors, Muscarinic; D018723:Bethanechol; C065119:buxaminol E; D008455:(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride; D011813:Quinuclidinyl Benzilate; D001285:Atropine; C006649:methylatropine