Effect of modulators of the polyamine site on the development of seizures induced by systemic and intracerebral administration of N-methyl-D-aspartate in albino mice.
Systemic intraperitoneal administration of polyamine agonist IEM-1460 containing the Me3N(+) group with a stable positive charge preventing permeation of this substance through the blood-brain barrier and polyamine antagonist arcaine had no effect on the development of seizures caused by intracerebral injection of N-methyl-D-aspartate in mice. Intraperitoneal injection of IEM-40 potentiated, while arcaine decreased the severity of seizures induced by intraperitoneal treatment with N-methyl-D-aspartate. This effect was related to modulation of the permeability of the blood-brain barrier for N-methyl-D-aspartate probably due to modulating effects of IEM-40 and arcaine on the polyamine site of N-methyl-D-aspartate receptors in the blood-brain barrier.
Efremov
O M
OM
Institute of Experimental Medicine, Russian Academy of Medical Sciences, St Petersburg, Russia.
Serdyuk
S E
SE
Gmiro
V E
VE
D000818:Animals; D001812:Blood-Brain Barrier; D007276:Injections, Intraventricular; D008297:Male; D051379:Mice; D016202:N-Methylaspartate / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000633:toxicity*; D011073:Polyamines / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000139:chemically induced*
D011073:Polyamines; D016202:N-Methylaspartate