Pharmacological properties of some xanthone derivatives.
A series of aminoalkanolic derivatives of xanthone were examined in some experimental models of epilepsia, i.e., pilocarpine, aminophylline and pentetrazole-induced seizures. A final objective of this research was to examine the action of these compounds on the central nervous system, namely on spontaneous locomotor activity, amphetamine-induced hyperactivity and narcotic sleep induced by hexobarbital, as well as their influence on the gamma-aminobutyric acid (GABA) level and glutamic acid decarboxylase (GAD) activity in mice brain. The most interesting were the pharmacological results of (R)-2-N-methylamino-1-butanol derivative of 7-chloro-2-methylxanthone [Id], which displayed protective activity against the seizures induced by maximum electroshock and pentetrazole induced seizures; moreover, this compound had a relatively low toxicity and did not exhibit a neurotoxic effect. The influence on the locomotor activity as well as on the amphetamine-induced locomotor hyperactivity in mice was also seen for Id. Compound Id did not decrease the GABA level in mice brain.
Rajtar
G
G
Department of Pharmacology and Toxicology, Medical University School, Lublin, Poland.
Zółkowska
D
D
Kleinrok
Z
Z
Marona
H
H
D000628:Aminophylline; D000661:Amphetamine; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects*; D005968:Glutamate Decarboxylase / Q000378:metabolism; D006591:Hexobarbital / Q000633:toxicity; D006948:Hyperkinesis / Q000139:chemically induced; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole; D010862:Pilocarpine; D012890:Sleep / Q000187:drug effects; D014966:Xanthenes / Q000494:pharmacology*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000927:Anticonvulsants; D014966:Xanthenes; D010862:Pilocarpine; D000628:Aminophylline; D005680:gamma-Aminobutyric Acid; D006591:Hexobarbital; D000661:Amphetamine; D005968:Glutamate Decarboxylase; D010433:Pentylenetetrazole