The biological activity of d- and l-baclofen (Lioresal).
Racemic d,l-baclofen and l-baclofen depressed the patellar, flexor, linguo-mandibular (0.1--30 mg/kg i.v.) and the H-reflex (1--3 mg/kg i.v.) in a dose-dependent fashion. Racemic and l-baclofen partly antagonized electroshock-induced convulsions in mice (30--60 mg/kg p.o.) and depressed the firing rate of nigral cells when applied iontophoretically. d,l-Baclofen and l-baclofen (0.1--3.0 mg/kg i.v.) moderately reduced the blood pressure in cats. Dextrorotatory baclofen, at identical doses was inactive in all these tests. It is concluded that the biological activity of baclofen resides with the l-enantiomer.
D000613:Aminobutyrates / Q000494:pharmacology*; D000818:Animals; D001418:Baclofen / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D012018:Reflex / Q000187:drug effects; D012640:Seizures / Q000188:drug therapy; D013378:Substantia Nigra / Q000187:drug effects; D009435:Synaptic Transmission / Q000187:drug effects
D000613:Aminobutyrates; D001418:Baclofen