[The influence of the GABA-B receptor antagonists 2-hydoxysaclofen and faclofen on the sedative effect of fenibut and baclofen].
Pretreatment of NIH-Swiss mice with HYS (8 mg/kg) is shown to reduce the inhibiting effect (namely, the reduction of the locomotion rate and the number of horizontal movements) of PHE (80 mg/kg) and do not affect the action of an equipotent dose (4 mg/kg) of BAC. BAC induced shortening of the locomotion period is reduced by HYS. HYS appeared to be inactive with respect to inhibiting effect of PHE. PHE and BAC shortening of the distance covered was insensitive to HYS administration. HYS reduces decrease in the rate and duration of rearings induced by PHE. PHA (8 mg/kg) do not change the sedative effect of PHE and BAC on locomotion, attenuated the PHE-induced inhibition of rearings and increase the effect of BAC. It is suggested that GABA-B receptors affect the inhibitory action of PHE rather strong than that of BAC and differ in the inhibition of horizontal and vertical components of the locomotor activity of mice.
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D000818:Animals; D001418:Baclofen / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004347:Drug Interactions; D018755:GABA Agonists / Q000494:pharmacology*; D058788:GABA-B Receptor Antagonists; D006993:Hypnotics and Sedatives / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology
D018755:GABA Agonists; D058788:GABA-B Receptor Antagonists; D006993:Hypnotics and Sedatives; C052329:phaclofen; D005680:gamma-Aminobutyric Acid; D001418:Baclofen; C008842:4-amino-3-phenylbutyric acid; C057491:2-hydroxysaclofen
Vliianie antagonistov GAMK B-retseptorov 2-gidroksisaklofena i faklofena na sedativnyĭ éffekt fenibut i baklofena.