The prolonging effect of N,N'-diallylpentobarbital on the drug-induced sleep and motor incoordination
Yamamoto, I.; Tateoka, Y.; Watanabe, K.; Nabeshima, T.; Fontenot, H.J.; Ho, I.K.
Research Communications in Chemical Pathology and Pharmacology 50(2): 209-219
1985
ISSN/ISBN: 0034-5164 PMID: 4081315 Document Number: 246513
N-Allyl substituted derivatives of pentobarbital were prepared, and their pharmacological activities (hypnotic activity and anticonvulsant activity against pentylenetetrazol (PTZ)-induced seizures) were investigated with single intraperitoneal (i.p.) injection using mice. N-Monoallylpentobarbital (MAPB) was found to possess hypnotic activity [HD50 = 77.5(64.3-93.4) mg/kg, i.p.] and anticonvulsant activity [PTZ-ED50 = 23.5(14.2-38.9)mg/kg, i.p.]. N,N'-Diallylpentobarbital (DAPB) was devoid of not only the hypnotic activity of parent compound but also the anticonvulsant activity. The interaction of these N-allyl derivatives with barbiturates (pentobarbital (PB), barbital (B), phenobarbital (PheB), amobarbital (AB) and thiopental (TP] or diazepam (DZ) was further studied to characterize as antagonist or agonist. MAPB and DAPB (5-160mg/kg, i.p.) showed potent prolonging effect on PB-induced sleeping time and time of their peak effect was observed. The prolonging effects of these allyl compounds on PB-induced sleep were dose-dependent. Both compounds (80mg/kg, i.p.) also prolonged sleeping time induced by PheB, AB and TP. Although DAPB showed prolonging effect on B-induced sleep at a time interval 1 min, the compound shortened the sleeping time at 15 and 60 min. DAPB (5, 10 and 80mg/kg, i.p.) enhanced the DZ-induced motor incoordination.