Abstract |
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.
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Authors | I Yamamoto, Y Tateoka, K Watanabe, T Nabeshima, H J Fontenot, I K Ho |
Journal | Research communications in chemical pathology and pharmacology
(Res Commun Chem Pathol Pharmacol)
Vol. 50
Issue 2
Pg. 209-19
(Nov 1985)
ISSN: 0034-5164 [Print] United States |
PMID | 4081315
(Publication Type: Journal Article)
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Chemical References |
- Anticonvulsants
- Barbiturates
- Hypnotics and Sedatives
- N,N-diallylpentobarbital
- N-allylpentobarbital
- Pentobarbital
- Diazepam
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Topics |
- Animals
- Anticonvulsants
- Barbiturates
(pharmacology)
- Diazepam
(pharmacology)
- Dose-Response Relationship, Drug
- Drug Synergism
- Hypnotics and Sedatives
- Male
- Mice
- Pentobarbital
(analogs & derivatives, pharmacology)
- Psychomotor Performance
(drug effects)
- Sleep
(drug effects)
- Time Factors
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