Abstract |
Pharmacological activities ( hypnotic, anticonvulsant and convulsant activities, acute toxicity and pentobarbital (PB) synergism) of N-allyl,N'-methyl derivatives of barbiturates and related N-allyl substituted compounds were studied in mice. N-Allylhexobarbital (AHB), N-allylglutethimide (AGI) and N-allylmethyprylon ( AMP) showed hypnotic activity. N-Allyl,N'-methyl derivatives of barbital (B), phenobarbital (PheB) and PB (AMB, AMPheB and AMPB), AHB and AMP exhibited anticonvulsant activity against pentylenetetrazol (PTZ)-induced seizures. AMP was the most potent agent among the allyl compounds tested in the protective effect against PTZ-induced seizures. N-Allyl, N'-methylallobarbital (AMAlloB) showed a weak convulsant activity at a dose of 640 mg/kg, i.p. All allyl compounds tested showed potentiation of the PB-induced sleep. AMB prolonged the PB-induced sleep 30-fold as compared with the control. These results indicate that AMB, AMP and the other N- allyl compounds possess some depressant effects on the central nervous system.
|
Authors | I Yamamoto, Y Tateoka, T Kimura, F Yamazaki, K Hamajima, K Watanabe, I K Ho |
Journal | Research communications in chemical pathology and pharmacology
(Res Commun Chem Pathol Pharmacol)
Vol. 54
Issue 2
Pg. 191-9
(Nov 1986)
ISSN: 0034-5164 [Print] United States |
PMID | 2878477
(Publication Type: Journal Article)
|
Chemical References |
- Allyl Compounds
- Anticonvulsants
- Barbiturates
- Central Nervous System Depressants
- Convulsants
- Piperidones
- N-allylmethyprylon
|
Topics |
- Allyl Compounds
(pharmacology)
- Animals
- Anticonvulsants
(pharmacology)
- Barbiturates
(pharmacology)
- Brain
(drug effects)
- Central Nervous System Depressants
(pharmacology)
- Convulsants
(pharmacology)
- Male
- Mice
- Mice, Inbred Strains
- Piperidones
(analogs & derivatives, pharmacology)
- Sleep
(drug effects)
- Structure-Activity Relationship
|