Potentiation of barbiturate-induced narcosis by N,N'- (or N,S-) diallyl-substituted derivatives of phenobarbital, amobarbital and thiopental in mice
| Autor: | Yuji Tateoka, Ikuo Yamamoto, Toshiyuki Kimura, Kazuhito Watanabe, Ing Kang Ho |
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| Rok vydání: | 1987 |
| Předmět: |
Male
medicine.drug_class Amobarbital medicine.medical_treatment Allyl compound Mice Inbred Strains Pharmacology Hypnotic Mice Structure-Activity Relationship Drug Discovery medicine Animals Thiopental Chemistry Long-term potentiation Biological activity General Chemistry General Medicine Allyl Compounds Anticonvulsant Barbiturate Phenobarbital Anticonvulsants Sleep medicine.drug |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 35:778-784 |
| ISSN: | 1347-5223 0009-2363 |
| Popis: | N- (or S-) Allyl derivatives of phenobarbital (PheB), amobarbital (AB) and thiopental (TP) were prepared, and their pharmacological activities (hypnotic activity and anticonvulsant activity against pentylenetetrazol-induced seizures) were investigated in mice. N-Monoallyl-substituted derivatives (MAPheB, MAAB and MATP) of PheB, AB and TP exhibited hypnotic and anticonvulsant activities. N, S-Diallylthiopental (N, S-DATP) possessed hypnotic activity, but failed to show anticonvulsant activity even at a dose of 250 mg/kg (i.p.). N, N '- Diallyl-substituted derivatives (DAPheB, DAAB and DATP) were devoid of not only the hypnotic activity, but also-the anticonvulsant activity. The interactions of these allyl derivatives with various barbiturates were then studied in order to characterize whether the allyl compounds have antagonistic or potentiating properties. MAPheB, DAPheB, MAAB and DAAB showed dose-dependent potentiation of the sleep induced by the corresponding mother compounds. All the allyl compounds tested prolonged the pentobarbital-induced sleeping time more than 7- to 19-fold as compared with the control. MAAB markedly prolonged the PheB-induced sleeping time by 25-fold, but it did not potentiate the barbital-induced sleep. These results indicate that N- (or S-) allyl derivatives of PheB, AB and TP interact differently with the barbiturates. |
| Databáze: | OpenAIRE |
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