The antagonistic effects of 5-ethyl-5-(3-hydroxy-1-methylbutyl)-barbituric acid on pentobarbital narcosis in both naïve and tolerant mice

I. Yamamoto; I. K. Ho; H. H. Loh

doi:10.1016/0024-3205(78)90281-3

The antagonistic effects of 5-ethyl-5-(3-hydroxy-1-methylbutyl)-barbituric acid on pentobarbital narcosis in both naïve and tolerant mice

I. Yamamoto, I. K. Ho, H. H. Loh

Pharmacology

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Abstract

These studies demonstrated that 5-ethyl-5-(3-hydroxyl-1-methyl-butyl)-barbituric acid (PB-OH), a major metabolite of pentobarbital, antagonized pentobarbital-induced narcosis in both naive and pentobarbital tolerant mice. In PB-OH pretreated mice, the sleeping time induced by sodium pentobarbital was significantly shorter than that of the saline control animals. However, PB-OH failed to modify the pentobarbital-induced hypothermia. The findings also demonstrated that hepatic microsomal enzyme activity and half lives of pentobarbital and PB-OH in both plasma and brain were not modified by the pretreatment of PB-OH. The specific antagonistic effect of PB-OH appears to be a direct effect on sites in the CNS.

Original language	English (US)
Pages (from-to)	1103-1111
Number of pages	9
Journal	Life Sciences
Volume	22
Issue number	12
DOIs	https://doi.org/10.1016/0024-3205(78)90281-3
State	Published - Mar 1978

Bibliographical note

Funding Information:
These studies were supported by NIDA grant DA-01403 . H . H . Loh is a recipient of a NIMH Research Scientist Development Award, K2-DA-70554 . The authors wish to thank Mrs . Susan Culbertson for assistance in preparation of the manuscript and Dr . Mary E . Davis for many helpful suggestions .

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title = "The antagonistic effects of 5-ethyl-5-(3-hydroxy-1-methylbutyl)-barbituric acid on pentobarbital narcosis in both na{\"i}ve and tolerant mice",

abstract = "These studies demonstrated that 5-ethyl-5-(3-hydroxyl-1-methyl-butyl)-barbituric acid (PB-OH), a major metabolite of pentobarbital, antagonized pentobarbital-induced narcosis in both naive and pentobarbital tolerant mice. In PB-OH pretreated mice, the sleeping time induced by sodium pentobarbital was significantly shorter than that of the saline control animals. However, PB-OH failed to modify the pentobarbital-induced hypothermia. The findings also demonstrated that hepatic microsomal enzyme activity and half lives of pentobarbital and PB-OH in both plasma and brain were not modified by the pretreatment of PB-OH. The specific antagonistic effect of PB-OH appears to be a direct effect on sites in the CNS.",

author = "I. Yamamoto and Ho, {I. K.} and Loh, {H. H.}",

note = "Funding Information: These studies were supported by NIDA grant DA-01403 . H . H . Loh is a recipient of a NIMH Research Scientist Development Award, K2-DA-70554 . The authors wish to thank Mrs . Susan Culbertson for assistance in preparation of the manuscript and Dr . Mary E . Davis for many helpful suggestions .",

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AU - Ho, I. K.

AU - Loh, H. H.

N1 - Funding Information: These studies were supported by NIDA grant DA-01403 . H . H . Loh is a recipient of a NIMH Research Scientist Development Award, K2-DA-70554 . The authors wish to thank Mrs . Susan Culbertson for assistance in preparation of the manuscript and Dr . Mary E . Davis for many helpful suggestions .

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N2 - These studies demonstrated that 5-ethyl-5-(3-hydroxyl-1-methyl-butyl)-barbituric acid (PB-OH), a major metabolite of pentobarbital, antagonized pentobarbital-induced narcosis in both naive and pentobarbital tolerant mice. In PB-OH pretreated mice, the sleeping time induced by sodium pentobarbital was significantly shorter than that of the saline control animals. However, PB-OH failed to modify the pentobarbital-induced hypothermia. The findings also demonstrated that hepatic microsomal enzyme activity and half lives of pentobarbital and PB-OH in both plasma and brain were not modified by the pretreatment of PB-OH. The specific antagonistic effect of PB-OH appears to be a direct effect on sites in the CNS.

AB - These studies demonstrated that 5-ethyl-5-(3-hydroxyl-1-methyl-butyl)-barbituric acid (PB-OH), a major metabolite of pentobarbital, antagonized pentobarbital-induced narcosis in both naive and pentobarbital tolerant mice. In PB-OH pretreated mice, the sleeping time induced by sodium pentobarbital was significantly shorter than that of the saline control animals. However, PB-OH failed to modify the pentobarbital-induced hypothermia. The findings also demonstrated that hepatic microsomal enzyme activity and half lives of pentobarbital and PB-OH in both plasma and brain were not modified by the pretreatment of PB-OH. The specific antagonistic effect of PB-OH appears to be a direct effect on sites in the CNS.

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The antagonistic effects of 5-ethyl-5-(3-hydroxy-1-methylbutyl)-barbituric acid on pentobarbital narcosis in both naïve and tolerant mice

Abstract

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