UK PubMed Central (United Kingdom)

1. The structural requirements of an allosteric barbiturate binding site on acetylcholine receptor-rich membranes isolated from Torpedo electroplaques have been characterized by the ability of fourteen...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

Barbiturates substituted at the 5-position with organyltelluroalkyl or organylselenoalkyl groups were prepared by ring annulation of appropriately substituted diethyl malonates with urea or thiourea. The substituted diethyl malonates (phenyltellurobutyl(ethyl), i-propyltelluropropyl(ethyl), i-propyltelluropropyl(allyl), i-propyselenopropyl(ethyl), and phenylselenohexyl(methyl)) were prepared in 55-91% yield by reaction of diethyl omega-bromoalkyl(alkyl)malonates with organyltellurolates or selenolates (RXNa; X = Se, Te) in ethanol/benzene. The following barbiturates were obtained in 28-84% yield: phenyltellurobutyl(ethyl), m.p. 100/sup 0/C; i-propyltelluropropyl(ethyl), m.p. 119/sup 0/C; i-propylselenopropyl(ethyl), m.p. 137/sup 0/C; phenyl-selenohexyl(methyl), m.p. 124/sup 0/C. The 5-substituted thiobarbiturates i-propyltelluropropyl(ethyl)-(m.p. 75/sup 0/C) and i-propylselenopropyl(ethyl)thiobarbiturate (m.p. 83/sup 0/C) were isolated in 32 ...

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The anticonvulsant drugs carbamazepine, phenobarbital, trimethadione, valproic acid and ethosuximide at pharmacologically relevant concentrations inhibit (/sup 3/H)diazepam binding to astrocytes in primary cultures but have much less effect on a corresponding preparation of neurons. Phenytoin as well as pentobarbital (which is not used chronically as an anticonvulsant) are equipotent in the two cell types. The convulsants picrotoxinin and pentylenetetrazol, the convulsant benzodiazepine RO 5-3663 and the two convulsant barbiturates DMBB and CHEB similarly inhibit diazepam binding to astrocytes but have little effect on neurons. On the basis of these findings it is suggested that these convulsants and anticonvulsants owe at least part of their effect to an interaction with the astrocytic benzodiazepine receptor, perhaps by interference with a calcium channel.

Energy Technology Data Exchange (ETDEWEB)

To determine if barbiturates would protect brain at high doses of radiation, survival rates in rats that received whole-brain x-irradiation during pentobarbital- or lidocaine-induced anesthesia were compared with those of control animals that received no medication and of animals anesthetized with ketamine. The animals were shielded so that respiratory and digestive tissues would not be damaged by the radiation. Survival rates in rats that received whole-brain irradiation as a single 7500-rad dose under pentobarbital- or lidocaine-induced anesthesia was increased from between from 0% and 20% to between 45% and 69% over the 40 days of observation compared with the other two groups (p less than 0.007). Ketamine anesthesia provided no protection. There were no notable differential effects upon non-neural tissues, suggesting that pentobarbital afforded protection through modulation of ambient neural activity during radiation exposure. Neural suppression during ...

International Nuclear Information System (INIS)

Objectives: To minimize movement artifacts during tracer imaging studies, the animals are generally sedated. Although many reports describe the effect of barbiturates on brain function, less is published about the general impact on the extracerebral metabolism and tracer biodistribution. This report describes the influence of pentobarbital on tumor uptake of ["1"2"3I]-2-iodo-L-phenylalanine (["1"2"3I]-2I-L-PA) using dissection and nuclear imaging. Methods: R1M tumor-bearing athymic mice were divided into two populations: untreated and pentobarbital-treated. Each group was subjected to dynamic and static planar imaging and organ dissection after ["1"2"3I]-2I-L-PA injection. Two-compartment blood modeling was performed. Analysis of variance (ANOVA), t test and clustered boxplot analyses were used to compare the results between the treatment groups and between the data acquisition methods. Results: Two-compartment blood modeling demonstrated that pentobarbital ...