An evaluation of the selectivity of fenmetozole (DH-524) reversal of ethanol-induced changes in central nervous system function

  title={An evaluation of the selectivity of fenmetozole (DH-524) reversal of ethanol-induced changes in central nervous system function},
  author={Gerald D. Frye and George R. Breese and Richard B. Mailman and Richard A. Vogel and M. Gene Ondrusek and Robert A. Mueller},
The selectivity and specificity of fenmetozole (DH-524) [2(3,4-dichlorophenoxy-methy))2-imidazole HCl] as an antagonist of the actions of ethanol were examined. Fenmetozole (15–30 g/kg) reduced ethanol-induced impairment of the aerial righting reflex without changing blood or brain ethanol content, indicating that the antagonistic actions of fenmetozole were not due to change in the pharmacokinetics of ethanol. Since fenmetozole also reduced aerial righting reflex impairment due to… 

An evaluation of the locomotor stimulating action of ethanol in rats and mice

The findings suggest that biological differences in strains and species of laboratory rodents contribute to the apparent variability of locomotor stimulation caused by ethanol, and that ethanol-induced increases in the spontaneous locomotor activity of CD-1 mice in photocell activity monitors and in intertrial-interval crosses in rats in a shuttle box task do not appear to share a common mechanism.

Pharmacology of flibanserin.

Flibanserin displays antidepressant-like activity in most animal models sensitive to antidepressants and does not display consistent effects in animal models of anxiety and seems to exert potential antipsychotic effects.

Environmental variables differentially affect ethanol-stimulated activity in selectively bred mouse lines

The experiments confirm the importance of lighting condition, order of testing, dose, and route of administration in eliciting EtOH-stimulated open field activity in mice, and demonstrate a genotype-environment interaction, since the magnitude of difference between genetically selected lines varied as a function of the testing parameters chosen.

Developmental PBDE Exposure and IQ/ADHD in Childhood: A Systematic Review and Meta-analysis

There was sufficient evidence supporting an association between developmental PBDE exposure and reduced IQ, and the body of evidence was of “moderate” quality for ADHD with “limited” evidence for an association with PBDEs.



Antagonism of Depressant Activity of Ethanol by DH-524; a Comparative Study with Bemegride, Doxapram and d-Amphetamine

  • A. AbdallahD. Roby
  • Medicine
    Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine
  • 1975
The purpose of this study was to compare the effects of DH-524 (2(3,4-dichlorophenoxy)-methyl-2-imidazoline), bemegride, doxapram and d-amphetamine on the narcotic and hypothermic effect of ethanol in mice.

Depression of some drug-induced in vivo changes of cerebellar guanosine 3',5'-monophosphate by control of motor and respiratory responses.

It is concluded that a significant portion of the drug-induced changes in cerebellar cGMP content produced in vivo may be secondary to altered motor and/or respiratory actions of these drugs.

Antagonism of ethanol's central stimulation in mice by small doses of catecholamine-receptor agonists

Ethanol's behavioural stimulant action in mice can be largely suppressed by apomorphine or clonidine, drugs which in the small doses used probably inhibit central catecholamine (CA) neurons.

Selective Antagonism of Central Nervous System Depressants by DH-524; A Comparative Study with Bemegride

Data suggest that DH-524 would be more selective and have a wider margin of safety than the commonly used analeptics in the treatment of barbiturate or methaqualone overdose.

Stress-induced alterations of cyclic nucleotide levels in brain: Effects of centrally acting drugs

The results suggest that norepinephrine, serotonin, acetylcholine, or prostaglandins are not involved in the elevation of cGMP levels elicited by acute stress, and participation of other neurotransmitters, such as dopamine or GABA, cannot be excluded.

Alteration of ethanol-induced changes in locomotor activity by adrenergic blockers in mice

Results indicate that the SLMA-depressant effect of ETOH may be mediated by central “beta-type” receptors, that theSLMA-stimulant effect by ETOh may bemediated by central "alpha-type" receptors, and that at least part of EtoH's action may be due to dopaminergic mechanisms.

Thyrotropin-releasing hormone reversal of ethanol-induced decreases in cerebellar cGMP

It is reported here that decreases in cerebellar cGMP induced by ethanol are antagonised by administration of TRH and that administration ofTRH itself results in significant elevation in CerebellarcGMP.

Comparison of tyrosine hydroxylase and dopamine-Β-hydroxylase inhibition with the effects of various 6-hydroxydopamine treatments on d-amphetamine induced motor activity

In rats with chronic depletions of brain norepinephrine, dopamine, or both catecholamines produced by different 6-OHDA treatments, both amphetamine-stimulated motor activity and stereotyped behavior were antagonized by treatments reducing dopamine or bothcatecholamine but not in animals in which brain norpinephrine was reduced.