Ethanol and benzodiazepines. The influence of CGS 8216 on the ethanol-induced hypothermia and motor incoordination in mice and rats. 1995

S Fidecka, and R Langwínski
Department of Pharmacodynamics, Medical Academy, Lublin, Poland.

Ethanol has pharmacological profile very similar to benzodiazepines which facilitate GABA-ergic neurotransmission. In addition, a lot of ethanol-induced effects are partially antagonized by Ro 15-4513, a benzodiazepine inverse agonist. In our study, the influence of CGS 8216, another benzodiazepine inverse agonist, on the hypothermic (3.5 g/kg in mice, 3.0 g/kg in rats) and disturbing the motor coordination (3.2 g/kg in mice, 2.5 g/kg in rats, aerial righting reflex) effects of ethanol was investigated. The hypothermic effects of ethanol were antagonized in mice, and significantly attenuated in rats by CGS 8216 (10 and 20 mg/kg). Ethanol-induced motor incoordination was significantly diminished by 10 and 20 mg/kg of CGS 8216 in mice but not in rats. These data suggest that some effects of ethanol may result from the intensification of benzodiazepine/GABA-ergic activity. In addition, they let us presume that the activity of CGS 8216 is connected with a benzodiazepine receptor named BZ-1 or omega 1. The results indicate the need of further work on the benzodiazepine inverse agonists for use in treatment of ethanol poisoning.

UI MeSH Term Description Entries
D007036 Hypothermia, Induced Abnormally low BODY TEMPERATURE that is intentionally induced in warm-blooded animals by artificial means. In humans, mild or moderate hypothermia has been used to reduce tissue damages, particularly after cardiac or spinal cord injuries and during subsequent surgeries. Induced Hypothermia,Mild Hypothermia, Induced,Moderate Hypothermia, Induced,Targeted Temperature Management,Therapeutic Hypothermia,Hypothermia, Therapeutic,Induced Mild Hypothermia,Induced Mild Hypothermias,Induced Moderate Hypothermia,Induced Moderate Hypothermias,Mild Hypothermias, Induced,Moderate Hypothermias, Induced,Targeted Temperature Managements
D008297 Male Males
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D012018 Reflex An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
D001831 Body Temperature The measure of the level of heat of a human or animal. Organ Temperature,Body Temperatures,Organ Temperatures,Temperature, Body,Temperature, Organ,Temperatures, Body,Temperatures, Organ
D002492 Central Nervous System Depressants A very loosely defined group of drugs that tend to reduce the activity of the central nervous system. The major groups included here are ethyl alcohol, anesthetics, hypnotics and sedatives, narcotics, and tranquilizing agents (antipsychotics and antianxiety agents). CNS Depressants,Depressants, CNS
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004856 Postural Balance A POSTURE in which an ideal body mass distribution is achieved. Postural balance provides the body carriage stability and conditions for normal functions in stationary position or in movement, such as sitting, standing, or walking. Postural Control,Posture Balance,Posture Control,Posture Equilibrium,Balance, Postural,Musculoskeletal Equilibrium,Postural Equilibrium,Balance, Posture,Control, Postural,Control, Posture,Equilibrium, Musculoskeletal,Equilibrium, Postural,Equilibrium, Posture,Postural Controls,Posture Balances,Posture Controls,Posture Equilibriums
D000431 Ethanol A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES. Alcohol, Ethyl,Absolute Alcohol,Grain Alcohol,Alcohol, Absolute,Alcohol, Grain,Ethyl Alcohol
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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