Publication Title: 
Journal of Neuroscience Research

It is widely accepted that the GABAergic system plays an important role in the action of ethanol in vivo. GABA transporter subtype 1 (GAT1) constructs high affinity reuptake sites in the CNS and regulates GABAergic transmissions. In this study, mice lacking the GAT1 were developed by homologous recombination. Both hetero- and homozygous GAT1 mutant mice were tested for ethanol, saccharin or quinine consumption, ethanol-conditioned place preference, ethanol-conditioned taste aversion, ethanol-simulated motor activity, and ethanol-induced sedation/hypnosis.

Cai, You-Qing
Cai, Guo-Qiang
Liu, Guo-Xiang
Cai, Qing
Shi, Jia-Hao
Shi, Jun
Ma, Sun-Kai
Sun, Xia
Sheng, Zhe-Jin
Mei, Zhen-Tong
Cui, Dafu
Guo, Lihe
Wang, Zhugang
Fei, Jian
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Despite the pervasiveness of alcohol (ethanol) use, it is unclear how the multiple molecular targets for ethanol contribute to its many behavioral effects. The function of GABA type A receptors (GABA(A)-Rs) is altered by ethanol, but there are multiple subtypes of these receptors, and thus far, individual subunits have not been definitively linked with specific behavioral actions. The alpha1 subunit of the GABA(A)-R is the most abundant alpha subunit in the brain, and the goal of this study was to determine the role of receptors containing this subunit in alcohol action.

Werner, David F.
Blednov, Yuri A.
Ariwodola, Olusegun J.
Silberman, Yuval
Logan, Exazevia
Berry, Raymond B.
Borghese, Cecilia M.
Matthews, Douglas B.
Weiner, Jeffrey L.
Harrison, Neil L.
Harris, R. Adron
Homanics, Gregg E.
Publication Title: 
Anesthesia and Analgesia

Recent pharmacological studies suggest that N-methyl-D-aspartate (NMDA) receptors play an important role in neuroadaptive processes in the development of tolerance to addictive drugs, such as opioids, amphetamine, and cocaine. In the present study, we investigated the contribution of the NMDA receptor to ethanol-induced hypnotic tolerance using NMDA receptor epsilon1 subunit knockout mice. Hypnotic sensitivity to a single injection of 3, 3.5, and 4 g/kg ethanol was not significantly different between wild-type mice and NMDA receptor epsilon1 subunit knockout mice.

Sato, Yuki
Seo, Norimasa
Kobayashi, Eiji
Publication Title: 
Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology

GABA(A) receptors mediate both fast phasic inhibitory postsynaptic potentials and slower tonic extrasynaptic inhibition. Hyperpolarizing phasic GABAergic inhibition requires the activity of neuron-specific chloride-extruding potassium-chloride cotransporter KCC2 in adult CNS. However, the possible role of KCC2 in tonic GABAergic inhibition and the associated behaviors is unknown.

Tornberg, Janne
Segerstråle, Mikael
Kulesskaya, Natalia
Voikar, Vootele
Taira, Tomi
Airaksinen, Matti S.
Publication Title: 
Alcoholism, Clinical and Experimental Research

BACKGROUND: Increasing evidence supports a role for 5-hydroxytryptamine (5-HT) and the 5-HT transporter (5-HTT) in modulating the neural and behavioral actions of ethanol (EtOH) and other drugs of abuse. METHODS: We used a 5-HTT knockout (KO) mouse model to further study this relationship. 5-Hydroxytryptamine transporter KO mice were tested for the sedative/hypnotic, hypothermia-inducing, motor-incoordinating (via accelerating rotarod), and depression-related (via tail suspension test) effects of acute EtOH administration.

Boyce-Rustay, Janel M.
Wiedholz, Lisa M.
Millstein, Rachel A.
Carroll, Jenna
Murphy, Dennis L.
Daws, Lynette C.
Holmes, Andrew
Publication Title: 
Indian Journal of Experimental Biology

Rosa damascena has been found to act on central nervous system including brain. It inhibits the reactivity of the hypothalamous and pituitary systems in rat. In traditional medicine hypnotic effect of Rose is also suggested. In the present study hypnotic effect of ethanolic, aqueous and chloroformic extracts of R. damascena was investigated in mice. Hypnotic method was based on potentiation of pentobarbital induced sleeping time by extracts. Three doses of extracts (100, 500 and 1000 mg/kg) were injected i.p.

Rakhshandah, H.
Hosseini, M.
Publication Title: 
Pharmacology, Biochemistry, and Behavior

This study was undertaken to evaluate the psychopharmacological effects in mice of the hydroethanolic extract (HE), aqueous, hexane and ethyl acetate (EA) fractions, and 6-methoxy-7-prenyloxycoumarin, three dihydrostyryl-2-pyrones and three styryl-2-pyrones isolated from Polygala sabulosa (Polygalaceae), a folk medicine used as a topical anesthetic. In the elevated plus-maze test (EPM), the HE of P.

Duarte, Filipe Silveira
Duzzioni, Marcelo
Mendes, Beatriz Garcia
Pizzolatti, Moacir Geraldo
de Lima, Thereza Christina Monteiro
Publication Title: 
Alcoholism, Clinical and Experimental Research

BACKGROUND: Emerging evidence implicates metabotropic glutamate receptor (mGluR) function in the neurobiological effects of ethanol. The recent development of subtype specific mGluR antagonists has made it possible to examine the roles of specific mGluRs in biochemical and behavioral responses to ethanol. The purpose of the present study was to determine if mGluRs modulate the acute sedative-hypnotic properties of ethanol in mice.

Sharko, Amanda C.
Hodge, Clyde W.
Publication Title: 
British Journal of Pharmacology

Despite the generally held view that alcohol is an unspecific pharmacological agent, recent molecular pharmacology studies demonstrated that alcohol has only a few known primary targets. These are the NMDA, GABA(A), glycine, 5-hydroxytryptamine 3 (serotonin) and nicotinic ACh receptors as well as L-type Ca(2+) channels and G-protein-activated inwardly rectifying K(+) channels.

Vengeliene, V.
Bilbao, A.
Molander, A.
Spanagel, R.
Publication Title: 
Journal of Pharmacological Sciences

Nociceptin/orphanin FQ peptide (NOP)-receptor agonists have been shown to produce anxiolytic-like effects in rodents subjected to various behavioral assays. Recently, we developed a new nonpeptide agonist of the NOP receptor, 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole (MCOPPB), as an anxiolytic agent.

Hirao, Akiko
Imai, Aki
Sugie, Yutaka
Yamada, Yoshinari
Hayashi, Shigeo
Toide, Katsuo


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