A novel positive modulator of α4-GABAA receptors, XHe-III-74, reduces ethanol intake in mouse „drinking in the dark“ model

2018 ◽  
Author(s):  
Bojan Batinic
Keyword(s):  
Gabaa Receptors ◽  
Ethanol Intake ◽  
Positive Modulator ◽  
Drinking In The Dark

Androstenol (5α-androst-16-en-3α-ol) Is a Novel Neurosteroid Positive Modulator of GABAA Receptors: In Vitro and In Vivo Studies

NeuroRx ◽  
2006 ◽  
Vol 3 (3) ◽  
pp. 413-414
Author(s):  
R KAMINSKI ◽  
H MARINI ◽  
P ORTINSKI ◽  
W YONEKAWA ◽  
S VICINI ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
In Vivo Studies ◽  
Positive Modulator

scholarly journals Effects of Tacrolimus and Other Immune Targeting Compounds on Binge-Like Ethanol Drinking in High Drinking in the Dark Mice

2020 ◽  
Vol 15 ◽  
pp. 263310552097541
Author(s):  
Kolter B Grigsby ◽  
Antonia M Savarese ◽  
Pamela Metten ◽  
Barbara J Mason ◽  
Yuri A Blednov ◽  
...  
Keyword(s):  
Risk Model ◽  
Ethanol Intake ◽  
Blood Alcohol ◽  
Saccharin Intake ◽  
Ethanol Drinking ◽  
Wide Range ◽  
Blood Alcohol Levels ◽  
Drinking In The Dark ◽  
Compare And Contrast

High Drinking in the Dark (HDID-1) mice represent a unique genetic risk model of binge-like drinking and a novel means of screening potential pharmacotherapies to treat alcohol use disorders (AUDs). We tested the effects of tacrolimus (0, 0.5, 1, and 2 mg/kg), sirolimus (0, 5, 10, and 20 mg/kg), palmitoylethanolamide (PEA; 0, 75, 150, and 225 mg/kg), and secukinumab (0, 5, 20, and 60 mg/kg) on binge-like ethanol intake (2-day, “Drinking in the Dark” [DID]) and blood alcohol levels (BALs) in HDID-1 mice. Tacrolimus reduced ethanol intake and BALs. Tacrolimus had no effect on water intake, but reduced saccharin intake. There was no effect of sirolimus, PEA, or secukinumab on ethanol intake or BALs. These results compare and contrast with previous work addressing these compounds or their targeted mechanisms of action on ethanol drinking, highlighting the importance of screening a wide range of models and genotypes to inform the role of neuroimmune signaling in AUDs.

scholarly journals Neurosteroid Modulators of GABAA Receptors Differentially Modulate Ethanol Intake Patterns in Male C57BL/6J Mice

2005 ◽  
Vol 29 (9) ◽  
pp. 1630-1640 ◽  
Author(s):  
Matthew M. Ford ◽  
Jeffrey D. Nickel ◽  
Tamara J. Phillips ◽  
Deborah A. Finn
Keyword(s):  
Gabaa Receptors ◽  
Ethanol Intake

Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate is a novel positive modulator of GABAA receptors

2005 ◽  
Vol 516 (3) ◽  
pp. 204-211 ◽  
Author(s):  
Maria Paola Mascia ◽  
Battistina Asproni ◽  
Fabio Busonero ◽  
Giuseppe Talani ◽  
Elisabetta Maciocco ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
Positive Modulator

A42 WEAK ANXIOLYTIC-LIKE PROFILE OF SB-205384, A SELECTIVE POSITIVE MODULATOR OF ??3??2??2 GABAA RECEPTORS

2005 ◽  
Vol 16 (Supplement 1) ◽  
pp. S36-S37
Author(s):  
R.J. Rodgers ◽  
C.N. Johnson ◽  
C. Ruckledge
Keyword(s):  
Gabaa Receptors ◽  
Positive Modulator

scholarly journals Corticotropin Releasing Factor Type 1 and 2 Receptor Signaling in the Medial Prefrontal Cortex Modulates Binge-Like Ethanol Consumption in C57BL/6J Mice

2019 ◽  
Vol 9 (7) ◽  
pp. 171 ◽  
Author(s):  
Stacey L. Robinson ◽  
Carlos A. Perez-Heydrich ◽  
Todd E. Thiele
Keyword(s):  
Prefrontal Cortex ◽  
Medial Prefrontal Cortex ◽  
Ethanol Consumption ◽  
Inhibitory Effect ◽  
Ethanol Intake ◽  
Corticotropin Releasing Factor ◽  
Factor Type ◽  
Drinking In The Dark

Corticotropin releasing factor (CRF) signaling via limbic CRF1 and 2 receptors (CRF1R and CRF2R, respectively) is known to modulate binge-like ethanol consumption in rodents. Though CRF signaling in the medial prefrontal cortex (mPFC) has been shown to modulate anxiety-like behavior and ethanol seeking, its role in binge ethanol intake is unknown. Here, we used “drinking-in-the-dark” (DID) procedures in male and female C57BL/6J mice to address this gap in the literature. First, the role of CRF1R and CRF2R signaling in the mPFC on ethanol consumption was evaluated through site-directed pharmacology. Next, we evaluated if CRF1R antagonist reduction of binge-intake was modulated in part through CRF2R activation by co-administration of a CRF1R and CRF2R antagonist. Intra-mPFC inhibition of CRF1R and activation of CRF2R resulted in decreased binge-like ethanol intake. Further, the inhibitory effect of the CRF1R antagonist was attenuated by co-administration of a CRF2R antagonist. We provide novel evidence that (1) inhibition of CRF1R or activation of CRF2R in the mPFC reduces binge-like ethanol intake; and (2) the effect of CRF1R antagonism may be mediated via enhanced CRF2R activation. These observations provide the first direct behavioral pharmacological evidence that CRF receptor activity in the mPFC modulates binge-like ethanol consumption.

scholarly journals Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit

2016 ◽  
Vol 791 ◽  
pp. 433-443 ◽  
Author(s):  
Tamara Timić Stamenić ◽  
Michael M. Poe ◽  
Sabah Rehman ◽  
Anja Santrač ◽  
Branka Divović ◽  
...  
Keyword(s):  
Gabaa Receptors ◽  
Kinetic Behavior ◽  
Positive Modulator

The Pheromone Androstenol (5α-Androst-16-en-3α-ol) Is a Neurosteroid Positive Modulator of GABAA Receptors

2006 ◽  
Vol 317 (2) ◽  
pp. 694-703 ◽  
Author(s):  
Rafal M. Kaminski ◽  
Herbert Marini ◽  
Pavel I. Ortinski ◽  
Stefano Vicini ◽  
Michael A. Rogawski
Keyword(s):  
Gabaa Receptors ◽  
Positive Modulator
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