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Orexin receptor blockers: A tool for lowering alcohol intake and alcohol addictive behavior in the light of preclinical studies

Open Access
|Dec 2021

Figures & Tables

Summary of behavioral preclinical experiments using antagonists of OXR along with a brief description of some experimental details

AntagonistIn vitro study (Cellular measurements)In vivo (Proven action)ProcedureDose/AdministrationEffect specificityAuthor’s
SB-334867N/l+P female rat 2-bottle choice3, 10, or 30 mg/kg, i.p.N/l[4]
N/l-P female rat Operant progressive ratio N/l
N/l+Male C57BL/6 mice Binge drinking -

SB-334867++All procedures 15%EtOH Male C57BL/6 mice Binge drinking 20%EtOH5 mg/kg, i.p.N/l[48]

SB-334867N/l+Male P rat Operant progressive ratio 10%EtOH3 μg VTA+[61]

SB-334867N/l+Female P rat Operant progressive ratio for EtOH->PSR ->Relapse ->SB administration>PSR ->Relapse 15%EtOH10 or 20 mg/kg, i.p.N/l[59]

SB-334867++Male P rat Operant progressive ratio 10%EtOH5 or 10 mg/kg i.p.+[57]

SB-334867++Male C57BL/6 mice 2-bottle choice 15%EtOH0.3, 1, 3 or 10 mg/kg i.p.+[49]

SB-334867+mNAsh + mPFC +Male C57BL/6 mice Binge drinking 15%EtOH3 μg mNAsh and mPFC+[50]
+Male Long Evans rat Operant progressive ratio 20%EtOH N/l

SB-334867++Male P rat Operant responding ratio 10%EtOH20 mg/kg, i.p.+[58]

GSK1059865++Male C57BL/6 mice intermittent ethanol or air exposure in inhalation chambers 15%EtOH10, 25, 50 mg/kg i.p+[60]

SB-334867N/l+Male Wistar rat 2-bottle choice 10%EtOH3 ng, 6 ng NAcc-[44]

SB-334867N/l+Male Sprague Dawley rat 2-bottle choice 10%EtOH30 mg/kg, i.p.+[46]

SB-334867N/l+Male Sprague-Dawley rat Operant progressive ratio cue-induced reinstatement10, or 20 mg/kg i.p.+[47]
+20%EtOH

SB-334867++Male C57BL/6 mice Binge drinking 20%EtOH5 or 10 mg/kg, i.p.-[51]

SB-334867++Male C57BL/6 mice Binge drinking 20%EtOH6.0 pg VTA and CeA+[55]

SB-334867-+Male Long-Evans rat Operant progressive ratio 10%EtOH5, 10, 15, 20 mg/kg, i.p.+[43]

SB-408124+-Male DBA/2 mice CPP3, 10, 30 mg/kg, s.c.N/l[45]
-Male Wistar rat Operant progressive ratio
All procedures 8%EtOH

SB-334867+-Male DBA/2J mice CPP10, 15, 20, 30, 40 mg/kg, i.p.N/l[52]
20%EtOH

LSN2424100N/l-P female rat 2-bottle choice10 or 30 mg/kg, i.p.N/l[4]
N/l+P female rat Operant progressive ratio3, 10, 30 mg/kg i.pN/l
N/l+Male C57BL/6 mice Binge drinking5, 30, 60 mg/kg i.p-
All procedures 15%EtOH

TCS-OX2-29+aPVT + pPVT-Male Long-Evans rat 2-bottle-choice 20%EtOH10 nmol aPVT, pPVTaPVT + pPVT-[42]

TCS-OX2-29+NAcc + NAcsh -Male P rats cue-induced reinstatement of ethanol-seeking100 μg or 300 μg NAcsh or NAcc+[56]
+Operant responding ratio 10%EtOH

TCS-OX2-29+ Male C57BL/6 mice 2-bottle choice 15%EtOH3 or 10 mg/kg i.pN/l[49]

TCS-OX2-29+ Male C57BL/6 mice Binge drinking 15%EtOH3 μg mNAshN/l[50]
-Operant progressive ratio 20%EtOH N/l

TCS-OX2-29+ Male C57BL/6 mice Binge drinking 20%EtOH5.0, or 7.5 μg VTA, CeA-[55]

JNJ10397049+-Male DBA/2 mice CPP1, 3, and 10 mg/kg, s.c.+[45]
+Male Wistar rat Operant progressive ratio
All procedures 8%EtOH

AlmorexantN/l+P female rat 2-bottle choice60 or 100 mg/kg, i.p.N/l[4]
+P female rat Operant progressive ratio10, 30, or 60 mg/kg, i.p.N/l
+Male C57BL/6 mice Binge drinking5, 50, or 100 mg/kg, i.p.-
All procedures 15%EtOH

Almorexant+VTA + SN -Male Long-Evans rat Operant progressive ratio 20%EtOH3, 10 and 15 mg/kg, i.p. VTA and SN-[62]
Language: English
Page range: 959 - 969
Submitted on: Aug 16, 2020
Accepted on: Apr 16, 2021
Published on: Dec 29, 2021
Published by: Hirszfeld Institute of Immunology and Experimental Therapy
In partnership with: Paradigm Publishing Services
Publication frequency: 1 issue per year

© 2021 Kamila Czora-Poczwardowska, Radosław Kujawski, Julia Słyńko-Krzyżostaniak, Przemysław Ł. Mikołajczak, Michał Szulc, published by Hirszfeld Institute of Immunology and Experimental Therapy
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.