The selective kappa-opioid receptor agonist U50,488H attenuates voluntary ethanol intake in the rat.
paper
Cited
Public
Unavailable
- Authors
- Lindholm, S; Werme, M; BrenΓ©, S; Franck, J
- Year
- 2001
- Journal
- Behavioural brain research
- PMID
- 11182162
- DOI
- 10.1016/s0166-4328(00)00368-5
Non-selective opioid receptor antagonists are increasingly used in the treatment of alcohol dependence. The clinical effects are significant but the effect size is rather small and unpleasant side effects may limit the benefits of the compounds. Ligands acting at mu- and/or delta- receptors can alter the voluntary intake of ethanol in various animal models. Therefore, the attenuating effects of selective opioid receptor ligands on ethanol intake may be of clinical interest in the treatment of alcoholism. The objective of this study was to examine the effects of a selective kappa-receptor agonist, U50,488H on voluntary ethanol intake in the rat. We used a restricted access model with a free choice between an ethanol solution (10% v/v) and water. During the 3-days baseline period, the rats received a daily saline injection (1 ml/kg, i.p.) 15 min before the 2 h access to ethanol. The animals had free access to water at all times. The control group received a daily saline injection during the 4-days treatment-period, whereas the treatment groups received a daily dose of U50,488H (2.5, 5.0 or 10 mg/kg per day). Animals treated with U50,488H dose-dependently decreased their ethanol intake. The effect of the highest dose of U50,488H was reduced by pre-treatment with the selective kappa-antagonist nor-binaltorphimine (nor-BNI). These results demonstrate that activation of kappa-opioid receptors can attenuate voluntary ethanol intake in the rat, and the data suggest that the brain dynorphin/kappa-receptor systems may represent a novel target for pharmacotherapy in the treatment of alcohol dependence.
No figures extracted from this document.
No chunks β full text not yet ingested.
No entities extracted from this document yet.
No uploaded files.
Not in any collection.
No citations found.
In this knowledge base
External
| Title | Authors | Journal | Year | Link |
|---|---|---|---|---|
| Effects of kappa-opioid receptor stimulation on addiction-related behavior in female rats: differences along the rostro-caudal axis of the nucleus accumbens shell. | Hawks A et al. | β | 2026 | β |
| Kappa opioid receptor control of motivated behavior revisited. | Farahbakhsh ZZ et al. | β | 2026 | β |
| Modulatory effects of orexin and dynorphin on stress-related alcohol seeking and relapse: pivotal role of the posterior paraventricular nucleus of the thalamus. | Holguin G et al. | β | 2026 | β |
| Interaction between corticotropin-releasing factor, orexin, and dynorphin in the infralimbic cortex may mediate exacerbated alcohol-seeking behavior. | Flores-Ramirez FJ et al. | β | 2024 | β |
| Opioid modulation of prefrontal cortex cells and circuits. | Cole RH et al. | β | 2024 | β |
| A critical review of effects on ethanol intake of the dynorphin/kappa opioid receptor system in the extended amygdala: From inhibition to stimulation. | Pirino BE et al. | β | 2023 | β |
| Insula Dynorphin and Kappa Opioid Receptor Systems Regulate Alcohol Drinking in a Sex-Specific Manner in Mice. | Pina MM et al. | β | 2023 | β |
| Systemic kappa opioid receptor antagonism accelerates reinforcement learning via augmentation of novelty processing in male mice. | Farahbakhsh ZZ et al. | β | 2023 | β |
| Pain-induced alterations in the dynorphinergic system within the mesocorticolimbic pathway: Implication for alcohol addiction. | Lorente JD et al. | β | 2022 | β |
| Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist. | Zhou Y et al. | β | 2022 | β |
| Kappa opioid receptors in the bed nucleus of the stria terminalis regulate binge-like alcohol consumption in male and female mice. | Haun HL et al. | β | 2020 | β |
| Nicotine and alcohol: the role of midbrain dopaminergic neurons in drug reinforcement. | Morel C et al. | β | 2019 | β |
| Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine. | Kaski SW et al. | β | 2019 | β |
| Prenatal ethanol exposure and enkephalinergic neurotransmission. | MΓ©ndez M et al. | β | 2019 | β |
| Age as a factor in stress and alcohol interactions: A critical role for the kappa opioid system. | Diaz MR et al. | β | 2018 | β |
| Contribution of Dynorphin and Orexin Neuropeptide Systems to the Motivational Effects of Alcohol. | Anderson RI et al. | β | 2018 | β |
| Involvement of Activated Brain Stress Responsive Systems in Excessive and "Relapse" Alcohol Drinking in Rodent Models: Implications for Therapeutics. | Zhou Y et al. | β | 2018 | β |
| Preclinical evaluation of the kappa-opioid receptor antagonist CERC-501 as a candidate therapeutic for alcohol use disorders. | Domi E et al. | β | 2018 | β |
| The ΞΊ-opioid receptor antagonist JDTic decreases ethanol intake in alcohol-preferring AA rats. | Uhari-VÀÀnΓ€nen J et al. | β | 2018 | β |
| Dynorphin/Kappa Opioid Receptor Signaling in Preclinical Models of Alcohol, Drug, and Food Addiction. | Karkhanis A et al. | β | 2017 | β |
| Nicotine Increases Alcohol Intake in Adolescent Male Rats. | LΓ‘rraga A et al. | β | 2017 | β |
| Prenatal ethanol exposure modifies locomotor activity and induces selective changes in Met-enk expression in adolescent rats. | Abate P et al. | β | 2017 | β |
| Role of the Dynorphin/Kappa Opioid Receptor System in the Motivational Effects of Ethanol. | Anderson RI et al. | β | 2017 | β |
| Synergistic blockade of alcohol escalation drinking in mice by a combination of novel kappa opioid receptor agonist Mesyl Salvinorin B and naltrexone. | Zhou Y et al. | β | 2017 | β |
| The phosphodiesterase-4 inhibitor roflumilast decreases ethanol consumption in C57BL/6J mice. | Liu X et al. | β | 2017 | β |
| Accumbal ΞΌ-Opioid Receptors Modulate Ethanol Intake in Alcohol-Preferring Alko Alcohol Rats. | Uhari-VÀÀnΓ€nen J et al. | β | 2016 | β |
| Early-Life Social Isolation Stress Increases Kappa Opioid Receptor Responsiveness and Downregulates the Dopamine System. | Karkhanis AN et al. | β | 2016 | β |
| Kappa-opioid receptors differentially regulate low and high levels of ethanol intake in female mice. | Van't Veer A et al. | β | 2016 | β |
| Switch from excitatory to inhibitory actions of ethanol on dopamine levels after chronic exposure: Role of kappa opioid receptors. | Karkhanis AN et al. | β | 2016 | β |
| The kappa-opioid receptor antagonist, nor-binaltorphimine (nor-BNI), decreases morphine withdrawal and the consequent conditioned place aversion in rats. | Kelsey JE et al. | β | 2015 | β |
| The opioid receptors as targets for drug abuse medication. | Noble F et al. | β | 2015 | β |
| Alcohol: a stimulant activating brain stress responsive systems with persistent neuroadaptation. | Zhou Y et al. | β | 2014 | β |
| A molecular prospective provides new insights into implication of PDYN and OPRK1 genes in alcohol dependence. | Faisal M et al. | β | 2014 | β |
| Brief prenatal ethanol exposure alters behavioral sensitivity to the kappa opioid receptor agonist (U62,066E) and antagonist (Nor-BNI) and reduces kappa opioid receptor expression. | Nizhnikov ME et al. | β | 2014 | β |
| Effects of systemic opioid receptor ligands on ethanol- and sucrose seeking and drinking in alcohol-preferring (P) and Long Evans rats. | Henderson-Redmond A et al. | β | 2014 | β |
| Effects of the kappa opioid receptor antagonist, nor-binaltorphimine, on ethanol intake: impact of age and sex. | Morales M et al. | β | 2014 | β |
| Prenatal ethanol exposure alters met-enkephalin expression in brain regions related with reinforcement: possible mechanism for ethanol consumption in offspring. | Abate P et al. | β | 2014 | β |
| The kappa opioid receptor: from addiction to depression, and back. | Lalanne L et al. | β | 2014 | β |
| Effects of voluntary alcohol drinking on corticotropin-releasing factor and preprodynorphin mRNA levels in the central amygdala of Sardinian alcohol-preferring rats. | Zhou Y et al. | β | 2013 | β |
| Long-term ethanol effects on acute stress responses: modulation by dynorphin. | RΓ‘cz I et al. | β | 2013 | β |
| Stress, ΞΊ manipulations, and aversive effects of ethanol in adolescent and adult male rats. | Anderson RI et al. | β | 2013 | β |
| ΞΊ-Opioid receptors in the central amygdala regulate ethanol actions at presynaptic GABAergic sites. | Kang-Park M et al. | β | 2013 | β |
| Alcohol-induced plasticity in the dynorphin/kappa-opioid receptor system. | Sirohi S et al. | β | 2012 | β |
| Differences in basal and ethanol-induced levels of opioid peptides in Wistar rats from five different suppliers. | Palm S et al. | β | 2012 | β |
| Early role of the ΞΊ opioid receptor in ethanol-induced reinforcement. | Pautassi RM et al. | β | 2012 | β |
| Electroacupuncture decreases excessive alcohol consumption involving reduction of FosB/ΞFosB levels in reward-related brain regions. | Li J et al. | β | 2012 | β |
| Increased ethanol intake in prodynorphin knockout mice is associated to changes in opioid receptor function and dopamine transmission. | FemenΓa T et al. | β | 2012 | β |
| Naloxone attenuation of ethanol-reinforced operant responding in infant rats in a re-exposure paradigm. | Miranda-Morales RS et al. | β | 2012 | β |
| Ontogenetic differences in ethanol's motivational properties during infancy. | Nizhnikov ME et al. | β | 2012 | β |
| Opioidergic modulation of ethanol self-administration in the ventral pallidum. | Kemppainen H et al. | β | 2012 | β |
| Role of mu, delta and kappa opioid receptors in ethanol-reinforced operant responding in infant rats. | Miranda-Morales RS et al. | β | 2012 | β |
| Targeting dynorphin/kappa opioid receptor systems to treat alcohol abuse and dependence. | Walker BM et al. | β | 2012 | β |
| The dynorphin/ΞΊ-opioid receptor system and its role in psychiatric disorders. | Tejeda HA et al. | β | 2012 | β |
| The kappa opioid receptor antagonist JDTic attenuates alcohol seeking and withdrawal anxiety. | Schank JR et al. | β | 2012 | β |
| ΞΊ-Opioid receptors within the nucleus accumbens shell mediate pair bond maintenance. | Resendez SL et al. | β | 2012 | β |
| Alcohol dependence, disinhibited behavior and variation in the prodynorphin gene. | Flory JD et al. | β | 2011 | β |
| Effects of corticotropin-releasing hormone receptor antagonists on the ethanol-induced increase of dynorphin A1-8 release in the rat central amygdala. | Lam MP et al. | β | 2011 | β |
| Fine mapping quantitative trait loci that influence alcohol preference behavior in the High and Low Alcohol Preferring (HAP and LAP) mice. | Bice PJ et al. | β | 2011 | β |
| Mice lacking adenylyl cyclase type 5 (AC5) show increased ethanol consumption and reduced ethanol sensitivity. | Kim KS et al. | β | 2011 | β |
| Differential role of mu, delta and kappa opioid receptors in ethanol-mediated locomotor activation and ethanol intake in preweanling rats. | Arias C et al. | β | 2010 | β |
| Endogenous kappa-opioid mediation of stress-induced potentiation of ethanol-conditioned place preference and self-administration. | Sperling RE et al. | β | 2010 | β |
| Ethanol action on dopaminergic neurons in the ventral tegmental area: interaction with intrinsic ion channels and neurotransmitter inputs. | Morikawa H et al. | β | 2010 | β |
| Opioids in the hypothalamic paraventricular nucleus stimulate ethanol intake. | Barson JR et al. | β | 2010 | β |
| The role of the dynorphin-kappa opioid system in the reinforcing effects of drugs of abuse. | Wee S et al. | β | 2010 | β |
| Blockade of ethanol reward by the kappa opioid receptor agonist U50,488H. | Logrip ML et al. | β | 2009 | β |
| Effect of acute ethanol administration on the release of opioid peptides from the midbrain including the ventral tegmental area. | Jarjour S et al. | β | 2009 | β |
| Opioid antagonists block the acquisition of ethanol-mediated conditioned tactile preference in infant rats. | Nizhnikov ME et al. | β | 2009 | β |
| The Central Reinforcing Properties of Ethanol Are Mediated by Endogenous Opioid Systems: Effects of Mu and Kappa Opioid Antagonists. | Nizhnikov ME et al. | β | 2009 | β |
| The kappa-opiate receptor impacts the pathophysiology and behavior of substance use. | Mysels D et al. | β | 2009 | β |
| A novel delta opioid receptor antagonist, SoRI-9409, produces a selective and long-lasting decrease in ethanol consumption in heavy-drinking rats. | Nielsen CK et al. | β | 2008 | β |
| A regulatory variation in OPRK1, the gene encoding the kappa-opioid receptor, is associated with alcohol dependence. | Edenberg HJ et al. | β | 2008 | β |
| Differences in ethanol drinking between mice selected for high and low swim stress-induced analgesia. | Sacharczuk M et al. | β | 2008 | β |
| Dynorphin is a downstream effector of striatal BDNF regulation of ethanol intake. | Logrip ML et al. | β | 2008 | β |
| Shared mechanisms of alcohol and other drugs. | Cruz MT et al. | β | 2008 | β |
| Dynorphin and the pathophysiology of drug addiction. | Shippenberg TS et al. | β | 2007 | β |
| Ethanol alters the effect of kappa receptor ligands on dopamine release in the nucleus accumbens. | Lindholm S et al. | β | 2007 | β |
| A microdialysis profile of dynorphin A(1-8) release in the rat nucleus accumbens following alcohol administration. | Marinelli PW et al. | β | 2006 | β |
| Anxiety and ethanol consumption in victorious and defeated mice; effect of kappa-opioid receptor activation. | Kudryavtseva N et al. | β | 2006 | β |
| Association of the kappa-opioid system with alcohol dependence. | Xuei X et al. | β | 2006 | β |
| Endogenous kappa opioid receptor systems modulate the responsiveness of mesoaccumbal dopamine neurons to ethanol. | Zapata A et al. | β | 2006 | β |
| Kappa-opioid receptor modulation of accumbal dopamine concentration during operant ethanol self-administration. | Doyon WM et al. | β | 2006 | β |
| Reduced alcohol consumption in mice lacking preprodynorphin. | Blednov YA et al. | β | 2006 | β |
| Reinforcing properties of ethanol in neonatal rats: involvement of the opioid system. | Nizhnikov ME et al. | β | 2006 | β |
| A single injection of the kappa opioid antagonist norbinaltorphimine increases ethanol consumption in rats. | Mitchell JM et al. | β | 2005 | β |
| Decreased oral self-administration of alcohol in kappa-opioid receptor knock-out mice. | Kovacs KM et al. | β | 2005 | β |
| Nalmefene induced elevation in serum prolactin in normal human volunteers: partial kappa opioid agonist activity? | Bart G et al. | β | 2005 | β |
| Systemic and intra-accumbens microinjections of naltrexone interfere with tolerance to ethanol in rats. | Varaschin RK et al. | β | 2005 | β |
| The "ups and downs" of signaling cascades in addiction. | Ron D et al. | β | 2005 | β |
| Pharmacogenetic studies of alcohol self-administration and withdrawal. | Crabbe JC et al. | β | 2004 | β |
| Predictors of high ethanol consumption in RIIbeta knock-out mice: assessment of anxiety and ethanol-induced sedation. | Fee JR et al. | β | 2004 | β |
| Effects of single and dual administration of cocaine and ethanol on opioid and ORL1 receptor expression in rat CNS: an autoradiographic study. | Rosin A et al. | β | 2003 | β |
| Variants of kappa-opioid receptor gene and mRNA in alcohol-preferring and alcohol-avoiding mice. | Saito M et al. | β | 2003 | β |
| Endogenous opiates and behavior: 2001. | Bodnar RJ et al. | β | 2002 | β |