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Dopamine D1 vs D5 receptor-dependent induction of seizures in relation to DARPP-32, ERK1/2 and GluR1-AMPA signallingGerard J O'Sullivan
Molecular and Cellular Therapeutics and RCSI Research Institute, Royal College of Surgeons in Ireland, Dublin 2, Ireland
Neuropharmacology 54:1051-61. 2008..These findings indicate that D(1), and to a lesser extent D(5), receptor coupling to DARPP-32, ERK1/2 and glutamatergic signalling is involved in mediating the convulsant effects of SKF 83822...
Varenicline reduces alcohol self-administration in heavy-drinking smokersSherry A McKee
Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut 06519, USA
Biol Psychiatry 66:185-90. 2009..Varenicline, a partial nicotinic agonist with high affinity for the alpha4beta2 nAChR receptor, reduced ethanol intake in rodents. We aimed to test whether varenicline would reduce alcohol consumption and alcohol craving in humans...
Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seekingPia Steensland
Ernest Gallo Clinic and Research Center, University of California, San Francisco, 5858 Horton Street, Suite 200, Emeryville, CA 94608, USA
Proc Natl Acad Sci U S A 104:12518-23. 2007..The selectivity of varenicline in decreasing ethanol consumption combined with its reported safety profile and mild side effects in humans suggest that varenicline may prove to be a treatment for alcohol dependence...
Multicenter, placebo-controlled trial of lorcaserin for weight managementSteven R Smith
Translational Research Institute for Metabolism and Diabetes, Florida Hospital and the Sanford Burnham Institute, Winter Park, FL 32789, USA
N Engl J Med 363:245-56. 2010..Lorcaserin is a selective serotonin 2C receptor agonist that could be useful in reducing body weight...
Long-term heart rate reduction induced by the selective I(f) current inhibitor ivabradine improves left ventricular function and intrinsic myocardial structure in congestive heart failurePaul Mulder
INSERM U644, , Rouen, France
Circulation 109:1674-9. 2004..The improvement of cardiac function is related not only to the HRR per se but also to modifications in the extracellular matrix and/or function of myocytes as a consequence of long-term HRR...
Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and womenSteven R Smith
Pennington Biomedical Research Center, Louisiana State University System, Baton Rouge, Louisiana, USA
Obesity (Silver Spring) 17:494-503. 2009..Lorcaserin was well tolerated and efficacious for weight reduction in this 12-week study. Longer-term trials employing behavior modification will be needed to more fully assess its safety and efficacy...
Varenicline and suicidal behaviour: a cohort study based on data from the General Practice Research DatabaseD Gunnell
University of Bristol, Department of Social Medicine, University of Bristol, Bristol BS8 2PS
BMJ 339:b3805. 2009..To determine whether varenicline, a recently licensed smoking cessation product, is associated with an increased risk of suicide and suicidal behaviour compared with alternative treatments bupropion and nicotine replacement therapy...
Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterizationWilliam J Thomsen
Arena Pharmaceuticals, Inc, 6166 Nancy Ridge Dr, San Diego, CA 92121, USA
J Pharmacol Exp Ther 325:577-87. 2008..Upon discontinuation, body weight returned to control levels. These data demonstrate lorcaserin to be a potent, selective, and efficacious agonist of the 5-HT(2C) receptor, with potential for the treatment of obesity...
Efficacy and safety of varenicline for smoking cessation in patients with cardiovascular disease: a randomized trialNancy A Rigotti
General Medicine Division, Department of Medicine, Massachusetts General Hospital, Harvard Medical School, Tobacco Research and Treatment Center, Boston, Mass 02114, USA
Circulation 121:221-9. 2010..Varenicline, a partial alpha4beta2 nicotinic acetylcholine receptor agonist, is effective for smoking cessation in healthy smokers, but its efficacy and safety in smokers with cardiovascular disease are unknown...
The smoking cessation medication varenicline attenuates alcohol and nicotine interactions in the rat mesolimbic dopamine systemMia Ericson
Institute of Neuroscience and Physiology, the Sahlgrenska Academy at University of Gothenburg, Gothenburg, Sweden
J Pharmacol Exp Ther 329:225-30. 2009....
Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognitionHans Rollema
Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
Biochem Pharmacol 78:813-24. 2009....
Adverse effects and tolerability of medications for the treatment of tobacco use and dependenceJ Taylor Hays
Mayo Clinic Nicotine Dependence Center, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA
Drugs 70:2357-72. 2010..Given these factors, the benefit : risk ratio is strongly in favour of pharmacotherapy for tobacco dependence treatment in virtually all smokers who are motivated to quit...
Varenicline ameliorates ethanol-induced deficits in learning in C57BL/6 miceDanielle Gulick
Department of Psychology, Neuroscience Program, Temple University, Weiss Hall, Rm 865, 1701 N 13th Street, Philadelphia, PA 19122, USA
Neurobiol Learn Mem 90:230-6. 2008..In addition, varenicline did not alter blood alcohol concentration. The smoking cessation aid varenicline may have therapeutic uses for treating ethanol-associated disruptions in cognitive processes...
Impact of symptoms experienced by varenicline users on tobacco treatment in a real world settingAbigail C Halperin
University of Washington, Seattle, 1107 NE 45th Street, Suite 345, Seattle, WA 98105, USA
J Subst Abuse Treat 36:428-34. 2009..21%, p < .01). Counseling may improve tolerance of this medication and reduce the rate of discontinuation due to side effects...
Smoking cessation efficacy and safety of varenicline, an alpha4beta2 nicotinic receptor partial agonistSerena Tonstad
Department of Preventive Cardiology, Ulleval University Hospital, Oslo, Norway
J Cardiovasc Nurs 21:433-6. 2006..Phase 3 studies have evaluated the effects of varenicline on inducing smoking cessation and maintaining smoking abstinence...
Dopamine receptors regulate NMDA receptor surface expression in prefrontal cortex neuronsCan Gao
Department of Neuroscience, Rosalind Franklin University of Medicine and Science, North Chicago, Illinois 60064 3095, USA
J Neurochem 106:2489-501. 2008..Our results show that tyrosine phosphorylation plays an important role in the trafficking of NR2B-containing NMDA receptors in PFC neurons and the regulation of their trafficking by DA receptors...
Partial agonists of the α3β4* neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in ratsSusmita Chatterjee
Ernest Gallo Clinic and Research Center, University of California San Francisco, Emeryville, CA 94608, USA
Neuropsychopharmacology 36:603-15. 2011..CP-601932 has been shown to be safe in humans and may represent a potential novel treatment for AUDs...
Psychiatric adverse events in randomized, double-blind, placebo-controlled clinical trials of varenicline: a pooled analysisSerena Tonstad
Department of Preventive Cardiology, Oslo University Hospital Ulleval, Oslo, Norway
Drug Saf 33:289-301. 2010..In postmarketing surveillance, neuropsychiatric symptoms have appeared; however, their incidence and causal relationship to varenicline is not known...
Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trialDavid Gonzales
Smoking Cessation Center, Department of Medicine, Oregon Health and Science University, Portland, OR 97239, USA
JAMA 296:47-55. 2006..TRIAL REGISTRATION: clinicaltrials.gov Identifier: NCT00141206...
Distinct functions of the two isoforms of dopamine D2 receptorsA Usiello
Institut de Genetique et de Biologie Moleculaire et Cellulaire, CNRS, INSERM, ULP, Illkirch, C U de Strasbourg, France
Nature 408:199-203. 2000..The absence of D2L reveals that D2S inhibits D1 receptor-mediated functions, uncovering a circuit of signalling interference between dopamine receptors...
Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive ratsJeanette M Wood
Novartis Institute for Biomedical Research, Basel, Switzerland
J Hypertens 23:417-26. 2005..Aliskiren may therefore represent an effective, novel approach to the treatment of hypertension and related disorders, alone or in combination with other antihypertensive agents...
Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable anginaJean Claude Tardif
Montreal Heart Institute, 5000 Belanger Street, Montreal, Quebec H1T 1C8, Canada
Eur Heart J 26:2529-36. 2005..Ivabradine has shown anti-ischaemic and anti-anginal activity in a placebo-controlled trial. The objective of this study was to compare the anti-anginal and anti-ischaemic effects of ivabradine and the beta-blocker atenolol...
Effectiveness of smoking cessation therapies: a systematic review and meta-analysisPing Wu
Department of Clinical Epidemiology and Biostatistics, McMaster University, Hamilton, Canada
BMC Public Health 6:300. 2006..These include Nicotine Replacement Therapy [NRT], bupropion, and varenicline. We aimed to assess their relative efficacy in smoking cessation by conducting a systematic review and meta-analysis...
Potentiation of NMDA receptor currents by dopamine D1 receptors in prefrontal cortexGuojun Chen
Department of Physiology and Biophysics, School of Medicine and Biomedical Sciences, University at Buffalo, State University of New York, Buffalo, NY 14214, USA
Proc Natl Acad Sci U S A 101:2596-600. 2004..These interactions may play an important role in modulating synaptic plasticity and thus in cognitive and emotional processes...
Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitroR Scott Obach
Department of Pharmacokinetics, Dynamics, and Drug Metabolism, Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA
Drug Metab Dispos 34:121-30. 2006..The straightforward dispositional profile of varenicline should simplify its use in the clinic as an aid in smoking cessation...
Inhibition of cdk1 by alsterpaullone and thioflavopiridol correlates with increased transit time from mid G2 through prophaseDeena V Soni
Environmental Health Sciences Department, Case Western Reserve University, Cleveland, Ohio, USA
Cell Cycle 3:349-57. 2004..These results suggest that cdk1-cyclin activity is rate limiting for cell cycle progression during a period from mid G2 through prophase...
Non-nicotinic therapies for smoking cessationEric C K Siu
Center for Addiction and Mental Health and Department of Pharmacology, University of Toronto, Toronto, Canada
Annu Rev Pharmacol Toxicol 47:541-64. 2007..In conclusion, promising new therapeutic products are emerging and they will provide smokers additional options to assist in achieving smoking cessation...
Antianginal efficacy and safety of ivabradine compared with amlodipine in patients with stable effort angina pectoris: a 3-month randomised, double-blind, multicentre, noninferiority trialWitold Ruzyllo
Department of Coronary Artery Disease and Cardiac Catheterization Laboratory, Institute of Cardiology, Warsaw, Poland
Drugs 67:393-405. 2007..This study was undertaken to compare the antianginal and anti-ischaemic effects of the novel heart-rate-lowering agent ivabradine and of the calcium channel antagonist amlodipine...
Blockade of D1 dopaminergic transmission alleviates c-fos induction and cleaved caspase-3 expression in the brains of rat pups exposed to prenatal cocaine or perinatal asphyxiaEllen S Mitchell
Department of Biomedical Sciences, State University at Albany, Albany, NY, USA
Exp Neurol 182:64-74. 2003..SCH 23390 decreased caspase-3 expression after both birth insults, indicating that the increased incidence of apoptosis is related to overactivation of dopaminergic pathways...
Functional consequences of neuropeptide Y Y 2 receptor knockout and Y2 antagonism in mouse and human colonic tissuesNiall P Hyland
Centre for Neuroscience Research, King s College London, GKT School of Biomedical Sciences, Guy s Campus, London SE1 1UL, UK
Br J Pharmacol 139:863-71. 2003....
Comparative effects of ivabradine, a selective heart rate-lowering agent, and propranolol on systemic and cardiac haemodynamics at rest and during exerciseRobinson Joannides
Department of Pharmacology, Rouen University Hospital, INSERM U644, Rouen, France
Br J Clin Pharmacol 61:127-37. 2006....
Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channelsA Bucchi
Laboratory of Molecular Physiology and Neurobiology, Department of Biomolecular Sciences and Biotechnology, University of Milano, Italy
J Physiol 572:335-46. 2006..The mode of action of ivabradine on the two channels is discussed by implementing a simplified version of a previously developed model of f-channel kinetics...
The neurobiological basis for partial agonist treatment of nicotine dependence: vareniclineJ Foulds
Tobacco Dependence Program, UMDNJ School of Public Health, New Brunswick, NJ 08901, USA
Int J Clin Pract 60:571-6. 2006..Phase II and III trials have yielded promising results suggesting that varenicline could be an important advance in the treatment of nicotine dependence...
Funny channels in the control of cardiac rhythm and mode of action of selective blockersDario DiFrancesco
University of Milano, Department of Biomolecular Sciences and Biotechnology, Laboratory of Molecular Physiology and Neurobiology, Via Celoria 26, 20133 Milano, Italy
Pharmacol Res 53:399-406. 2006..Finally, a channel mutation responsible for one type of a relatively common rhythm disturbance, sinus bradycardia, has been recently identified, highlighting the clinical relevance of funny channels in the pacemaker function...
Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trialDouglas E Jorenby
University of Wisconsin School of Medicine and Public Health, Center for Tobacco Research and Intervention, Madison, Wis 53711, USA
JAMA 296:56-63. 2006..Varenicline, a partial agonist at the alpha4beta2 nicotinic acetylcholine receptor, has the potential to aid smoking cessation by relieving nicotine withdrawal symptoms and reducing the rewarding properties of nicotine...
VareniclineRaymond Niaura
Nat Rev Drug Discov 5:537-8. 2006
A double-blind study evaluating the long-term safety of varenicline for smoking cessationKathryn E Williams
Pfizer Global Research and Development, Groton, CT 06340, USA
Curr Med Res Opin 23:793-801. 2007..We assessed the safety of long-term varenicline administration for smoking cessation...
Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessationJotham W Coe
Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, USA
J Med Chem 48:3474-7. 2005..Varenicline displays high alpha4beta2 nAChR affinity and the desired in vivo dopaminergic profile...
Revealing the multidimensional framework of the Minnesota nicotine withdrawal scaleJoseph C Cappelleri
Pfizer Inc, Global Research and Development, Groton, CT 06340, USA
Curr Med Res Opin 21:749-60. 2005..No psychometric analyses of this version have been published. The objectives of this investigation were to perform a factor analysis and to further assess the psychometric properties of the MNWS...
Heart rate lowering by specific and selective I(f) current inhibition with ivabradine: a new therapeutic perspective in cardiovascular diseaseDario DiFrancesco
Dipartimento di Scienze Biomolecolari e Biotecnologie, , Milan, Italy
Drugs 64:1757-65. 2004..Experimental data indicate a potential role of pure heart rate lowering in other cardiovascular conditions, such as heart failure...
Pharmacokinetics, safety, and tolerability after single and multiple oral doses of varenicline in elderly smokersAaron H Burstein
Department of Medical and Developmental Sciences, Pfizer Global Research and Development, Groton/New London Labs, MS8260-2505, Groton, CT 06340, USA
J Clin Pharmacol 46:1234-40. 2006..Varenicline was well tolerated; all adverse events reported were mild to moderate in intensity. Thus, no dose adjustment is necessary based on age alone...
Multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy smokersHélène M Faessel
Department of Clinical Pharmacokinetics and Pharmacodynamics, Pfizer Global Research and Development, Eastern Point Road MS 8260 2309, Groton, CT 06340, USA
J Clin Pharmacol 46:1439-48. 2006..There was no evidence of concentration- or time-dependent changes in the pharmacokinetics of varenicline upon repeat dosing...
An employer-based cost-benefit analysis of a novel pharmacotherapy agent for smoking cessationKenneth C Jackson
Pharmacotherapy Outcomes Research Center, University of Utah College of Pharmacy, Salt Lake City, UT 84108, USA
J Occup Environ Med 49:453-60. 2007..An employer-based cost-benefit analysis for varenicline versus bupropion was conducted using clinical outcomes from a recently published trial...
Activation of the 5-HT1C receptor expressed in Xenopus oocytes by the benzazepines SCH 23390 and SKF 38393C A Briggs
Department of Neuroscience, Abbot Laboratories, Abbott Park, Illinois 60064
Br J Pharmacol 104:1038-44. 1991..receptor expressed in Xenopus laevis oocytes was used to characterize the action of four dopamine D1-selective benzazepines at the 5-HT1C receptor...
A preliminary benefit-risk assessment of varenicline in smoking cessationKate Cahill
Cochrane Tobacco Addiction Group, Department of Primary Health Care, Oxford University, Oxford, UK
Drug Saf 32:119-35. 2009....
Varenicline versus bupropion SR or placebo for smoking cessation: a pooled analysisMitchell Nides
Los Angeles Clinical Trials, 4116 W Magnolia Boulevard, Burbank, CA 91505, USA
Am J Health Behav 32:664-75. 2008....
Varenicline in prevention of relapse to smoking: effect of quit pattern on response to extended treatmentPeter Hajek
Wolfson Institute of Preventive Medicine, UK Centre for Tobacco Control Studies, Barts and The London, Queen Mary University of London, London E1 2AD, UK
Addiction 104:1597-602. 2009..In this secondary analysis, trial data were examined to see whether smokers who manage to achieve abstinence only later in the original course of treatment are more likely to benefit from having the course extended...
Mediation of hippocampal mossy fiber long-term potentiation by presynaptic Ih channelsJack Mellor
Department of Cellular and Molecular Pharmacology, University of California, San Francisco, CA 94143, USA
Science 295:143-7. 2002..Thus, Ih channels play an important role in the long-lasting control of transmitter release and neuronal excitability...
Varenicline versus transdermal nicotine patch for smoking cessation: results from a randomised open-label trialH J Aubin
Hôpital Emile Roux, Assistance Publique Hopitaux de Paris, Limeil Brevannes, Paris, France
Thorax 63:717-24. 2008..A study was undertaken to compare a 12-week standard regimen of varenicline with a 10-week standard regimen of transdermal nicotine replacement therapy (NRT) for smoking cessation...
Hypomania with agitation associated with varenicline use in bipolar II disorderAnne E Morstad
Ann Pharmacother 42:288-9. 2008
Varenicline treatment for smokers with schizophrenia: a case seriesA Eden Evins
J Clin Psychiatry 69:1016. 2008
Treatment of tobacco dependence: integrating recent progress into practiceBernard Le Foll
Translational Addiction Research Laboratory, Centre for Addiction and Mental Health, University of Toronto, Toronto, Ont
CMAJ 177:1373-80. 2007..Specifically, we discuss the use of nicotine replacement therapy, bupropion and varenicline in primary care settings...
Neuropsychiatric disturbance after initiation of varenicline in a patient with a history of alcohol abuse and major depressionPejman Pirmoradi
Medical City Dallas Hospital, Dallas, TX 75230, USA
Am J Health Syst Pharm 65:1624-6. 2008..The case of a patient with a history of alcohol abuse and major depression who developed neuropsychiatric symptoms after initiation of varenicline is reported...
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinasesD W Zaharevitz
Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, Maryland 20892 7444, USA
Cancer Res 59:2566-9. 1999..Cells exposed to kenpaullone and 10-bromopaullone display delayed cell cycle progression. Kenpaullone represents a novel chemotype for compounds that preferentially inhibit CDKs...
Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokersMasakazu Nakamura
Department of Health Promotion and Education, Osaka Medical Center for Health Science and Promotion, Osaka, Japan
Clin Ther 29:1040-56. 2007..Varenicline, a selective alpha4beta2 nicotinic acetylcholine receptor partial agonist, has been developed specifically for smoking cessation. In Japan, 39.3% of men smoke and this is a major public health concern...
Predictors of post-treatment relapse to smoking in successful quitters: pooled data from two phase III varenicline trialsJaimee L Heffner
Tri State Tobacco and Alcohol Research Center, University of Cincinnati Genome Research Institute, 2120 E Galbraith Rd, Bldg A, Cincinnati, OH 45237, USA
Drug Alcohol Depend 109:120-5. 2010..Identifying predictors of smoking relapse helps to elucidate the challenges of long-term smoking cessation and provides direction for improved treatment development...
Electrophysiological effects of S 16257, a novel sino-atrial node modulator, on rabbit and guinea-pig cardiac preparations: comparison with UL-FS 49C Thollon
Division Pathologies Cardiaques et Vasculaires, Institut de Recherches Servier, Suresnes, France
Br J Pharmacol 112:37-42. 1994..S 16257 and UL-FS 49 are equipotent in their bradycardic effect but S 16257 is more specific as it induces less increase in myocardial repolarization time...
Varenicline-induced manic episode in a patient with bipolar disorderIzchak Kohen
Am J Psychiatry 164:1269-70. 2007
Evidence for the sensitivity of operant timing behaviour to stimulation of D1 dopamine receptorsT H C Cheung
Psychopharmacology Section, Division of Psychiatry, University of Nottingham, Room B109, Medical School, Queen s Medical Centre, Nottingham, NG7 2UH, UK
Psychopharmacology (Berl) 195:213-22. 2007..It is not known whether this effect of d-amphetamine is mimicked by direct D(1)-like receptor stimulation...
Dual regulation of NMDA receptor functions by direct protein-protein interactions with the dopamine D1 receptorFrank J S Lee
Department of Neuroscience, Centre for Addiction and Mental Health, Clarke Division, University of Toronto, Toronto, M5T 1R8, Ontario, Canada
Cell 111:219-30. 2002..While one interaction is involved in the inhibition of NMDA receptor-gated currents, the other is implicated in the attenuation of NMDA receptor-mediated excitotoxicity through a PI-3 kinase-dependent pathway...
Thoughts and acts of aggression/violence toward others reported in association with vareniclineThomas J Moore
Institute for Safe Medication Practices, Horsham, PA, USA
Ann Pharmacother 44:1389-94. 2010..Thoughts and acts of aggression/violence toward others have been reported in postmarketing surveillance of varenicline, an aid to smoking cessation...
Heart rate reduction by ivabradine reduces oxidative stress, improves endothelial function, and prevents atherosclerosis in apolipoprotein E-deficient miceFlorian Custodis
Klinik fur Innere Medizin III, Kardiologie, Angiologie und Internistische Intensivmedizin, Universitatsklinikum des Saarlandes, 66424 Homburg Saar, Germany
Circulation 117:2377-87. 2008..We hypothesized that selective heart rate reduction may influence endothelial function and atherogenesis and tested the effects of the I(f) current inhibitor ivabradine in apolipoprotein E-deficient mice...
Topographical resolution of jaw movements mediated by cyclase- vs. non-cyclase-coupled dopamine D(1)-like receptors: studies with SK&F 83822Satoshi Fujita
Department of Pharmacology, Nihon University School of Dentistry, 1-8-13, Kanda-Surugadai, Chiyoda-ku, Tokyo 101-8310, Japan
Eur J Pharmacol 538:94-100. 2006....
Vitamin A deficiency induces motor impairments and striatal cholinergic dysfunction in ratsM Carta
Department of Applied Science for Biosystems, Section of Nutrition and Human Physiology, University of Cagliari, Italy
Neuroscience 139:1163-72. 2006..Our results stress the basic role of vitamin A in the maintenance of basal ganglia motor function in the adult rat brain...
D1 or D2 antagonism in nucleus accumbens core or dorsomedial shell suppresses lever pressing for food but leads to compensatory increases in chow consumptionK L Nowend
Unit 1020, Department of Psychology, University of Connecticut, 406 Babbidge Road, Storrs, CT 06269-1020, USA
Pharmacol Biochem Behav 69:373-82. 2001..Nevertheless, interference with accumbens DA does appear to set constraints upon which responses are selected for obtaining food, and may impair the ability of animals to overcome work-related response costs in order to obtain food...
Comparison of basal and D-1 dopamine receptor agonist-stimulated neuropeptide gene expression in caudate-putamen and nucleus accumbens of ad libitum fed and food-restricted ratsSandra L Haberny
Department of Pharmacology, Millhauser Laboratories, New York University School of Medicine, 550 First Avenue, New York, NY 10016, USA
Brain Res Mol Brain Res 141:121-7. 2005....
Receptor recycling mediates plasma membrane recovery of dopamine D1 receptors in dendrites and axons after agonist-induced endocytosis in primary cultures of striatal neuronsMarie Laure Martin-Negrier
CNRS UMR 5541, Université V Segalen Bordeaux 2, Laboratoire d Histologie Embryologie, Bordeaux Cedex, France
Synapse 60:194-204. 2006..Temporal characteristics observed for the recovery of D1R density to the basal state and those observed for the resensitization process strongly suggest that D1R recycling supports the receptor resensitization...
Behavioral and molecular effects of dopamine D1 receptor stimulation during naloxone-precipitated morphine withdrawalElena H Chartoff
Behavioral Genetics Laboratory, Department of Psychiatry, Harvard Medical School, McLean Hospital, Belmont, Massachusetts 02478, USA
J Neurosci 26:6450-7. 2006..Regardless, these findings suggest for the first time that D1 agonists might be useful for the treatment of withdrawal symptoms that contribute to the maintenance of opiate addiction in humans...
Dopamine D1 receptor activation regulates sodium channel-dependent EPSP amplification in rat prefrontal cortex pyramidal neuronsDiana C Rotaru
Translational Neuroscience Program, Department of Psychiatry, University of Pittsburgh School of Medicine, W1651 Biomedical Science Tower, 200 Lothrop Street, Pittsburgh, PA 15261, USA
J Physiol 581:981-1000. 2007..Therefore, the effects of D1R activation on Na+ channel-dependent EPSP amplification may regulate the impact of coincidence detection versus temporal integration mechanisms in PFC pyramidal neurons...
Role of dopamine D1 and D2 receptors in the nucleus accumbens shell on the acquisition and expression of fructose-conditioned flavor-flavor preferences in ratsSonia Y Bernal
Neuropsychology Doctoral Subprogram, Graduate Center, City University of New York, New York, NY, USA
Behav Brain Res 190:59-66. 2008..These data indicate that NAcS D1 and D2 antagonists significantly attenuated the expression of the fructose-CFP and did not block acquisition, but hastened extinction of fructose-CFP...
D1-like dopamine receptors selectively block P/Q-type calcium channels to reduce glutamate release onto cholinergic basal forebrain neurones of immature ratsToshihiko Momiyama
Division of Cerebral Structure, National Institute for Physiological Sciences, Okazaki 444 8787, Japan
J Physiol 580:103-17. 2007..These results suggest that D(1)-like receptor activation selectively blocks P/Q-type calcium channels to reduce glutamate release onto BF cholinergic neurones...
Dopamine receptors in the anterior insular cortex modulate long-term nociception in the ratUlises Coffeen
Laboratorio de Neurofisiología Integrativa, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de Fuente, Camino a Xochimilco 101, San Lorenzo Huipulco, Tlalpan, México D F CP 14370, Mexico
Eur J Pain 12:535-43. 2008..This work shows the differential role of dopamine receptors within the RAIC in which the activation of D(2) or the blockade of D(1) receptors elicit antinociception...
Pharmacological characterization of the effects of dopamine D(1) agonists on eye blinking in ratsRajeev I Desai
Preclinical Pharmacology Laboratory, McLean Hospital Harvard Medical School, Belmont, Massachusetts 02478, USA
Behav Pharmacol 18:745-54. 2007..Further studies with novel D(1)-like partial agonists may be useful in the development of pharmacotherapies for cocaine abuse...
Dopamine D2 receptor-dependent modulation of striatal NO synthase activityStephen Sammut
Department of Neuroscience, The Chicago Medical School at Rosalind Franklin University of Medicine and Science, 3333 Green Bay Road, North Chicago, IL, 60064, USA
Psychopharmacology (Berl) 191:793-803. 2007....
Motor-skill learning in a novel running-wheel task is dependent on D1 dopamine receptors in the striatumI Willuhn
Department of Cellular and Molecular Pharmacology, Rosalind Franklin University of Medicine and Science The Chicago Medical School, 3333 Green Bay Road, North Chicago, IL 60064, USA
Neuroscience 153:249-58. 2008..Furthermore, our findings demonstrate that D1 receptors in the striatum are critical for consolidation of long-term skill memory...
Effects of dopamine D1-like receptor agonists on food-maintained operant behavior in ratsJonathan L Katz
Psychobiology Section, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, Baltimore, Maryland 21224, USA
Behav Pharmacol 17:303-9. 2006....
Dopamine D1 receptor-dependent regulation of extracellular citrulline level in the rat nucleus accumbens during conditioned fear responseNatalia B Saulskaya
Laboratory of Higher Nervous Activity, I P Pavlov Institute of Physiology, Russian Academy of Sciences, 6 Admiral Makarov Embankment, St Petersburg 199034, Russia
Neurosci Lett 440:185-9. 2008....
Bidirectional dopaminergic modulation of excitatory synaptic transmission in orexin neuronsChristian O Alberto
Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Newfoundland, Canada A1B 3V6
J Neurosci 26:10043-50. 2006..In conclusion, our results suggest that D1- and D2-like receptors have opposing effects on the excitatory presynaptic terminals impinging onto orexin neurons...
The atypical dopamine D1 receptor agonist SKF 83959 induces striatal Fos expression in ratsDavid Wirtshafter
Laboratory of Integrative Neuroscience, Department of Psychology, M C 285, University of Illinois at Chicago, 1007 W Harrison St, Chicago, IL 60607 7137, USA
Eur J Pharmacol 528:88-94. 2005....
Differential actions of dopamine receptor antagonism in rats upon food intake elicited by either mercaptoacetate or exposure to a palatable high-fat dietR W Baker
Department of Psychology and Neuropsychology Doctoral Sub-Program, Queens College, City University of New York, 65-30 Kissena Boulevard, Flushing, NY 11367, USA
Pharmacol Biochem Behav 69:201-8. 2001....
Effects of individual and concurrent stimulation of striatal D1 and D2 dopamine receptors on electrophysiological and behavioral output from rat basal gangliaBarbara L Waszczak
Department of Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts, USA
J Pharmacol Exp Ther 300:850-61. 2002....
Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodentsAllison L Chausmer
Medications Discovery Research Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
Psychopharmacology (Berl) 159:145-53. 2002..Because A-77636 consistently attenuated the present effects of cocaine, it may prove more useful than the others as a pharmacotherapy to treat cocaine abuse...
Blockade or stimulation of D1 dopamine receptors attenuates cue reinstatement of extinguished cocaine-seeking behavior in ratsAndrea T Alleweireldt
Department of Psychology, Arizona State University, Box 871104, Tempe, AZ 85287-1104, USA
Psychopharmacology (Berl) 159:284-93. 2002..CONCLUSIONS: While the antagonist and full agonist produced similar effects on cocaine-seeking behavior, only the agonist increased response latency, suggesting that different processes mediate the effects of these drugs...
No change in dopamine D1 receptor in vivo binding in rats after sub-chronic haloperidol treatmentVito Sanci
PET Centre, Centre for Addiction and Mental Health, University of Toronto, ON, Canada
Can J Physiol Pharmacol 80:36-41. 2002..This study failed to link the purported D1 receptor-mediated behaviors with in vivo receptor binding measures of R-[11C]SKF 82957 or [11C]SCH 23390 in rat brain regions...
Neurohormonal antagonism in heart failure; beneficial effects of vasopressin V(1a) and V(2) receptor blockade and ACE inhibitionMareo Naitoh
Department of Medicine, University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Victoria 3084, Australia
Cardiovasc Res 54:51-7. 2002..These results suggest conivaptan may be a useful addition to ACE inhibitors in the management of vasoconstriction and fluid retention that characterizes CHF...
Striatal preprotachykinin mRNA levels are regulated by stimulatory agents and dopamine D1 receptor manipulation in rodent organotypic slice culturesB M Campbell
Cellular and Clinical Neurobiology Program, Department of Psychiatry and Behavioral Neurosciences, Wayne State University, School of Medicine, Detroit, MI 48201, USA
Brain Res 888:26-33. 2001..5+/-5.4%). These findings indicate that tachykinin gene expression is inducible within slice culture preparations and that the maintenance of normal striatal PPT mRNA levels depends on DA D1 receptor tone...
Injection of SCH 23390, but not 7-hydroxy-DPAT, into the ventral tegmental area blocks the acute motor-stimulant response to cocaineJ D Steketee
Department of Pharmacology and Therapeutics, Louisiana State University Medical Center at Shreveport 71130 3932, USA
Behav Pharmacol 8:58-64. 1997..These data suggest that DA D1 receptors in the VTA may play a role in psychostimulant-induced motor activity. However, the role DA D2/3 receptors in the VTA may have in cocaine-induced motor activity remains unclear...
D(1) dopamine receptor stimulation increases GluR1 phosphorylation in postnatal nucleus accumbens culturesSteven Z Chao
Department of Neuroscience, FUHS/The Chicago Medical School, North Chicago, Illinois 60064-3095, USA
J Neurochem 81:984-92. 2002..Thus, the present results suggest that AMPA receptor transmission in the nucleus accumbens may be augmented by concurrent D(1) receptor stimulation...
Concurrent activation of dopamine D1 and D2 receptors is required to evoke neural and behavioral phenotypes of cocaine sensitizationChristine Capper-Loup
Department of Neurology, University Hospital, 3010 Bern, Switzerland
J Neurosci 22:6218-27. 2002....
D1 dopamine receptor stimulation increases GluR1 surface expression in nucleus accumbens neuronsSteven Z Chao
Department of Neuroscience, The Chicago Medical School, 3333 Green Bay Road, North Chicago, IL 60064-3095, USA
J Neurochem 83:704-12. 2002..When dopamine receptors are over-stimulated during chronic drug administration, this regulation may be disrupted, leading to inappropriate plasticity in neuronal circuits governing motivation and reward...
SKF 83959 is an antagonist of dopamine D1-like receptors in the prefrontal cortex and nucleus accumbens: a key to its antiparkinsonian effect in animals?A R Cools
Department of Psychoneuropharmacology, Nijmegen Institute of Neurosciences, University of Nijmegen, P O Box 9101, 6500 HB Nijmegen, The Netherlands
Neuropharmacology 42:237-45. 2002..The role of these receptors in the antiparkinson profile of SKF 83959 is discussed...
Intrastriatal GABA(A) receptor blockade does not alter dopamine D(1)/D(2) receptor interactions in the intact rat striatumE A Jones
Department of Anatomy and Cell Biology, East Carolina University, School of Medicine, Greenville, NC 27858, USA
Neuroscience 102:381-9. 2001..These data indicate that blockade of striatal GABA(A) receptors has only a subtle effect on acute dopamine agonist-induced changes in gene expression. These results are discussed in the context of local intrastriatal interactions...
Decreased striatal dopamine efflux after intrastriatal application of benzazepine-class D1 agonists is not mediated via dopamine receptorsJ A Zackheim
Center for Molecular and Behavioral Neuroscience, Rutgers University, Newark, NJ 07102, USA
Brain Res Bull 54:603-7. 2001..There is therefore no indication for an intrastriatal population of D1 receptors capable of modulating dopamine efflux...
Substantia nigra pars reticulata is a highly potent site of action for the behavioral effects of the D1 antagonist SCH 23390 in the ratJ T Trevitt
Department of Psychology, University of Connecticut, Storrs 06269-1020, USA
Psychopharmacology (Berl) 156:32-41. 2001..It is possible that blockade of SNr D1 receptors modulates GABA release from striatonigral neurons...
Stimulation of D1-type dopamine receptors enhances excitability in prefrontal cortical pyramidal neurons in a state-dependent mannerA Lavin
Department of Neuroscience, University of Pittsburgh, 446 Crawford Hall, Pittsburgh, PA 15260, USA
Neuroscience 104:335-46. 2001..From these data we suggest that dopamine exerts state-dependent modulatory effects on the excitability of neurons in deep layers of the prefrontal cortex...
Ventral striatal vs. accumbal (shell) mechanisms and non-cyclase-coupled dopamine D(1)-like receptors in jaw movementsM Hasegawa
Department of Pharmacology, Nihon University School of Dentistry, 1-8-13 Kanda-Surugadai, Chiyoda, Tokyo 101-8310, Japan
Eur J Pharmacol 423:171-8. 2001....
Intrapallidal dopamine restores motor deficits induced by 6-hydroxydopamine in the ratA Galvan
, , , ,
J Neural Transm 108:153-66. 2001..Moreover, motor recovery was produced by selectively injecting dopamine into the globus pallidus...
The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptorsM J Millan
Institut de Recherches Servier, Psychopharmacology Department, Paris, France
Psychopharmacology (Berl) 156:58-62. 2001..57 nM. CONCLUSIONS: SCH23390 is a potent and high efficacy agonist at h5-HT2C receptors. Activation of 5-HT2C receptors by SCH23390 may contribute to its functional properties both in animals and in humans...
Influence of glucocorticoids on dopaminergic transmission in the rat dorsolateral striatumM Barrot
Psychobiologie des Comportements Adaptatifs, INSERM U259, , , 33077 Bordeaux Cedex, France
Eur J Neurosci 13:812-8. 2001..2000) Eur. J. Neurosci., 12, 973-979]. The present data highlight the profound heterogeneous influence of glucocorticoids within dopaminergic projections...
Stimulated D(1) dopamine receptors couple to multiple Galpha proteins in different brain regionsL Q Jin
Laboratory of Molecular Pharmacology, Department of Pharmacology and Physiology, MCP Hahnemann School of Medicine, Philadelphia 19102, USA
J Neurochem 78:981-90. 2001..The results indicate that in addition to the D(1)/G(s)/adenylyl cyclase system, brain D(1)-like dopamine receptor sites activate phospholipase C through Galpha(q) protein...
Stimulatory role of dopamine on fibroblast growth factor-2 expression in rat striatumM Roceri
Centre for Neuropharmacology, Department of Pharmacological Sciences, University of Milan, Milan, Italy
J Neurochem 76:990-7. 2001..On the basis of FGF-2 neurotrophic activity, these results suggest that direct or indirect activation of dopaminergic system can be neuroprotective and might reduce cell vulnerability in degenerative disorders...
Research Grants
- Synthesis of Bioactive Complex AlkaloidsDAVID GIN; Fiscal Year: 2006..pyrrolidines, as well as strain-accelerated [3,3]-sigmatropic rearrangement for the synthesis of complex benzazepines. Successful synthesis of these target molecules will not only lay the foundation for efficient and practical ..
- High Dose Nicotine Patch Therapy for Spit Tobacco UsersJon Ebbert; Fiscal Year: 2004..Our goal is to reduce the prevalence of ST use and decrease the incidence of oropharyngeal cancer through the development of effective treatment options for ST users. ..
- Brief Dental Office Intervention with Tobacco QuitlineJon Ebbert; Fiscal Year: 2005..S. adult population smoking; and 3) 75% of smokers quitting for at least one day or longer because they are trying to quit. ..
- Evaluating Nicoting Lozenges for Treatment of Smokeless Tobacco AddictionJon Ebbert; Fiscal Year: 2007..No drug therapies have been shown to be effective for helping smokeless tobacco users quit for good. The purpose of this study is to test drugs that can be used to help smokeless tobacco users quit for good. ..
- Evaluating Nicotine Lozenges for Treatment of Smokeless Tobacco AddictionJon Ebbert; Fiscal Year: 2009..No drug therapies have been shown to be effective for helping smokeless tobacco users quit for good. The purpose of this study is to test drugs that can be used to help smokeless tobacco users quit for good. ..
- Combination Therapy with Varenicline and Bupropion for Smoking CessationJon O Ebbert; Fiscal Year: 2010..Combining medications together may increase the long-term smoking quit rates and decrease the death and disability associated with cigarette smoking. ..
- Polycystic Kidney Disease: Innovative Imaging to Assess Progression (PCC)Vicente Torres; Fiscal Year: 2007....
- Novel treatments for polycystic kidney diseaseVicente Torres; Fiscal Year: 2009..abstract_text> ..
- CNS Mechanisms that Modulate RewardKenneth D Carr; Fiscal Year: 2010....
- REDOX, ACID/BASE, AND PATHOGENESIS OF ADPKDVicente Torres; Fiscal Year: 2002..The main thrust of the proposed studies is directed towards the identification of pathogenetic mechanisms than can be subject to preventive and therapeutic interventions. ..
- Novel treatment for polycystic kidney diseaseVicente E Torres; Fiscal Year: 2010....
- Novel treatments for polycystic kidney diseaseVicente Torres; Fiscal Year: 2007....
- CNS Mechanisms that Modulate RewardKENNETH CARR; Fiscal Year: 2007....
- KIDNEY DISEASE RESEARCH TRAINING PROGRAMVicente Torres; Fiscal Year: 2007..abstract_text> ..
- OPIOID MECHANISMS THAT FACILITATE REWARDKENNETH CARR; Fiscal Year: 2006..abstract_text> ..
- Controlled Trial of Renin Angiotensin Blockade in ADPKDVicente Torres; Fiscal Year: 2007..Approximately one-half of these patients will have normal or near-normal renal function and one-half have mild to moderate renal insufficiency. The protocols for the Pilot Study will be conducted only at the Mayo Clinic. ..
- AASK Cohort StudyKenneth Jamerson; Fiscal Year: 2007..Ultimately, data from the AASK Cohort Study should enhance our understanding of the determine the progression of kidney disease. Such results might eventually lead to new ESRD. ..
- CNS OPIOID MECHANISMS THAT MODULATE REWARD AND AVERSIONKENNETH CARR; Fiscal Year: 2002....
- RENIN ANGIOTENSIN SYSTEM IN THE PATHOGENESIS OF ADPKDVicente Torres; Fiscal Year: 1993..The results of these studies will augment the understanding of the pathogenesis of cyst formation and hypertension in ADPKD and are likely to have a significant impact on the treatment of this disease...
- CHRONIC AND ACUTE TOLERANCE TO NICOTINE IN HUMANSKenneth Perkins; Fiscal Year: 1999....
- Step Up Wellness Program for Depression Physical Inactivity and SmokingJENNIFER MC CLURE; Fiscal Year: 2007..This work will provide valuable information about the feasibility, acceptability, and impact of this comprehensive treatment approach and will lay the ground work for future research in this area. ..
- Optimizing an online motivational tobacco cessation programJENNIFER B MC CLURE; Fiscal Year: 2010..Information learned from this study will advance the science of tailoring health risk communications, as well as inform how to best design an online motivational intervention for smoking cessation. ..
- Tobacco Smoking, Nicotine and Negative Affect ReliefKenneth Perkins; Fiscal Year: 2009..In sum, this research will help address the fundamental question of why cigarette smoking is reinforcing. ..
- Tobacco Smoking, Nicotine and Negative Affect ReliefKenneth Perkins; Fiscal Year: 2007..In sum, this research will help address the fundamental question of why cigarette smoking is reinforcing. ..
- Proactive Cessation Intervention with Biomarker FeedbackJENNIFER MC CLURE; Fiscal Year: 2007..If effective, this treatment strategy could have broad potential as a public health intervention. ..
- SEX DIFFERENCES IN NICOTINE REINFORCEMENT: HUMAN/ANIMALKenneth Perkins; Fiscal Year: 2003....
- INDIVIDUAL VARIATION IN NICOTINE SENSITIVITY IN HUMANSKenneth Perkins; Fiscal Year: 2003..e., in nicotine-naive individuals). Results will provide directions for future research on vulnerability to tobacco dependence and for targeted efforts to prevent smoking onset. ..
- DISCRIMINATIVE STIMULUS EFFECTS OF NICOTINEKenneth Perkins; Fiscal Year: 2001....
- CHRONIC AND ACUTE TOLERANCE TO NICOTINE IN HUMANSKenneth Perkins; Fiscal Year: 1993..Results may proivde directions for the study of mechanisms responsible for tolerance, as well as for investigations of physiological and behavioral aspects of nicotine depenence and smoking relapse...
- Affect, Context, and Placebo Responses to NicotineKenneth Perkins; Fiscal Year: 2005..Secondary analyses may identify important individual characteristics associated with placebo responses, aiding in the prediction of which smokers ultimately are likely to benefit most from manipulation of placebo effects. ..
- ASK, ADVISE, REFER: Promoting Pharmacy-based Referrals to Tobacco QuitlinesKaren Hudmon; Fiscal Year: 2009....
- Safety of Nicotine Reduction StrategyNeal Benowitz; Fiscal Year: 2009..The proposed research is needed to guide governmental regulators as to how best to regulate nicotine in cigarettes and is an essential first step in examining the feasibility of a national regulation program. ..
