Research Topics
| H RollemaSummaryAffiliation: Pfizer Global Research and Development Country: USA Publications
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Detail Information
Publications
3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessationJotham W Coe
Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
Bioorg Med Chem Lett 15:4889-97. 2005..In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation...- Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessationHans Rollema
Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
Trends Pharmacol Sci 28:316-25. 2007.... 
Effect of co-administration of varenicline and antidepressants on extracellular monoamine concentrations in rat prefrontal cortexHans Rollema
Department of Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
Neurochem Int 58:78-84. 2011....
Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependenceH Rollema
Neuroscience Biology, Groton, CT 06340, USA
Br J Pharmacol 160:334-45. 2010..This work examines the origin of the differences by taking into account brain exposure and pharmacological effects at human alpha4beta2 nAChRs...- 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.... - Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effectHans Rollema
Department Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
Eur J Pharmacol 605:114-6. 2009..These data suggest that varenicline may have antidepressant potential and can, when combined, augment antidepressant responses of selective serotonin reuptake inhibitors... - Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aidH Rollema
Department of Neuroscience Biology, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
Neuropharmacology 52:985-94. 2007..Based on these findings, varenicline was advanced into clinical development and recently shown to be an effective and safe aid for smoking cessation treatment... - Do 5-HT1B/1D autoreceptors modulate dorsal raphe cell firing? In vivo electrophysiological studies in guinea pigs with GR127935J Sprouse
Pfizer Central Research, Groton, CT 06340, USA
Neuropharmacology 36:559-67. 1997.... - Clozapine increases dopamine release in prefrontal cortex by 5-HT1A receptor activationH Rollema
Pfizer Inc, Department of Neuroscience, Groton, CT 06340, USA
Eur J Pharmacol 338:R3-5. 1997..Agonist affinity for 5-HT1A receptors could thus be a desirable feature in the design of new antipsychotics... - Activation of postsynaptic 5-HT(1A) receptors by fluoxetine despite the loss of firing-dependent serotonergic input: electrophysiological and neurochemical studiesJ Sprouse
Pfizer Global Research and Development, Groton, Connecticut 06340, USA
Synapse 41:49-57. 2001.... - Central nervous system pharmacokinetics of the Mdr1 P-glycoprotein substrate CP-615,003: intersite differences and implications for human receptor occupancy projections from cerebrospinal fluid exposuresKarthik Venkatakrishnan
Department of Clinical Pharmacology, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
Drug Metab Dispos 35:1341-9. 2007.... - In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisineJotham W Coe
Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
Bioorg Med Chem Lett 15:2974-9. 2005..In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine... - A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessationHélène M Faessel
Clinical Pharmacology, Primary Care Unit, Pfizer Inc, New London, Connecticut 06320, USA
Clin Pharmacokinet 49:799-816. 2010..In all, the predictable pharmacokinetic properties and straightforward dispositional profile of varenicline simplify its use in clinical practice... - 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... - Acute effects of atypical antipsychotics on whole-body insulin resistance in rats: implications for adverse metabolic effectsKaren L Houseknecht
Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA
Neuropsychopharmacology 32:289-97. 2007..OLAN and CLOZ can thus rapidly induce marked insulin resistance, which could contribute to the hyperglycemia and ketoacidosis reported for patients receiving those therapies... - Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brainD E Johnson
Department of Neuroscience, Pfizer Global Research and Development, MS 8220-4159, Groton, CT 06340, USA
Eur J Pharmacol 425:203-10. 2001.... - Inhibitory effects of antipsychotics on carbachol-enhanced insulin secretion from perifused rat islets: role of muscarinic antagonism in antipsychotic-induced diabetes and hyperglycemiaDavid E Johnson
Pfizer Global Research and Development, Department of Neuroscience, Groton Laboratories, MS 8220-4159, Eastern Point Road, Groton, CT 06340, USA
Diabetes 54:1552-8. 2005.... - Differential effects of various typical and atypical antipsychotics on plasma glucose and insulin levels in the mouse: evidence for the involvement of sympathetic regulationYvette E Savoy
Department of General Pharmacology, Pfizer Global Research and Development, Pfizer Inc, Groton, CT 06340, USA
Schizophr Bull 36:410-8. 2010.... - A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonistsJohn A Lowe
Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, United States
Bioorg Med Chem Lett 20:4749-52. 2010..Compound 17a may thus be a useful tool for studying the role of alpha3beta4 and alpha6/4beta4 nicotinic receptors in CNS pharmacology... - The role of muscarinic receptor antagonism in antipsychotic-induced hippocampal acetylcholine releaseDavid E Johnson
Department of Neuroscience, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
Eur J Pharmacol 506:209-19. 2005.... - Varenicline: new treatment with efficacy in smoking cessationVictor I Reus
Department of Psychiatry, University of California School of Medicine, San Francisco, California 94143 0984, USA
Drugs Today (Barc) 43:65-75. 2007..Its targeted mechanism of action, superior efficacy and excellent tolerability make varenicline a welcome and useful addition to the therapeutic options for smoking cessation... - AAPS-FDA workshop white paper: microdialysis principles, application and regulatory perspectivesChandra S Chaurasia
Division of Bioequivalence, Office of Generic Drugs, Food and Drug Administration, Rockville, MD, USA
Pharm Res 24:1014-25. 2007..Stakeholders from academia, industry and regulatory agencies presented their views on microD as a tool in drug research and development... - AAPS-FDA Workshop White Paper: microdialysis principles, application, and regulatory perspectivesChandra S Chaurasia
Division of Bioequivalence, Office of Generic Drugs, Food and Drug Administration, Room 1360/HFD-650, 7520 Standish Place, Rockville, MD 20855, USA
J Clin Pharmacol 47:589-603. 2007