H Rollema

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation
    Jotham W Coe
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 15:4889-97. 2005
  2. ncbi Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation
    Hans Rollema
    Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
    Trends Pharmacol Sci 28:316-25. 2007
  3. doi Effect of co-administration of varenicline and antidepressants on extracellular monoamine concentrations in rat prefrontal cortex
    Hans Rollema
    Department of Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
    Neurochem Int 58:78-84. 2011
  4. pmc Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
    H Rollema
    Neuroscience Biology, Groton, CT 06340, USA
    Br J Pharmacol 160:334-45. 2010
  5. doi Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognition
    Hans Rollema
    Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
    Biochem Pharmacol 78:813-24. 2009
  6. pmc Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect
    Hans Rollema
    Department Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
    Eur J Pharmacol 605:114-6. 2009
  7. ncbi Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid
    H Rollema
    Department of Neuroscience Biology, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Neuropharmacology 52:985-94. 2007
  8. ncbi Do 5-HT1B/1D autoreceptors modulate dorsal raphe cell firing? In vivo electrophysiological studies in guinea pigs with GR127935
    J Sprouse
    Pfizer Central Research, Groton, CT 06340, USA
    Neuropharmacology 36:559-67. 1997
  9. ncbi Clozapine increases dopamine release in prefrontal cortex by 5-HT1A receptor activation
    H Rollema
    Pfizer Inc, Department of Neuroscience, Groton, CT 06340, USA
    Eur J Pharmacol 338:R3-5. 1997
  10. ncbi Activation of postsynaptic 5-HT(1A) receptors by fluoxetine despite the loss of firing-dependent serotonergic input: electrophysiological and neurochemical studies
    J Sprouse
    Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Synapse 41:49-57. 2001

Detail Information

Publications23

  1. ncbi 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation
    Jotham 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...
  2. ncbi Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation
    Hans Rollema
    Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
    Trends Pharmacol Sci 28:316-25. 2007
    ....
  3. doi Effect of co-administration of varenicline and antidepressants on extracellular monoamine concentrations in rat prefrontal cortex
    Hans Rollema
    Department of Neuroscience, Pfizer Global Research and Development, Groton, CT 06340, USA
    Neurochem Int 58:78-84. 2011
    ....
  4. pmc Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
    H 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...
  5. doi Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognition
    Hans Rollema
    Department of Neuroscience Biology, Pfizer Global Research and Development, Groton, CT 06340, USA
    Biochem Pharmacol 78:813-24. 2009
    ....
  6. pmc Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect
    Hans 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...
  7. ncbi Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid
    H 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...
  8. ncbi Do 5-HT1B/1D autoreceptors modulate dorsal raphe cell firing? In vivo electrophysiological studies in guinea pigs with GR127935
    J Sprouse
    Pfizer Central Research, Groton, CT 06340, USA
    Neuropharmacology 36:559-67. 1997
    ....
  9. ncbi Clozapine increases dopamine release in prefrontal cortex by 5-HT1A receptor activation
    H 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...
  10. ncbi Activation of postsynaptic 5-HT(1A) receptors by fluoxetine despite the loss of firing-dependent serotonergic input: electrophysiological and neurochemical studies
    J Sprouse
    Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Synapse 41:49-57. 2001
    ....
  11. ncbi 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 exposures
    Karthik Venkatakrishnan
    Department of Clinical Pharmacology, Pfizer Global Research and Development, Groton, Connecticut 06340, USA
    Drug Metab Dispos 35:1341-9. 2007
    ....
  12. ncbi In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine
    Jotham 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...
  13. doi A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessation
    Hélène 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...
  14. ncbi Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation
    Jotham 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...
  15. ncbi Acute effects of atypical antipsychotics on whole-body insulin resistance in rats: implications for adverse metabolic effects
    Karen 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...
  16. ncbi Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain
    D E Johnson
    Department of Neuroscience, Pfizer Global Research and Development, MS 8220-4159, Groton, CT 06340, USA
    Eur J Pharmacol 425:203-10. 2001
    ....
  17. ncbi Inhibitory effects of antipsychotics on carbachol-enhanced insulin secretion from perifused rat islets: role of muscarinic antagonism in antipsychotic-induced diabetes and hyperglycemia
    David 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
    ....
  18. pmc Differential effects of various typical and atypical antipsychotics on plasma glucose and insulin levels in the mouse: evidence for the involvement of sympathetic regulation
    Yvette E Savoy
    Department of General Pharmacology, Pfizer Global Research and Development, Pfizer Inc, Groton, CT 06340, USA
    Schizophr Bull 36:410-8. 2010
    ....
  19. doi A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists
    John 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...
  20. ncbi The role of muscarinic receptor antagonism in antipsychotic-induced hippocampal acetylcholine release
    David E Johnson
    Department of Neuroscience, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Eur J Pharmacol 506:209-19. 2005
    ....
  21. ncbi Varenicline: new treatment with efficacy in smoking cessation
    Victor 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...
  22. ncbi AAPS-FDA workshop white paper: microdialysis principles, application and regulatory perspectives
    Chandra 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...
  23. ncbi AAPS-FDA Workshop White Paper: microdialysis principles, application, and regulatory perspectives
    Chandra 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