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Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation.
Varenicline displays high alpha4beta2 nAChR affinity and the desired in vivo dopaminergic profile and provides relief from the craving and withdrawal syndrome that accompanies cessation attempts.
Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Varenicline displays high α4β2 nAChR affinity and the desired in vivo dopaminergic profile and provides relief from the craving and withdrawal syndrome that accompanies cessation attempts.
Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid
Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid.
The data suggest that varenicline can reproduce to some extent the subjective effects of smoking by partially activating alpha4beta2 nAChRs, while preventing full activation of these receptors by nicotine.
Nicotinic acetylcholine receptors: from basic science to therapeutics.
Rationale, pharmacology and clinical efficacy of partial agonists of α4β2 nACh receptors for smoking cessation
Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation.
- H. Rollema, J. Coe, L. Chambers, R. Hurst, S. Stahl, K. Williams
- Biology, MedicineTrends in pharmacological sciences
The rationale for and the design of alpha(4)beta(2) nAChR partial agonists as novel treatments for tobacco addiction are discussed and varenicline, which has significantly better quit rates than do other treatments and offers a new option for smoking cessation pharmacotherapy, is demonstrated.
Acute Effects of Atypical Antipsychotics on Whole-Body Insulin Resistance in Rats: Implications for Adverse Metabolic Effects
- K. Houseknecht, A. Robertson, W. Zavadoski, E. M. Gibbs, David E. Johnson, H. Rollema
- 1 February 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.
5-HT1A receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex
Pre‐clinical properties of the α4β2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence
The origin of the differences in clinical efficacy in smoking cessation trials with three high‐affinity partial agonists of α4β2 neuronal nicotinic acetylcholine receptors is examined by taking into account brain exposure and pharmacological effects at human α4 β2 nAChRs.