Publicaciones 2011-2020

@article{RN127,
title = {Varenicline and Cytisine: Two Nicotinic Acetylcholine Receptor Ligands Reduce Ethanol Intake in University of Chile Bibulous Rats},
author = { R. Sotomayor-Zarate and K. Gysling and U.E. Busto and B.K. Cassels and L. Tampier and M.E. Quintanilla},
url = {/brokenurl#<Go to ISI>://WOS:000318310400010},
doi = {10.1007/s00213-013-2974-3},
issn = {0033-3158},
year = {2013},
date = {2013-01-01},
journal = {Psychopharmacology},
volume = {227},
number = {2},
pages = {287-298},
abstract = {Neuronal nicotinic acetylcholine receptors (nAChRs) are pharmacological targets that have recently been implicated in the reinforcing effects of many drugs of abuse, including ethanol. Varenicline and cytisine are nAChR partial agonists in clinical use as smoking cessation aids. However, their efficacies to reduce alcohol consumption have not been fully studied., This study aims to compare the effects of varenicline and cytisine on ethanol consumption by rats bred for many generations as high ethanol drinkers (UChB)., Repeated dosing (0.5 or 1.0 mg/kg/day i.p.) of varenicline or cytisine, for three consecutive days, to male UChB rats pre-exposed to 10 % (v/v) ethanol and water 24 h/day for 4 weeks, significantly reduced alcohol intake and preference of ethanol over water during 1- and 24-h ethanol access periods. This effect was specific for ethanol intake and was not observed for 0.2 % saccharin or water consumption. Varenicline appears to be more effective than cytisine, probably due to its more favorable pharmacokinetic and pharmacodynamic properties. Long-term use of both nAChRs ligands for more than 8-10 days induced tolerance to their effects on ethanol consumption., This preclinical study in UChB rats demonstrated that both varenicline and cytisine reduce alcohol intake, with varenicline producing a greater and longer-lasting reduction than cytisine. However, dose adjustment will have to be considered as a possible way to counter tolerance arising after continued use.},
keywords = {agonist, alpha-4-beta-2, beta-2 clinical-efficacy, consumption, cytisine, dependence ethanol high-alcohol-drinking modulation, partial preference, rats, sazetidine-a, smoking-cessation, subunit, uchb varenicline},
pubstate = {published},
tppubtype = {article}
}

@article{RN14g,
title = {Crystal Structure of (1r,5s)-9-Nitro-1,2,3,4,5,6-Hexahydro-1,5-Methanopyrido[1,2-a][1,5] Diazocin-8-One (9-Nitrocytisine), C11h13o3n3},
author = {A. Gald\'{a}mez and M. Gutierrez-Hernandez and B.K. Cassels and P. Saez-Briones},
url = {/brokenurl#<Go to ISI>://WOS:000290700500016},
doi = {10.4067/S0717-97072011000100016},
issn = {0717-9324},
year = {2011},
date = {2011-01-01},
journal = {Journal of the Chilean Chemical Society},
volume = {56},
number = {1},
pages = {595-597},
abstract = {The title compound (1, trivial name: 9 (or 3)-nitrocytisine) crystallizes with two independent molecules in the asymmetric unit. In its structure two rings form a bispidine framework that is fused to a 3-nitro-2-pyridone group. The half-normal probability plot reveals that the two molecules do not show any significant geometrical differences, except in conformations of the nitro-group, which is involved in intermolecular interactions. The crystal packing structure of the title compound is described in terms of three-dimensional supramolecular arrays built up from chains of N-H center dot center dot center dot O (nitro-group), hydrogen bonds and weak intermolecular C-H center dot center dot center dot O=C interactions, with graph-set descriptors C-2(2)(6) and C-2(2)(10) motifs, which together result in R-4(4)(26) rings motifs. These chains are additionally stabilized by intermolecular NO2.pi interactions.},
keywords = {agonists, alpha-4-beta-2, crystal cytisine cytisinoid, derivatives, design diffraction, halogenated hydrogen-bond, in-vivo, nicotinic patterns, smoking-cessation, structure, therapeutic-efficacy, x-ray},
pubstate = {published},
tppubtype = {article}
}