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Natalie Walker et al.
BMC public health, 11, 880-880 (2011-11-23)
Smokers need effective support to maximise the chances of successful quit attempts. Current smoking cessation medications, such as nicotine replacement therapy (NRT), bupropion, nortriptyline or varenicline, have been shown to be effective in clinical trials but are underused by smokers...
Colin S Cunningham et al.
The Journal of pharmacology and experimental therapeutics, 341(3), 840-849 (2012-03-23)
This study examined mechanisms by which nicotine (1.78 mg/kg base s.c.) produces discriminative stimulus effects in rhesus monkeys. In addition to nicotine, various test compounds were studied including other nicotinic acetylcholine receptor agonists (varenicline and cytisine), antagonists [mecamylamine and the...
Natalie Walker et al.
The New England journal of medicine, 371(25), 2353-2362 (2014-12-18)
Placebo-controlled trials indicate that cytisine, a partial agonist that binds the nicotinic acetylcholine receptor and is used for smoking cessation, almost doubles the chances of quitting at 6 months. We investigated whether cytisine was at least as effective as nicotine-replacement...
Christopher I Richards et al.
Nano letters, 12(7), 3690-3694 (2012-06-07)
We exploit the optical and spatial features of subwavelength nanostructures to examine individual receptors on the plasma membrane of living cells. Receptors were sequestered in portions of the membrane projected into zero-mode waveguides. Using single-step photobleaching of green fluorescent protein...
Iwona Zieleń et al.
Przeglad lekarski, 69(10), 1098-1102 (2013-02-21)
Tobacco smoking in Poland is fairly widespread on a large scale. Research suggests that the early twenty-first century, the percentage of female daily smokers aged 20 and above was 26%, and men the same age 43%. In addition, epidemiological studies...
Hugo R Arias et al.
The international journal of biochemistry & cell biology, 43(9), 1330-1339 (2011-06-07)
The interaction of ibogaine analogs with nicotinic acetylcholine receptors (AChRs) in different conformational states was studied by functional and structural approaches. The results established that ibogaine analogs: (a) inhibit (±)-epibatidine-induced Ca²⁺ influx in human embryonic muscle AChRs with the following...
Magdalena Majewska et al.
Przeglad lekarski, 68(8), 523-526 (2011-10-21)
Serotonin syndrome is caused by excess serotonin in the central nervous system. It usually occurs as adverse drug-therapy (neuroleptic agents, monoamine oxidase inhibitors, serotonin reuptake inhibitors and others). a 50-year-old woman with a history of depression, was admitted to our...
Michael J Marks et al.
Journal of neurochemistry, 130(2), 185-198 (2014-03-26)
Nicotinic acetylcholine receptors (nAChR) of the α6β2* subtype (where *indicates the possible presence of additional subunits) are prominently expressed on dopaminergic neurons. Because of this, their role in tobacco use and nicotine dependence has received much attention. Previous studies have...
Edwin G Pérez et al.
Natural product reports, 29(5), 555-567 (2012-03-01)
Covering: up to the end of 2011. This review covers classical and modern structural modifications of the alkaloid, the more recent (since 2007) syntheses of cytisine and analogues, and the pharmacology of these compounds, with emphasis on their interactions with...
Ramón Sotomayor-Zárate et al.
Psychopharmacology, 227(2), 287-298 (2013-01-25)
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...
B T O'Neill et al.
Organic letters, 2(26), 4201-4204 (2001-01-11)
[reaction:see text] The nicotine partial agonist cytisine was prepared in five steps featuring an "in situ" Stille or Suzuki biaryl pyridine coupling. Differentiation of the pyridyl rings was accomplished via selective benzylation and then reduction of a pyridinium ring. The...
Erin E Meyers et al.
Pharmacology, biochemistry, and behavior, 130, 1-8 (2015-01-07)
The role of neuronal nicotinic acetylcholine receptors (nAChR) containing the β4 subunit in tolerance development and nicotinic binding site levels following chronic nicotine treatment was investigated. Mice differing in expression of the β4-nAChR subunit [wild-type (β4(++)), heterozygote (β4(+-)) and null...
Mariaelvina Sala et al.
British journal of pharmacology, 168(4), 835-849 (2012-09-11)
Many of the addictive and rewarding effects of nicotine are due to its actions on the neuronal nicotinic ACh receptor (nAChR) subtypes expressed in dopaminergic mesocorticolimbic cells. The partial agonists, cytisine and varenicline, are helpful smoking cessation aids. These drugs...
Yann S Mineur et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 40(4), 938-946 (2014-10-08)
Nicotinic acetylcholine receptor (nAChR) blockers potentiate the effects of selective serotonin reuptake inhibitors (SSRIs) in some treatment-resistant patients; however, it is not known whether these effects are independent, or whether the two neurotransmitter systems act synergistically. We first determined that...
Yann S Mineur et al.
Neuropharmacology, 52(5), 1256-1262 (2007-02-27)
The nicotine in tobacco is thought to modulate neuronal systems regulating mood. Moreover, it appears possible that blockade rather than activation of beta2-containing (beta2*) nicotinic acetylcholine receptors (nAChRs) may lead to antidepressant-like effects. We used cytisine, a partial agonist of...
Yu-Jiao Li et al.
Neurotoxicology, 34, 219-225 (2012-10-02)
Cytisine (CYT), one of the principal bioactive components derived from the seeds of Cytisus laborinum L, has been widely used for central nervous system (CNS) diseases treatment. The present study investigated the protective effect of CYT on cultured cortical neural...
Hiroto Kuwabara et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 53(1), 121-129 (2011-12-17)
There are only 2 currently available radioligands, 2-(18)F-FA and 6-(18)F-FA, for quantitative PET of the main cerebral subtype of nicotinic acetylcholine receptors (α4β2-nAChRs) in humans. Both exhibit slow distribution kinetics in the brain and require several hours for PET imaging....
Cytisine and the failure to market and regulate for human health.
Paul Aveyard et al.
Thorax, 68(11), 989-989 (2013-08-03)
Noah S Philip et al.
TheScientificWorldJournal, 2012, 104105-104105 (2012-05-24)
An important new area of antidepressant drug development involves targeting the nicotinic acetylcholine receptor (nAChR). This receptor, which is distributed widely in regions of the brain associated with depression, is also implicated in other important processes that are relevant to...
P A Iavich et al.
Georgian medical news, (201)(201), 65-69 (2012-02-07)
The aim of the research was to develop a method for quantitative determination of cytisine in Spartium junceum L. We used the above-ground parts of plants. In developing a method of analysis we used the method of 3-phase extraction. In...
Jean-François Etter
Archives of internal medicine, 166(15), 1553-1559 (2006-08-16)
Cytisine is an agonist of nicotinic receptors; in particular, it binds strongly with alpha(4)beta(2) nicotinic receptors. Cytisine has been used to treat tobacco dependence for 40 years in Eastern Europe. The objective of this study was to review the literature...
Kathryn M Albers et al.
Molecular pain, 10, 31-31 (2014-06-03)
Artemin (Artn), a member of the glial cell line-derived growth factor (GDNF) family, supports the development and function of a subpopulation of peptidergic, TRPV1-positive sensory neurons. Artn (enovin, neublastin) is elevated in inflamed tissue and its injection in skin causes...
Kasper Harpsøe et al.
The Journal of biological chemistry, 288(4), 2559-2570 (2012-12-12)
Deciphering which specific agonist-receptor interactions affect efficacy levels is of high importance, because this will ultimately aid in designing selective drugs. The novel compound NS3861 and cytisine are agonists of nicotinic acetylcholine receptors (nAChRs) and both bind with high affinity...
Jean-François Etter et al.
Drug and alcohol dependence, 92(1-3), 3-8 (2007-09-11)
Cytisine has a molecular structure somewhat similar to that of nicotine and varenicline. The concept for the new smoking cessation drug varenicline was based partly on cytisine. Like varenicline, cytisine is a partial agonist of nicotinic acetylcholine receptors, with high...
Can Peng et al.
The Journal of pharmacology and experimental therapeutics, 347(2), 424-437 (2013-08-21)
Partial agonist therapies for the treatment of nicotine addiction and dependence depend on both agonistic and antagonistic effects of the ligands, and side effects associated with other nAChRs greatly limit the efficacy of nicotinic partial agonists. We evaluated the in...
Prakash Rucktooa et al.
The Journal of biological chemistry, 287(28), 23283-23293 (2012-05-04)
Smoking cessation is an important aim in public health worldwide as tobacco smoking causes many preventable deaths. Addiction to tobacco smoking results from the binding of nicotine to nicotinic acetylcholine receptors (nAChRs) in the brain, in particular the α4β2 receptor....
Soo Hee Jeong et al.
Drug testing and analysis, 7(6), 475-482 (2014-09-19)
Cytisine, an α4 β2 nicotinic receptor partial agonist, is a plant alkaloid that is commercially extracted for use as a smoking cessation medication. Despite its long history of use, there is very little understanding of the pharmacokinetics of cytisine. To...
Kate Cahill et al.
The Cochrane database of systematic reviews, 4(4), CD006103-CD006103 (2012-04-20)
Nicotine receptor partial agonists may help people to stop smoking by a combination of maintaining moderate levels of dopamine to counteract withdrawal symptoms (acting as an agonist) and reducing smoking satisfaction (acting as an antagonist). The primary objective of this...
Anders Ettrup et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 52(9), 1449-1456 (2011-08-11)
Small-molecule α(7) nicotinic acetylcholine receptor (α(7)nAChR) agonists are currently validated for use as treatment for cognitive disturbances in schizophrenia and in Alzheimer disease. A suitable radiolabeled α(7)nAChR PET tracer would be important for in vivo quantification of α(7)nAChR binding in...
Hong Xu et al.
Journal of neurophysiology, 113(4), 1165-1174 (2014-11-28)
The caudal nucleus of the solitary tract (NTS) serves as the site of the first synapse for visceral sensory inputs to the central nervous system. The NTS sends functional projections to multiple brain nuclei, with gastric-related projections primarily targeting the...
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