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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
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
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
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
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
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
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
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
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
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
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
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
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
Y E Slater et al.
Neuropharmacology, 44(4), 503-515 (2003-03-21)
Cytisine (cy) is a potent and competitive partial agonist at alpha4 subunit-containing nicotinic acetylcholine (nACh) receptors while at homomeric alpha7-nACh receptors it behaves as a full agonist with a relatively lower potency. In the present study, we assessed the effects
Ravi K Sajja et al.
Pharmacology, biochemistry, and behavior, 102(1), 36-43 (2012-06-29)
Alcohol and nicotine are commonly abused drugs in humans and evidence suggests that neuronal nicotinic acetylcholine receptors (nAChRs) in the midbrain dopamine system are common targets for the neurobehavioral interactions between alcohol (ethanol) and nicotine. The present study examined the
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
Cytisine--a tobacco treatment hiding in plain sight.
Nancy A Rigotti
The New England journal of medicine, 371(25), 2429-2430 (2014-12-18)
Yann S Mineur et al.
Science (New York, N.Y.), 332(6035), 1330-1332 (2011-06-11)
Smoking decreases appetite, and smokers often report that they smoke to control their weight. Understanding the neurobiological mechanisms underlying the anorexic effects of smoking would facilitate the development of novel treatments to help with smoking cessation and to prevent or
D S Turcanu et al.
Neuroscience letters, 516(2), 212-216 (2012-04-17)
Repeated stress is a major public health concern where many stress responses are mediated by neuronal nicotinic acetylcholine receptors. In the present study we evaluated the effects of the nicotinic receptor partial agonists, cytisine and its derivative 3-(pyridin-3'-yl)-cytisine (3-pyr-Cyt) on
Caterina Canu Boido et al.
Farmaco (Societa chimica italiana : 1989), 58(3), 265-277 (2003-03-07)
Neuronal nicotinic acetylcholine receptors (nAChRs) form a family of ACh-gated cation channels made up of different subtypes. They are widely distributed in peripheral and central nervous systems and are involved in complex cerebral processes as learning, memory, nociception, movement, etc.
Matthew R Costello et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 39(8), 1843-1851 (2014-02-12)
Tobacco dependence is difficult to treat, with the vast majority of those who try to quit relapsing within the first year. Improvements in smoking cessation therapies may be achieved by improving current preclinical research methods. However, most experimental tests in
Core modification of cytisine: a modular synthesis.
Christoph Hirschhäuser et al.
Angewandte Chemie (International ed. in English), 50(22), 5162-5165 (2011-04-27)
Jesse S Rodriguez et al.
Psychopharmacology, 231(23), 4455-4466 (2014-05-08)
Receptor mechanisms underlying the in vivo effects of nicotinic acetylcholine receptor (nAChR) drugs need to be determined to better understand possible differences in therapeutic potential. This study compared the effects of agonists that are reported either to differ in intrinsic
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