Showing 1-30 of 56 resultados for "C2899"
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...
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...
Jotham W Coe et al.
Journal of medicinal chemistry, 48(10), 3474-3477 (2005-05-13)
Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified for smoking cessation. Neuronal nicotinic acetylcholine receptors (nAChRs) mediate the dependence-producing effects of nicotine. We have pursued alpha4beta2 nicotinic receptor partial agonists to inhibit...
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...
Daniel Yohannes et al.
Bioorganic & medicinal chemistry letters, 18(7), 2316-2319 (2008-03-22)
A novel fused tricyclic analog (11) of cytisine has been prepared (coined 'cyfusine') and determined to have high affinity at neuronal nicotinic acetylcholine receptors. A [3+2] cycloaddition protocol permitted entry into a 3,4-differentially difunctionalized dihydropyrrole (7). The penultimate cyclization was...
Jotham W Coe et al.
Bioorganic & medicinal chemistry letters, 15(22), 4889-4897 (2005-09-21)
3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha4beta2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha4beta2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements...
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...
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Anders A Jensen et al.
Journal of medicinal chemistry, 48(15), 4705-4745 (2005-07-22)
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...
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...
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...
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...
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...
Sheela K Chellappan et al.
Journal of medicinal chemistry, 49(9), 2673-2676 (2006-04-28)
We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar...
Nicolas Houllier et al.
Bioorganic & medicinal chemistry letters, 20(22), 6667-6670 (2010-10-01)
(-)-9-Fluorocytisine, (-)-9-methylcytisine and (-)-9-trifluoromethylcytisine were synthesized from the natural product (-)-cytisine. 9-Methyl and 9-trifluoromethyl cytisines display a remarkable affinity at the α(4)β(2) nicotinic receptor subtype (0.2 nM) with a high selectivity versus the α(7) nAChR subtype. Comparison of the affinity...
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...
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...
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...
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...
Paulo César Ghedini et al.
Brain research, 1483, 96-104 (2012-09-22)
Lack of dystrophin in Duchenne muscle dystrophy (DMD) and in the mutant mdx mouse results in progressive muscle degeneration, structural changes at the neuromuscular junction, and destabilization of the nicotinic acetylcholine receptors (nAChRs). One-third of DMD patients also present non-progressive...
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...
Juan Andrés Abin-Carriquiry et al.
Bioorganic & medicinal chemistry letters, 20(12), 3683-3687 (2010-05-25)
Homology models of nicotinic acetylcholine receptors (nAChRs) suggest that subtype specificity is due to non-conserved residues in the complementary subunit of the ligand-binding pocket. Cytisine and its derivatives generally show a strong preference for heteromeric alpha4beta2* nAChRs over the homomeric...
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...
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...

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