|
α4β2
The alpha-4 beta-2 nicotinic receptor, also known as the α4β2 receptor, is a type of nicotinic acetylcholine receptor implicated in learning, consisting of α4 and β2 subunits. It is located in the brain, where activation yields post- and presynaptic excitation, mainly by increased Na+ and K+ permeability. Stimulation of this receptor subtype is also associated with growth hormone secretion. People with the inactive CHRNA4 mutation Ser248Phe are an average of 10 cm (4 inches) shorter than average and predisposed to obesity. A 2015 review noted that stimulation of the α4β2 nicotinic receptor in the brain is responsible for certain improvements in attentional performance; among the nicotinic receptor subtypes, nicotine has the highest binding affinity at the α4β2 receptor (ki=1 ), which is also the primary biological target that mediates nicotine's addictive properties. The receptors exist in the two stoichiometries: *(α4)2(β2)3 receptors have high sensitivi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nicotine
Nicotine is a naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve withdrawal symptoms. Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist. Nicotine constitutes approximately 0.6–3.0% of the dry weight of tobacco. Nicotine is also present at ppb-concentrations in edible plants in the family Solanaceae, including potatoes, tomatoes, and eggplants, though sources disagree on whether this has any biological significance to human consumers. It functions as an antiherbivore toxin; consequently, nicotine was widely used as an insecticide in the past, and neonicotinoids (structurally similar to nicotine), such as imidacloprid, are s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nicotine
Nicotine is a naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve withdrawal symptoms. Nicotine acts as a receptor agonist at most nicotinic acetylcholine receptors (nAChRs), except at two nicotinic receptor subunits (nAChRα9 and nAChRα10) where it acts as a receptor antagonist. Nicotine constitutes approximately 0.6–3.0% of the dry weight of tobacco. Nicotine is also present at ppb-concentrations in edible plants in the family Solanaceae, including potatoes, tomatoes, and eggplants, though sources disagree on whether this has any biological significance to human consumers. It functions as an antiherbivore toxin; consequently, nicotine was widely used as an insecticide in the past, and neonicotinoids (structurally similar to nicotine), such as imidacloprid, are s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epiboxidine
Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It was developed as a less toxic analogue of the potent frog-derived alkaloid epibatidine, which is around 200 times stronger than morphine as an analgesic but produces extremely dangerous toxic nicotinic side effects. Epiboxidine is around one-tenth as potent as epibatidine as an α4β2 agonist, but has around the same potency as an α3β4 agonist. It has only one-tenth of the analgesic power of epibatidine, but is also much less toxic. Uses Despite its decreased potency and toxicity compared to epibatidine, epiboxidine itself is still too toxic to be developed as a drug for use in humans. It is used in scientific research and as a parent compound to derive newer analogues which may be safer and have greater potential for clinical development. See also * ABT-418 ABT-418 is a drug developed by Abbott, tha ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epibatidine
Epibatidine is a chlorinated alkaloid that is secreted by the Ecuadoran frog '' Epipedobates anthonyi'' and poison dart frogs from the Ameerega genus. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated until 1992. Whether epibatidine is the first observed example of a chlorinated alkaloid remains controversial, due to challenges in conclusively identifying the compound from the limited samples collected by Daly. By the time that high-resolution spectrometry was used in 1991, there remained less than one milligram of extract from Daly's samples, raising concerns about possible contamination. Samples from other batches of the same species of frog failed to yield epibatidine. Epibatidine is toxic. Its toxicity stems from its ability to interact with nicotinic and muscarinic acetylcholine receptors. These receptors are involved in the transmission of painful sensations, and in movement, among other functions. Epibatidine then causes numbness ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nicotinic Acetylcholine Receptor
Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral nervous system, muscle, and many other tissues of many organisms. At the neuromuscular junction they are the primary receptor in muscle for motor nerve-muscle communication that controls muscle contraction. In the peripheral nervous system: (1) they transmit outgoing signals from the presynaptic to the postsynaptic cells within the sympathetic and parasympathetic nervous system, and (2) they are the receptors found on skeletal muscle that receive acetylcholine released to signal for muscular contraction. In the immune system, nAChRs regulate inflammatory processes and signal through distinct intracellular pathways. In insects, the cholinergic system is limited to the central nervous system. The nicotinic receptors are considered cholinergi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cytisine
Cytisine, also known as baptitoxine, cytisinicline, or sophorine, is an alkaloid that occurs naturally in several plant genera, such as ''Laburnum'' and ''Cytisus'' of the family Fabaceae. It has been used medically to help with smoking cessation. Although widely used for smoking cessation in Eastern Europe, cytisine remains relatively unknown beyond it. However, it has been found effective in several randomized clinical trials, including some in the United States and a large one in New Zealand, and is being investigated in additional trials in the United States (being conducted by Achieve Life Sciences) and a non-inferiority trial in Australia in which it is being compared head-to-head with the smoking cessation aid varenicline (sold in the United States as Chantix). It has also been used entheogenically via mescalbeans by some Native American groups, historically in the Rio Grande Valley predating even peyote. Sources Cytisine is extracted from the seeds of ''Cytisus la ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ispronicline
Ispronicline (TC-1734, AZD-3480) is an experimental drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease, but is no longer under development. It has also progressed to phase II as a potential treatment for ADHD. With dosages of 50mg day showing a significant improvement in ADHD symptoms Ispronicline is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects. Early stage clinical trials showed that ispronicline was well tolerated, with the main side effects being dizziness and headache. However, mid stage clinical trials failed to show sufficient efficacy to continue development as a pharmaceutical drug. See also * Rivanicline Rivanicline (TC-2403, RJR-2403, (E)-metanicotine) is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dianicline
Dianicline (SSR-591,813) is a drug developed by Sanofi-Aventis which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It is being developed as a medication for the treatment of nicotine dependence to assist in smoking cessation. Dianicline is very similar to the already marketed drug varenicline Varenicline (trade name Chantix and Champix) is a medication used for smoking cessation. Varenicline is also used for the treatment of dry eye disease. The most common side-effects include nausea (feeling sick), insomnia (difficulty sleeping), a ... and it is unclear what advantages it will have over the older drug, although it may have an improved side effect profile. It has been through human trials up to Phase II, although results have not yet been reported. Drug development has been discontinued after reporting of unfavourable results during Phase III trials. References {{Nicotinic acetyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Altinicline
Altinicline (SIB-1508Y, SIB-1765F) is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It stimulates release of dopamine and acetylcholine in the brain in both rodent and primate models, and progressed as far as Phase II clinical trials for Parkinson's disease Parkinson's disease (PD), or simply Parkinson's, is a long-term degenerative disorder of the central nervous system that mainly affects the motor system. The symptoms usually emerge slowly, and as the disease worsens, non-motor symptoms becom ..., where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear. References Nicotinic agonists Stimulants Pyridines Pyrrolidines Ethynyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
A-366,833
A-366,833 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors selective for the α4β2 subtype, and has been researched for use as an analgesic, although it has not passed clinical trials Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar .... Its structure has a nicotinonitrile ( 3-cyanopyridine) core bound through C5 to the N6 of (1''R'',5''S'')-3,6-diazabicyclo .2.0eptane. References Analgesics Azetidines Nicotinic agonists Nitriles Pyridines Pyrrolidines Stimulants {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
A-84,543
A-84543 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype. It is widely used in scientific research into the structure and function of this receptor subtype and has been the lead compound A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, b ... for the development of a large family of related derivatives. References Nicotinic agonists Aromatic ethers 3-Pyridyl compounds Pyrrolidines Stimulants {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Galantamine
Galantamine is used for the treatment of cognitive decline in mild to moderate Alzheimer's disease and various other memory impairments. It is an alkaloid that has been isolated from the bulbs and flowers of ''Galanthus nivalis'' (Common snowdrop), ''Galanthus caucasicus'' (Caucasian snowdrop), '' Galanthus woronowii'' (Voronov's snowdrop), and some other members of the family '' Amaryllidaceae'', such as ''Narcissus'' (daffodil), '' Leucojum aestivum'' (snowflake), and ''Lycoris'' including ''Lycoris radiata'' (red spider lily). It can also be produced synthetically. Studies of usage in modern medicine began in the Soviet Union in the 1950s. Galantamine was isolated for the first time from bulbs of ''Galanthus nivalis'' (common snowdrop) by the Bulgarian chemist D. Paskov and his team in 1956. The active ingredient was extracted, identified, and studied, in particular in relation to its acetylcholinesterase (AChE)-inhibiting properties. The first industrial process was devel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
