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α4β2 Nicotinic Receptor
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 sensit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nicotinic Acetylcholine Receptor
Nicotinic acetylcholine receptors, or nAChRs, are Receptor (biochemistry), 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 nervous system, 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. ... [...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. It has been found effective in several randomized clinical trials, including in the United States and New Zealand, and is being investigated in additional trials in the United States 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 laburnum'' L. (Golden Rain acacia), and is found in several genera of the subfamily Faboideae of the family Fabaceae, including '' Laburnum'', '' Anagyris'', '' Thermopsis'', '' C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pozanicline
Pozanicline (INN, codenamed ABT-089) is a drug developed by Abbott, that has nootropic and neuroprotective effects. Animal studies suggested it useful for the treatment of ADHD and subsequent human trials have shown ABT-089 to be effective for this application. It binds with high affinity subtype-selective to the α4β2 nicotinic acetylcholine receptors 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 ner ... and has partial agonism to the α6β2 subtype, but not the α7 and α3β4 subtypes familiar to nicotine. It has particularly low tendency to cause side effects compared to other drugs in the class. Synthesis Pozanicline is synthesized from 2-methyl-3-hydroxypyridine and Boc-L-Prolinol through a dehydration reaction followed by deprotection of the nitrogen atom of prolinol ... [...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 50 mg/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 Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as '' effectiveness'', and it has often been used synonymously, although in pharmacology a distinction is no ... [...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 Smoking cessation, usually called quitting smoking or stopping smoking, is the process of discontinuing tobacco smoking. Tobacco smoke contains nicotine, which is Addiction, addictive and can cause Substance dependence, dependence. As a resu .... Dianicline is very similar to the already marketed drug varenicline 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 acet ... [...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 neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become ..., where "no antiparkinsonian or cognitive-enhancing effects were demonstrated", although its current status is unclear. References Nicotinic agonists Stimulants Disubstituted pyridines Pyrrolidines Ethynyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Behavioural Pharmacology
Behavior (American English) or behaviour (British English) is the range of actions of individuals, organisms, systems or artificial entities in some environment. These systems can include other systems or organisms as well as the inanimate physical environment. It is the computed response of the system or organism to various stimuli or inputs, whether internal or external, conscious or subconscious, overt or covert, and voluntary or involuntary. While some behavior is produced in response to an organism's environment (extrinsic motivation), behavior can also be the product of intrinsic motivation, also referred to as "agency" or "free will". Taking a behavior informatics perspective, a behavior consists of actor, operation, interactions, and their properties. This can be represented as a behavior vector. Models Biology Definition Behavior may be defined as "the internally coordinated responses (actions or inactions) of whole living organisms (individuals or groups) to in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arecoline
Arecoline is a cholinergic agent, stimulant, and natural product, naturally occurring alkaloid found in areca nut, areca (betel) nuts of the areca palm (''Areca catechu'') found in South Asia, South and Southeast Asia. Its effects, depending on the dose, include stimulation, alertness, increased concentration, nootropic, cognitive enhancement, mood lift, elation, euphoriant, euphoria, aphrodisiac, pro-sexual effects, mental relaxation, relaxation, anxiolytic, reduced anxiety, and sedation, as well as drug addiction, addiction and drug withdrawal, withdrawal symptoms upon drug discontinuation, discontinuation. Its effects are described as subtle and it has been likened to a strong cup of coffee. There are also active constituents of areca nuts, but arecoline is the key active component, with a percentage of ~0.3 to 0.6%. Areca nuts are drug administration, administered by chewing for 5 to 20minutes without swallowing. Side effects of arecoline include hypersalivation, hypotensio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ABT-418
ABT-418 is a drug developed by Abbott, that has nootropic, neuroprotective and anxiolytic effects, and has been researched for treatment of both Alzheimer's disease and ADHD. It acts as an agonist at neural nicotinic acetylcholine receptors, subtype-selective binding with high affinity to the α4β2, α7/ 5-HT3, and α2β2 nicotinic acetylcholine receptors but not α3β4 receptors ABT-418 was reasonably effective for both applications and fairly well tolerated, but produced some side effects, principally nausea, and it is unclear whether ABT-418 itself will proceed to clinical development or if another similar drug will be used instead. See also * Epiboxidine * Anabaseine Anabaseine (3,4,5,6-tetrahydro-2,3′-bipyridine) is an alkaloid toxin produced by ''Nemertines'' worms and ''Aphaenogaster'' ants. It is structurally similar to nicotine and anabasine. Similarly, it has been shown to act as an agonist on most ni ... References Isoxazoles Nicotinic ago ... [...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 subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v .... 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 3-Aminopyridines 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 receptor Nicotinic acetylcholine receptors, or nAChRs, are Receptor (biochemistry), receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the c ...s 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 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] |
Nicotine
Nicotine is a natural product, naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreational drug use, recreationally as a stimulant and anxiolytic. As a pharmaceutical drug, it is used for smoking cessation to relieve drug withdrawal, 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 Parts-per notation, 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 plant defense against herbivory, antiherbivore toxin; consequently, nicotine was widely used as an insecti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
