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GSK-598809
GSK-598809 is a binding selectivity, selective dopamine D3 receptor, D3 receptor receptor antagonist, antagonist that is or was under development for the treatment of substance use disorder, substance-related disorders, smoking withdrawal, and eating disorders like binge eating disorder. The drug is highly selective for the dopamine D3 receptor (Ki = 6.2nM) over the dopamine D2 receptor, D2 receptor (Ki = 740nM) (~120-fold preference for the D3 receptor over the D2 receptor). A single dose of GSK-598809 achieved 72 to 89% occupancy of the D3 receptor in smokers. Side effects of GSK-598809 in clinical trials have included headache and somnolence with no sedation or extrapyramidal symptoms. This is in contrast to dopamine D2 receptor antagonists, which are associated with sedation, motor side effects, reduced locomotor activity, activity, and emotional blunting. However, GSK-598809 has been associated with cardiovascular side effects at high doses. It increases blood pressure in an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D3 Receptor
Dopamine receptor D3 is a protein that in humans is encoded by the ''DRD3'' gene. This gene encodes the D3 subtype of the dopamine receptor. The D3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that this receptor plays a role in cognitive and emotional functions. It is a target for drugs which treat schizophrenia, drug addiction, and Parkinson's disease. Alternative splicing of this gene results in multiple transcript variants that would encode different isoforms, although some variants may be subject to nonsense-mediated decay (NMD). On a side note, it is also the Dopamine Receptor sub-type possessing the highest binding affinity for Dopamine itself and may explain why non-ergoline Dopamine agonist, Dopamine Agonists are D3-preferring Function Alpha-synuclein (α-Syn) aggregation via Lewy bodies inclusion, a pathogenic signature exclusively present in PD patients, is decr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SB-277,011-A
SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist, which is around 80–100times selective for D3 over D2, and lacks any partial agonist activity. SB-277,011A is used in the study of addiction to stimulant drugs such as nicotine and cocaine. Where cocaine reduces the threshold for brain electrical self-stimulation in rats, an indication of cocaine's rewarding effects, SB-277,011A completely reverses this effect. It may thus be useful in the treatment of addiction to nicotine and cocaine, and is also being investigated for potential uses in the treatment of other drug addictions, such as addiction to heroin and alcohol. Another potential application for SB-277,011A is in the treatment of schizophrenia, and it may be particularly useful in treating comorbid patients who are both schizophrenic and addicted to drugs. However it may worsen side effects such as tardive dyskinesia in patients who are already prescribed antipsychotic drugs. S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PNU-99,194
PNU-99,194(A) (or U-99,194(A)) is a drug which acts as a moderately selective D3 receptor antagonist with ~15-30-fold preference for D3 over the D2 subtype. Though it has substantially greater preference for D3 over D2, the latter receptor does still play some role in its effects, as evidenced by the fact that PNU-99,194 weakly stimulates both prolactin secretion and striatal dopamine synthesis, actions it does not share with the more selective (100-fold) D3 receptor antagonists S-14,297 and GR-103,691. In rodent studies, low doses of PNU-99,194 produce conditioned place preference (CPP) with no effect on intracranial self-stimulation (ICSS), whereas low doses of D3 agonists like 7-OH-DPAT inhibit ICSS behavior and cause conditioned place aversion (CPA). In contrast, high doses of PNU-99,194 produce CPA and inhibit ICSS, while high doses of 7-OH-DPAT result in the opposite. Paralleling this, low doses of PNU-99,194 and 7-OH-DPAT induce hyperactivity and hypoactivity, r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nafadotride
Nafadotride is a dopamine antagonist with some selectivity for the D3 subtype (9.6-fold preference for D3 over D2).Pilla M, Perachon S, Sautel F, Garrido F, Mann A, Wermuth CG, Schwartz JC, Everitt BJ, Sokoloff P. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 agonist. ''Nature''. 1999;400:371–375. See also * GSK-598809 * PNU-99,194 * SB-277,011-A SB-277,011A is a drug which acts as a potent and selective dopamine D3 receptor antagonist, which is around 80–100times selective for D3 over D2, and lacks any partial agonist activity. SB-277,011A is used in the study of addiction to stimul ... References Carboxamides Dopamine antagonists Naphthol ethers Nitriles Pyrrolidines Methoxy compounds {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine
Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized by removing a carboxyl group from a molecule of its precursor chemical, L-DOPA, which is synthesized in the brain and kidneys. Dopamine is also synthesized in plants and most animals. In the brain, dopamine functions as a neurotransmitter—a chemical released by neurons (nerve cells) to send signals to other nerve cells. The brain includes several distinct dopamine pathways, one of which plays a major role in the motivational component of reward-motivated behavior. The anticipation of most types of rewards increases the level of dopamine in the brain, and many addictive drugs increase dopamine release or block its reuptake into neurons following release. Other brain dopamine pathways are involved in motor control and in controllin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D3 Antagonists
D3, D03, D.III, D III or D-3 may refer to: Transportation Roads * London Buses route D3, a Transport for London contracted bus route * D3 motorway (Czech Republic), a motorway in the Czech Republic * D3 road (Croatia), a state road in Croatia * D3 motorway (Slovakia), a motorway in northern Slovakia Aircraft * Albatros D.III, a 1916 German biplane fighter aircraft * Dewoitine D.3, a Dewoitine aircraft * Dunne D.3, a British Dunne aircraft * Fokker D.III, a 1916 German single-seat fighter aircraft * Mercedes D.III, a 1914 German 6-cylinder, liquid-cooled inline aircraft engine * Phönix D.III, a variant of the Austro-Hungarian First World War Phönix D.I biplane fighter * Pfalz D.III, a 1917 German fighter aircraft * Schütte-Lanz D.III, a 1918 German fighter aircraft prototype * Siemens-Schuckert D.III, a 1917 German prototype single-seat fighter aircraft Automobiles * Ford D3 platform, a full-size car automobile platform * Peugeot D3, a panel van manufactured from 1950 t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phases Of Clinical Research
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases start with testing for drug safety in a few human subjects, then expand to many study participants (potentially tens of thousands) to determine if the treatment is effective. Clinical research is conducted on drug candidates, vaccine candidates, new medical devices, and new diagnostic assays. Description Clinical trials testing potential medical products are commonly classified into four phases. The drug development process will normally proceed through all four phases over many years. When expressed specifically, a clinical trial phase is capitalized both in name and Roman numeral, such as "Phase I" clinical trial. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory aut ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Scientific Literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical contributions. These papers serve as essential sources of knowledge and are commonly referred to simply as "the literature" within specific research fields. The process of academic publishing involves disseminating research findings to a wider audience. Researchers submit their work to reputable journals or conferences, where it undergoes rigorous evaluation by experts in the field. This evaluation, known as peer review, ensures the quality, validity, and reliability of the research before it becomes part of the scientific literature. Peer-reviewed publications contribute significantly to advancing our understanding of the world and shaping future research endeavors. Original scientific research first published in scientific journals co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cocaine Use Disorder
Cocaine dependence is a neurological disorder that is characterized by withdrawal symptoms upon cessation from cocaine use. It also often coincides with cocaine addiction which is a biopsychosocial disorder characterized by persistent use of cocaine and/or crack despite substantial harm and adverse consequences. The Diagnostic and Statistical Manual of Mental Disorders (5th ed., abbreviated DSM-5), classifies problematic cocaine use as a stimulant use disorder. The International Classification of Diseases (11th rev., abbreviated ICD-11), includes "Cocaine dependence" as a classification (diagnosis) under "Disorders due to use of cocaine". The use of cocaine creates euphoria and high amounts of energy. If taken in large doses, it is possible to cause mood swings, paranoia, insomnia, psychosis, high blood pressure, a fast heart rate, panic attacks, seizures that are extremely difficult to control, cognitive impairments and drastic changes in personality. Cocaine overdose may resul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
