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Tavapadon
Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease. It is under development by Cerevel Therapeutics, which acquired tavapadon from Pfizer in 2018. It is taken by mouth. Tavapadon acts as a highly selective partial agonist of the dopamine D1 receptor (Ki = 9nM; = 65%) and the dopamine D5 receptor (Ki = 13nM; = 81%). It has no significant affinity or functional activity at the D2-like receptors ( D2, D3, D4) (Ki ≥ 4,870 to 6,720nM). Tavapadon also shows biased agonism for Gs-coupled signaling at the D1-like receptors. As of December 2024, tavapadon has completed phase 3 clinical trial 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 ...s for Parkinson's disease. See ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerevel Therapeutics
Cerevel Therapeutics Holdings, Inc. is an American biotechnology and pharmaceuticals company based in Cambridge, Massachusetts, focused on the development of novel therapies for mental and neurological illnesses. History Cerevel was established in October 2018. The company was formed in a collaboration between pharmaceuticals company Pfizer and private equity firm Bain Capital. In 2019, Cerevel appointed N. Anthony Coles as its chief executive officer. In 2020, Coles led Cerevel's effort to raise $445 million for brain drugs, the third largest biotech public listing at that time (after Legend Biotech and Moderna). In May 2023, Coles resigned from his position as CEO, yet retained his role as board chairman of Cerevel. In December 2023, American pharmaceutical company AbbVie announced its intention to acquire Cerevel for US$8.7 billion. The acquisition was completed in August 2024 with Cerevel becoming a subsidiary of Abbvie. Pipeline Cerevel uses novel approaches and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Razpipadon
Razpipadon (developmental codes CVL-871, PF-06669571, and PW-0464) is a dopamine receptor agonist which is under development for the treatment of dementia-related apathy. It is taken orally. Razpipadon acts as a selective partial agonist of the dopamine D1 and D5 receptors. The drug has been found to increase willingness to exert effort for rewards in humans and hence appears to show pro-motivational effects. The drug was originated by Pfizer and is under development by Cerevel Therapeutics. As of April 2022, razpipadon is in phase 2 clinical trials for dementia-related apathy. See also * 6-Br-APB * Mevidalen (LY-3154207) * Tavapadon Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist which is under development for the treatment of Parkinson's disease. It is under development by Cerevel Therapeutics, which acquired tavapadon from Pfizer i ... (CVL-751) References External links CVL-871 - AdisInsightCVL-871 - Cerevel Therapeutic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D4 Receptor
The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5. The structure of DRD4 was recently reported in complex with the antipsychotic drug nemonapride. As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many neurological and psychiatric conditions including schizophrenia and bipolar disorder, ADHD, addictive behaviors, Parkinson's disease, and eating disorders such as anorexia nervosa. A weak association has been drawn between DRD4 and borderline personality disorder. It is also a target for drugs which treat schizophrenia and Parkinson's disease. The D4 receptor is considered to be D2-like in which the activated receptor inhibits the enzyme adenylate cyclase, thereby reducing the intracellular concentration of the second messenger cyclic AMP. Genetics The human protein is coded by the ''DRD4'' on chromosome 11 located in ... [...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] |
Diketones
In organic chemistry, a dicarbonyl is a molecule containing two carbonyl () groups. Although this term could refer to any organic compound containing two carbonyl groups, it is used more specifically to describe molecules in which both carbonyls are in close enough proximity that their reactivity is changed, such as 1,2-, 1,3-, and 1,4-dicarbonyls. Their properties often differ from those of monocarbonyls, and so they are usually considered functional groups of their own. These compounds can have symmetrical or unsymmetrical substituents on each carbonyl, and may also be functionally symmetrical (dialdehydes, diketones, diesters, ''etc.'') or unsymmetrical (keto-esters, keto-acids, ''etc.''). 1,2-Dicarbonyls 1,2-Dialdehyde The only 1,2-dialdehyde is glyoxal, . Like many alkyldialdehydes, glyoxal is encountered almost exclusively as its hydrate and oligomers thereof. These derivatives often behave equivalently to the aldehydes since hydration is reversible. Glyoxal condenses ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D5 Receptor Agonists
D5 or D05 may refer to: Arts and fiction * '' Dedication 5'', a 2013 mixtape by American rapper Lil Wayne * D5 class Klingon starships, in the ''Star Trek'' science fiction series * Dimension Delete and Deadly Destruction Day, featured in '' Digimon Xros Wars'' Other uses * Digital 5, a network of leading digital governments * D5 HD, a professional digital video format * Demand 5, a video on demand website * The fifth D: All Things Digital, conference * Nikon D5, a 20.9 megapixel DSLR camera * Trident D5 ballistic missile * Volvo D5 engine, an engine family made by Volvo Cars Transport, aviation and logistics * Citroën D5 * Albatros D.V, a German World War I fighter plane * Identification symbol for ''Nachtjagdgeschwader'' 3, a Luftwaffe night fighter-wing of World War II * Dauair (IATA code D5) * Dublin 5, an Irish postal district * Land Rover D5 - Discovery 5 Roads * D5 motorway (Czech Republic) * D5 road (Croatia), a state road * Detour for the M5 South Wes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D1 Receptor Agonists
D1, D01, D.I, D.1 or D-1 can refer to: Science and technology Biochemistry and medicine * ATC code D01 ''Antifungals for dermatological use'', a subgroup of the Anatomical Therapeutic Chemical Classification System * Dopamine receptor D1, a protein * Haplogroup D1 (Y-DNA) * Vitamin D1, a form of Vitamin D * DI, Iodothyronine deiodinase type I, an enzyme involved with thyroid hormones Technology * Nikon D1, a digital single-lens reflex camera * D1, former brand of T-Mobile in Germany * D1, an abbreviation for DOCSIS 1.0 1.0, an international telecommunications standard * D-1 (Sony), an early digital video recording format * STS-61-A, also known as D-1, the 22nd mission of NASA's Space Shuttle program * D-1, from the Proton (rocket family), Russian rockets * Mercedes D.I, a 1913 German aircraft engine Military World War I fighter aircraft * AEG D.I * Albatros D.I * Halberstadt D.I, experimental version of Halberstadt D.II (and Aviatik D.I variant) * Aviatik (Berg) D.I * Daimler ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biased Ligands
Bias is an inclination toward something, or a predisposition, partiality, prejudice, preference, or predilection. Bias may also refer to: Scientific method and statistics * The bias introduced into an experiment through a confounder * Algorithmic bias, machine learning algorithms that exhibit politically unacceptable behavior * Cultural bias, interpreting and judging phenomena in terms particular to one's own culture * Funding bias, bias relative to the commercial interests of a study's financial sponsor * Infrastructure bias, the influence of existing social or scientific infrastructure on scientific observations * Publication bias, bias toward publication of certain experimental results * Bias (statistics), the systematic distortion of a statistic ** Biased sample, a sample falsely taken to be typical of a population ** Estimator bias, a bias from an estimator whose expectation differs from the true value of the parameter * Personal equation, a concept in 19th- and earl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mevidalen
Mevidalen (developmental code name LY-3154207) is a dopaminergic drug which is under development for the treatment of Lewy body disease, including those with Parkinson's disease. It acts as a selective positive allosteric modulator (PAM) of the dopamine D1 receptor. The drug is orally active and crosses the blood–brain barrier. It is a tetrahydroisoquinoline and is a close analogue of DETQ, another D1 receptor PAM. Mevidalen has been found to have wakefulness-promoting effects in sleep-deprived humans. Side effects of mevidalen have been reported to include increased heart rate and blood pressure, insomnia, dizziness, nausea, vomiting, anxiety, nervousness, fatigue, headaches, palpitations, and contact dermatitis, as well as falls in those with dementia. As of March 2022, mevidalen is in phase 2 clinical trials for the treatment of Lewy body disease. Besides for movement disorders and dementia, D1 receptor PAMs like mevidalen might have value in the treatment of certain neuro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
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 vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...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 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. Summary 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. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory authority for use in the general population. Phase IV trials are 'post-marketing' or 'surveillance' studies conducted to monitor safety over sever ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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