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Befiradol
Befiradol (F-13,640; NLX-112) is an experimental drug being studied for the treatment of levodopa-induced dyskinesia. It is a potent and selective 5-HT1A receptor full agonist. Pharmacology In recombinant cell lines expressing human 5-HT1A receptors, befiradol exhibits high agonist efficacy for a variety of signal transduction read-outs, including ERK phosphorylation, G-protein activation, receptor internalization and adenylyl cyclase inhibition. In rat hippocampal membranes it preferentially activates GalphaO proteins. In neurochemical experiments, befiradol activated 5-HT1A autoreceptors in rat dorsal Raphe nucleus as well as 5-HT1A heteroreceptors on pyramidal neurons in the frontal cortex. In rat models, it has powerful analgesic and antiallodynic effects comparable to those of high doses of opioid painkillers, but with fewer and less prominent side effects, as well as little or no development of tolerance with repeated use. A structure–activity relationship (SAR ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurolixis
Neurolixis is a biopharmaceutical company focused on novel drugs for the treatment of human central nervous system diseases. Neurolixis Inc. was founded in 2011 by Mark A. Varney, PhD, and Adrian Newman-Tancredi, PhD, DSc.. The company's therapeutic focus is on CNS disorders including Parkinson's disease, neurological orphan disorders, depression and cognitive deficits. The company has offices in USA and in France. In September 2013, Neurolixis in-licensed two clinical-phase drugs, befiradol and F-15599 from Pierre Fabre Group, Pierre Fabre Laboratories, a French pharmaceutical company. Befiradol (also known as NLX-112) is targeted to the treatment of movement disorders, notably dyskinesia in Parkinson's disease, whereas F-15599 (also known as NLX-101) is intended for the treatment of autism spectrum disorders including Rett syndrome and Fragile X syndrome. In addition, Neurolixis is developing its own novel chemical entities (NCEs), notably NLX-204 (see below). Development of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Levodopa-induced Dyskinesia
Levodopa-induced dyskinesia (LID) is a form of dyskinesia associated with levodopa (l-DOPA), used to treat Parkinson's disease. It often involves hyperkinetic movements, including chorea, dystonia, and athetosis. In the context of Parkinson's disease (PD), dyskinesia is often the result of long-term dopamine therapy. These motor fluctuations occur in up to 80% of PD patients after 5–10 years of l-DOPA treatment, with the percentage of affected patients increasing over time. Based on the relationship with levodopa dosing, dyskinesia most commonly occurs at the time of peak l-DOPA plasma concentrations and is thus referred to as peak-dose dyskinesia (PDD). As patients advance, they may present with symptoms of diphasic dyskinesia (DD), which occurs when the drug concentration rises or falls. If dyskinesia becomes too severe or impairs the patient's quality of life, a reduction in l-Dopa might be necessary, however this may be accompanied by a worsening of motor performance. The ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzothiophene
Benzothiophene is an aromatic organic compound with a molecular formula C8H6S and an odor similar to naphthalene (mothballs). It occurs naturally as a constituent of petroleum-related deposits such as lignite tar. Benzothiophene has no household use. In addition to benzo hiophene, a second isomer is known: benzo hiophene. Benzothiophene finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is found within the chemical structures of pharmaceutical drugs such as raloxifene, zileuton, and sertaconazole, and also BTCP. It is also used in the manufacturing of dyes such as thioindigo. Synthesis Most syntheses of benzothiophene create substituted benzothiophenes as a precursor to further reactions. An example is the reaction of an alkyne-substituted 2-bromobenzene with either sodium sulfide or potassium sulfide to form benzothiophene with an alkyl substitution at position 2. Thiourea Thiourea () is an organosulfur com ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Michael J
Michael may refer to: People * Michael (given name), a given name * he He ..., a given name * Michael (surname), including a list of people with the surname Michael Given name * Michael (bishop elect)">Michael (surname)">he He ..., a given name * Michael (surname), including a list of people with the surname Michael Given name * Michael (bishop elect), English 13th-century Bishop of Hereford elect * Michael (Khoroshy) (1885–1977), cleric of the Ukrainian Orthodox Church of Canada * Michael Donnellan (fashion designer), Michael Donnellan (1915–1985), Irish-born London fashion designer, often referred to simply as "Michael" * Michael (footballer, born 1982), Brazilian footballer * Michael (footballer, born 1983), Brazilian footballer * Michael (footballer, born 1993), Brazilian footballer * Michael (footballer, born February 1996), Brazilian footballer * Michael (footballer, born March 1996), Brazilian footballer * Michael (footballer, born 1999), Brazilian football ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
The Sunday Times
''The Sunday Times'' is a British Sunday newspaper whose circulation makes it the largest in Britain's quality press market category. It was founded in 1821 as ''The New Observer''. It is published by Times Newspapers Ltd, a subsidiary of News UK (formerly News International), which is owned by News Corp. Times Newspapers also publishes ''The Times''. The two papers, founded separately and independently, have been under the same ownership since 1966. They were bought by News International in 1981. In March 2020, ''The Sunday Times'' had a circulation of 647,622, exceeding that of its main rivals, '' The Sunday Telegraph'' and '' The Observer'', combined. While some other national newspapers moved to a tabloid format in the early 2000s, ''The Sunday Times'' retained the larger broadsheet format and has said that it intends to continue to do so. As of December 2019, it sold 75% more copies than its sister paper, ''The Times'', which is published from Monday to Saturday. Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Investigational New Drug
The United States Food and Drug Administration's Investigational New Drug (IND) program is the means by which a pharmaceutical industry, pharmaceutical company obtains permission to start human clinical trials and to ship an experimental drug interstate commerce, across state lines (usually to clinical investigators) before a marketing application for the drug has been approved. Regulations are primarily at . Similar procedures are followed in the European Union, Japan, and Canada due to regulatory harmonization efforts by the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use, International Council for Harmonisation. Types * Research or investigator INDs are non-commercial INDs filed by researchers to study an unapproved drug or to study an approved drug for a new indication or in a new patient population. * Expanded access, Emergency Use INDs, also called compassionate use or single-patient INDs, are filed for emergency use of a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parkinson's UK
Parkinson's UK is a Parkinson's research and support charity in the United Kingdom. In April 2010, the Parkinson's Disease Society changed its name to become Parkinson's UK. Its aims are to improve the quality of life for people affected by Parkinson's and find a cure for the condition. Parkinson's UK is the largest charity funder of research into Parkinson's in the UK. It funds research aimed at finding better treatments and improving the understanding of Parkinson's and its causes. It raises money through donations, legacies, community fundraising, events and corporate partnerships. The charity offers support and information to people affected by Parkinson's, their families and carers through a network of 350 local groups across England, Wales, Scotland and Northern Ireland. History The Parkinson's Disease Society (Parkinson's UK) was formed in February 1969 by Mali Jenkins (4 July 1907 – 11 March 1989). Initially the organisation had 3 simple aims: * to help patients and th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Levodopa-induced Dyskinesia
Levodopa-induced dyskinesia (LID) is a form of dyskinesia associated with levodopa (l-DOPA), used to treat Parkinson's disease. It often involves hyperkinetic movements, including chorea, dystonia, and athetosis. In the context of Parkinson's disease (PD), dyskinesia is often the result of long-term dopamine therapy. These motor fluctuations occur in up to 80% of PD patients after 5–10 years of l-DOPA treatment, with the percentage of affected patients increasing over time. Based on the relationship with levodopa dosing, dyskinesia most commonly occurs at the time of peak l-DOPA plasma concentrations and is thus referred to as peak-dose dyskinesia (PDD). As patients advance, they may present with symptoms of diphasic dyskinesia (DD), which occurs when the drug concentration rises or falls. If dyskinesia becomes too severe or impairs the patient's quality of life, a reduction in l-Dopa might be necessary, however this may be accompanied by a worsening of motor performance. The ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MPTP
MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is an organic compound. It is classified as a tetrahydropyridine. It is of interest as a precursor to the monoaminergic neurotoxin MPP+, which causes permanent symptoms of Parkinson's disease by destroying dopaminergic neurons in the substantia nigra of the brain. It has been used to study disease models in various animals. While MPTP itself has no psychoactive effects, the compound may be accidentally produced during the manufacture of MPPP, a synthetic opioid drug with effects similar to those of morphine and pethidine (meperidine). The Parkinson-inducing effects of MPTP were first discovered following accidental injection as a result of contaminated MPPP. Toxicity Injection of MPTP causes rapid onset of Parkinsonism, hence users of MPPP contaminated with MPTP will develop these symptoms. MPTP itself is not toxic, but it is a lipophilic compound and can therefore cross the blood–brain barrier. Once inside the brai ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Animal Models Of Parkinson's Disease
Animal models of Parkinson's disease are essential in the research field and widely used to study Parkinson's disease. Parkinson's disease is a Neurodegeneration, neurodegenerative disorder, characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta (SNpc). The loss of the dopamine neurons in the brain, results in motor dysfunction, ultimately causing the four cardinal symptoms of PD: tremor, rigidity, postural instability, and bradykinesia. It is the second most prevalent neurodegenerative disease, following Alzheimer's disease. It is estimated that nearly one million people could be living with PD in the United States. There are a variety of models that can be utilized to be able to address important aspects of Parkinson's disease. Researchers can consider disease progression, cell death, behavioral characteristics, and more PD phenotypes. Parkinson's disease animal models are divided into two categories: neurotoxin models and genetic models. Neuroto ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
The Michael J
''The'' is a grammatical article in English, denoting nouns that are already or about to be mentioned, under discussion, implied or otherwise presumed familiar to listeners, readers, or speakers. It is the definite article in English. ''The'' is the most frequently used word in the English language; studies and analyses of texts have found it to account for seven percent of all printed English-language words. It is derived from gendered articles in Old English which combined in Middle English and now has a single form used with nouns of any gender. The word can be used with both singular and plural nouns, and with a noun that starts with any letter. This is different from many other languages, which have different forms of the definite article for different genders or numbers. Pronunciation In most dialects, "the" is pronounced as (with the voiced dental fricative followed by a schwa) when followed by a consonant sound, and as (homophone of the archaic pronoun ''thee' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
