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Nolomirole
Nolomirole (; developmental code name CHF-1035), also known as 5,6-diisobutyryloxy-''N''-methyl-2-aminotetralin, is a dual dopamine D2 and α2-adrenergic receptor agonist which was under development for the treatment of heart failure but was never marketed. It is taken orally. Pharmacology The drug acts as an agonist of the dopamine D2 receptor, with an affinity (Ki) of 120nM for the (–)- enantiomer and 2,400nM for the (+)- enantiomer, and as an agonist of the α2-adrenergic receptor, with an affinity (Ki) of 130nM for the (–)- enantiomer and 1,600nM for the (+)- enantiomer. It is a prodrug of CHF-1024 (5,6-dihydroxy-''N''-methyl-2-aminotetralin), to which it is rapidly hydrolyzed by circulating esterase enzymes. The elimination half-life of nolomirole is said to be 3hours and its log P is 1.97. Chemistry Nolomirole and its active form CHF-1024 are cyclized phenethylamines and 2-aminotetralin analogues of the catecholamine neurotransmitter dopamine and its ''N''-m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CHF-1024
CHF-1024, also known as 5,6-dihydroxy-2-methylaminotetralin, is a dopamine D2 receptor agonist and α2-adrenergic receptor agonist of the 2-aminotetralin family. It is a cyclized phenethylamine analogue of the neurotransmitter dopamine. The drug is the active form of nolomirole (CHF-1035), a prodrug of CHF-1024 and the ''N'',''N''-diisobutyryl diester of the compound. Nolomirole was investigated for the treatment of heart failure but was never marketed. See also * Chiesi Farmaceutici * Nolomirole * Cyclized phenethylamine * Rotigotine * 5-OH-DPAT * 7-OH-DPAT 7-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with reasonable selectivity for the D3 receptor subtype, and low affinity for serotonin receptors, unlike its structural isomer 8-OH-DPAT. 7-OH-DPAT is self-administer ... * Carmoxirole References 2-Aminotetralins Alpha-2 adrenergic receptor agonists Catecholamines D2 receptor agonists Human drug metabolites {{Cardiovascul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), 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 able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Log P
Log most often refers to: * Trunk (botany), the stem and main wooden axis of a tree, called logs when cut ** Logging, cutting down trees for logs ** Firewood, logs used for fuel ** Lumber or timber, converted from wood logs * Logarithm, in mathematics Log, LOG or LoG may also refer to: Arts, entertainment and media * ''Log'' (magazine), an architectural magazine * ''The Log'', a boating and fishing newspaper published by the Duncan McIntosh Company * Lamb of God (band) or LoG, an American metal band * The Log, an electric guitar by Les Paul * Log, a fictional product in ''The Ren & Stimpy Show'' * The League of Gentlemen or LoG, a British comedy show. Places * Log, Russia, the name of several places * Log, Slovenia, the name of several places Science and mathematics *Logarithm, a mathematical function * Log file, a computer file in which events are recorded * Laplacian of Gaussian or LoG, an algorithm used in digital image processing Other uses * Logbook, or log, a record ... [...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 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] |
Chiesi Farmaceutici
Chiesi Farmaceutici S.p.A. is an Italian family controlled global pharmaceutical company based in Parma, Emilia-Romagna. Chiesi has 31 affiliates in the world, nearly 6,500 total employees and provides medicines to patients in 100 nations. Chiesi currently has revenues of 3 billion euros. According to 2020 official data from the European Patent Office (EPO), Chiesi Group, with 42 patents filed, is confirmed as the first Italian Pharmaceutical Company and third among Italian Companies across all sectors for filing the highest number of patents. In June 2019, Chiesi became a certified B Corporation, thus choosing to adopt a new legal status under US and Italian law. This ensures Chiesi legal protection to pursue a business model placing social and environmental values on equal footing with profits. Following the acquisition, in 1999, of Huddersfield based Trinity Pharmaceuticals, Chiesi has also had a significant presence in Manchester, United Kingdom. History Established in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmaceutical Company
The pharmaceutical industry is a Medicine, medical industry that discovers, develops, produces, and markets pharmaceutical goods such as medications and medical devices. Medications are then administered to (or Self-medicate, self-administered by) patients for curing or preventing disease or for alleviating symptoms of illness or injury. List of pharmaceutical companies, Pharmaceutical companies may deal in Generic drug, generic drugs, branded drugs, or both, in different contexts. Generic materials are without the involvement of intellectual property, whereas branded materials are protected by Chemical patent, chemical patents. The industry's various subdivisions include distinct areas, such as manufacturing Biopharmaceutical, biologics and total synthesis. The industry is subject to a Legal drug trade, variety of laws and regulations that govern the patenting, efficacy testing, Drug safety, safety evaluation, and marketing of these drugs. The global pharmaceutical market produ ... [...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] |
Epinine
Deoxyepinephrine, also known by the common names ''N''-methyldopamine and epinine, is an organic compound and natural product that is structurally related to the important neurotransmitters dopamine and epinephrine. All three of these compounds also belong to the catecholamine family. The pharmacology of epinine largely resembles that of its "parent", dopamine. Epinine has been found in plants, insects and animals. It is also of significance as the active metabolic breakdown product of the prodrug ibopamine, which has been used to treat congestive heart failure. Occurrence Epinine does not seem to occur widely, but it is present as a minor alkaloid in some plants, such as the peyote cactus, ''Lophophora williamsii'', and a species of ''Acacia'', as well as in Scotch Broom, ''Cytisus scoparius''. This compound has also been isolated from the adrenal medulla of pigs and cows, and from the toad, ''Rhinella marina''. It has also been detected in the locust, ''Locusta migratoria''. C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Derivative
In chemistry, a derivative is a compound that is derived from a similar compound by a chemical reaction. In the past, derivative also meant a compound that ''can be imagined to'' arise from another compound, if one atom or group of atoms is replaced with another atom or group of atoms, but modern chemical language now uses the term structural analog for this meaning, thus eliminating ambiguity. The term "structural analogue" is common in organic chemistry. In biochemistry, the word is used for compounds that at least theoretically can be formed from the precursor compound. Chemical derivatives may be used to facilitate analysis. For example, melting point (MP) analysis can assist in identification of many organic compounds. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is availa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methyl Group
In organic chemistry, a methyl group is an alkyl derived from methane, containing one carbon atom bonded to three hydrogen atoms, having chemical formula (whereas normal methane has the formula ). In formulas, the group is often abbreviated as Me. This hydrocarbon group occurs in many organic compounds. It is a very stable group in most molecules. While the methyl group is usually part of a larger molecule, bonded to the rest of the molecule by a single covalent bond (), it can be found on its own in any of three forms: methanide anion (), methylium cation () or methyl radical (). The anion has eight valence electrons, the radical seven and the cation six. All three forms are highly reactive and rarely observed. Methyl cation, anion, and radical Methyl cation The methylium cation () exists in the gas phase, but is otherwise not encountered. Some compounds are considered to be sources of the cation, and this simplification is used pervasively in organic chemistry. For ex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotransmitters are released from synaptic vesicles into the synaptic cleft where they are able to interact with neurotransmitter receptors on the target cell. Some neurotransmitters are also stored in large dense core vesicles. The neurotransmitter's effect on the target cell is determined by the receptor it binds to. Many neurotransmitters are synthesized from simple and plentiful precursors such as amino acids, which are readily available and often require a small number of biosynthetic steps for conversion. Neurotransmitters are essential to the function of complex neural systems. The exact number of unique neurotransmitters in humans is unknown, but more than 100 have been identified. Common neurotransmitters include Glutamate (neurotransmi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
