|
McN5652
McN5652 is a molecule that can be radiolabeled and then used as a radioligand in positron emission tomography (PET) studies. The [11C]-(+)-McN5652 enantiomer binds to the serotonin transporter. The radioligand is used for molecular neuroimaging and for imaging of the lungs. It was developed by Johnson & Johnson's McNeil Laboratories. According to McNeil, McN5652 was among the strongest SRI ever reported at the time of its discovery (sub nM Ki). However, it is not completely 5-HT selective: the racemate has 5-HT=0.68, NA=2.9, and D=36.8nM, whereas (+)-enantiomer has 5-HT=0.39, NA=1.8, and D=23.5 nM. Paroxetine was listed as 5-HT=0.44 nM, NA=20, and DA=460nM in the same paper by the same authors. Derivatives McN5652 and related structures have been analyzed for QSAR in terms of binding to the MAT receptor binding site. See also * DASB DASB, also known as 3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, is a compound that binds to the serotonin transport ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DASB
DASB, also known as 3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile, is a compound that binds to the serotonin transporter. Labeled with carbon-11 — a radioactive isotope — it has been used as a radioligand in neuroimaging with positron emission tomography (PET) since around year 2000. In this context it is regarded as one of the superior radioligands for PET study of the serotonin transporter in the brain, since it has high selectivity for the serotonin transporter. The DASB image from a human PET scan shows high binding in the midbrain, thalamus and striatum, moderate binding in the medial temporal lobe and anterior cingulate, and low binding in neocortex. The cerebellum is often regarded as a region with no specific serotonin transporter binding and the brain region is used as a reference in some studies. Since the serotonin transporter is the target of SSRIs used in the treatment of major depression it has been natural to examine DASB binding in de ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Positron Emission Tomography
Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in metabolic processes, and in other physiological activities including blood flow, regional chemical composition, and absorption. Different tracers are used for various imaging purposes, depending on the target process within the body, such as: * Fluorodeoxyglucose ( 18F">sup>18FDG or FDG) is commonly used to detect cancer; * 18Fodium fluoride">sup>18Fodium fluoride (Na18F) is widely used for detecting bone formation; * Oxygen-15 (15O) is sometimes used to measure blood flow. PET is a common imaging technique, a medical scintillography technique used in nuclear medicine. A radiopharmaceutical—a radioisotope attached to a drug—is injected into the body as a tracer. When the radiopharmaceutical undergoes beta plus decay, a positron is emitted, and when the positron interacts with an ordinary electron, the tw ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Radioligand
A radioligand is a microscopic particle which consists of a Radiopharmaceutical, therapeutic radioactive isotope and the cell-targeting compound - the ligand. The ligand is the target binding site, it may be on the surface of the targeted cancer cell for therapeutic purposes. Radioisotopes can occur naturally or be synthesized and produced in a cyclotron/nuclear reactor. The different types of radioisotopes include Y-90, H-3, C-11, Lu-177, Ac-225, Ra-223, In-111, I-131, I-125, etc. Thus, radioligands must be produced in special nuclear reactors for the radioisotope to remain stable. Radioligands can be used to analyze/characterize receptors, to perform binding assays, to help in diagnostic imaging, and to provide targeted cancer therapy. Radiation is a novel method of treating cancer and is effective in short distances along with being unique/personalizable and causing minimal harm to normal surrounding cells. Furthermore, radioligand binding can provide information about receptor-l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enantiomer
In chemistry, an enantiomer (Help:IPA/English, /ɪˈnænti.əmər, ɛ-, -oʊ-/ Help:Pronunciation respelling key, ''ih-NAN-tee-ə-mər''), also known as an optical isomer, antipode, or optical antipode, is one of a pair of molecular entities which are mirror images of each other and non-superposable. Enantiomer molecules are like right and left hands: one cannot be superposed onto the other without first being converted to its mirror image. It is solely a relationship of chirality (chemistry), chirality and the permanent three-dimensional relationships among molecules or other chemical structures: no amount of re-orientation of a molecule as a whole or conformational isomerism, conformational change converts one chemical into its enantiomer. Chemical structures with chirality rotate plane-polarized light. A mixture of equal amounts of each enantiomer, a ''racemic mixture'' or a ''racemate'', does not rotate light. Stereoisomers include both enantiomers and diastereomers. Diaste ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Transporter
The serotonin transporter (SERT or 5-HTT) also known as the sodium-dependent serotonin transporter and solute carrier family 6 member 4 is a protein that in humans is encoded by the SLC6A4 gene. SERT is a type of monoamine transporter protein that transports the neurotransmitter serotonin from the synaptic cleft back to the presynaptic neuron, in a process known as serotonin reuptake. This transport of serotonin by the SERT protein terminates the action of serotonin and recycles it in a sodium-dependent manner. Many antidepressant medications of the SSRI and tricyclic antidepressant classes work by binding to SERT and thus reducing serotonin reuptake. It is a member of the sodium:neurotransmitter symporter family. A repeat length polymorphism in the promoter of this gene has been shown to affect the rate of serotonin uptake and may play a role in sudden infant death syndrome, aggressive behavior in Alzheimer disease patients, post-traumatic stress disorder and depression ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuroimaging
Neuroimaging is the use of quantitative (computational) techniques to study the neuroanatomy, structure and function of the central nervous system, developed as an objective way of scientifically studying the healthy human brain in a non-invasive manner. Increasingly it is also being used for quantitative research studies of brain disease and psychiatric illness. Neuroimaging is highly multidisciplinary involving neuroscience, computer science, psychology and statistics, and is not a medical specialty. Neuroimaging is sometimes confused with neuroradiology. Neuroradiology is a medical specialty that uses non-statistical brain imaging in a clinical setting, practiced by radiologists who are medical practitioners. Neuroradiology primarily focuses on recognizing brain lesions, such as vascular diseases, strokes, tumors, and inflammatory diseases. In contrast to neuroimaging, neuroradiology is qualitative (based on subjective impressions and extensive clinical training) but sometime ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Johnson & Johnson
Johnson & Johnson (J&J) is an American multinational pharmaceutical, biotechnology, and medical technologies corporation headquartered in New Brunswick, New Jersey, and publicly traded on the New York Stock Exchange. Its common stock is a component of the Dow Jones Industrial Average, and the company is ranked No. 42 on the 2024 ''Fortune'' 500 list of the largest United States corporations. In 2024, the company was ranked 45th in the ''Forbes'' Global 2000. Johnson & Johnson has a global workforce of approximately 138,000 employees who are led by the company's current chairman and chief executive officer, Joaquin Duato. Johnson & Johnson was founded in 1886 by three brothers, Robert Wood Johnson, James Wood Johnson, and Edward Mead Johnson, selling ready-to-use sterile surgical dressings. In 2023, the company split-off its consumer healthcare business segment into a new publicly traded company, Kenvue. The company is exclusively focused on developing and producing ph ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
McNeil Laboratories
McNeil Consumer Healthcare is an American medicals products company belonging to Kenvue consumer health group. It primarily sells fast-moving consumer goods such as Over-the-counter drug, over-the-counter drugs. History The company was founded on March 16, 1879, by 23-year-old Robert McNeil, who paid $167 for a Pharmacy, drugstore complete with fixtures, inventory and soda fountain, as a retail pharmacy, in the Kensington, Philadelphia, Pennsylvania, Kensington section of Philadelphia, Philadelphia, Pennsylvania, United States. Robert McNeil was a graduate of the Philadelphia College of Pharmacy and Science (University of the Sciences in Philadelphia). In 1904, one of McNeil's sons, Robert Lincoln McNeil, became part of the company and together they created McNeil Laboratories in 1933. The company would focus on direct marketing of prescription drugs to hospitals, pharmacists, and doctors. Development of acetaminophen began under the leadership of Robert L. McNeil, Jr., who late ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JNJ-7925476
JNJ-7925476 is a triple reuptake inhibitor antidepressant discovered by Johnson & Johnson, but never marketed. These molecules were first prepared by Bruce E. Maryanoff and coworkers during the late 1970s–1980s. The structure is a pyrroloisoquinoline core, with an overlaid benzhydryl motif. Incorporating the pyrrolidine, pyrrolidino ring onto the tetrahydroisoquinoline scaffolding markedly improves potency, although this only works for one of the available stereoisomers. JNJ-7925476 is a racemic preparation of the more potent diastereomer. Of these enantiomers, the eutomer is the (6''R'',10b''S'') stereoisomer, known as JNJ-39836966, and the distomer, (6''S'',10b''R''), is JNJ-39836732 There is some confusion over the nomenclature and Cis–trans isomerism, ''cis''/''trans'' isomeric relationship at the piperidine ring. The compounds as depicted have the carbon of the pyrrolidine carbon and the phenyl ''cis'', but Maryanoff and coworkers are of the opinion that the compound ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Radiopharmaceuticals
Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which is different from contrast media which absorb or alter external electromagnetism or ultrasound. Radiopharmacology is the branch of pharmacology that specializes in these agents. The main group of these compounds are the radiotracers used to diagnose dysfunction in body tissues. While not all medical isotopes are radioactive, radiopharmaceuticals are the oldest and remain the most common of such drugs. Drug nomenclature As with other pharmaceutical drugs, there is standardization of the drug nomenclature for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Names (INNs), United States Pharmacopeia (USP) names, and IUPAC names for these agents are usually similar other than trivial style di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
