DASB
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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 depre ...
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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-suscepti ...
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Carbon-11
Carbon (6C) has 15 known isotopes, from to , of which and are stable. The longest-lived radioisotope is , with a half-life of years. This is also the only carbon radioisotope found in nature—trace quantities are formed cosmogenically by the reaction + → + . The most stable artificial radioisotope is , which has a half-life of . All other radioisotopes have half-lives under 20 seconds, most less than 200 milliseconds. The least stable isotope is , with a half-life of . List of isotopes , - , , style="text-align:right" , 6 , style="text-align:right" , 2 , , [] , proton emission, 2p , Subsequently decays by double proton emission to for a net reaction of → + 4 , 0+ , , , - , rowspan=3, , rowspan=3 style="text-align:right" , 6 , rowspan=3 style="text-align:right" , 3 , rowspan=3, , rowspan=3, , β+ () , , rowspan=3, 3/2− , rowspan=3, , rowspan=3, , - , β+α () , Immediately decays by proton emission to for a net reaction of ↠...
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Radioligand
A radioligand is a radioactive biochemical substance (in particular, a ligand that is radiolabeled) that is used for diagnosis or for research-oriented study of the receptor systems of the body. In a neuroimaging application the radioligand is injected into the pertinent tissue, or infused into the bloodstream. It binds to its receptor. When the radioactive isotope in the ligand decays it can be measured by positron emission tomography (PET) or single-photon emission computed tomography (SPECT). In ''in vivo'' systems it is often used to quantify the binding of a test molecule to the binding site of a radioligand. The higher the affinity of the molecule the more radioligand is displaced from the binding site and the increasing radioactive decay can be measured by scintillography. This assay is commonly used to calculate the binding constant of molecules to receptors. The transport of the radioligand is described by receptor kinetics. History Radioligands are credited with maki ...
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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 Metabolism, 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. For example, 18F-FDG, -FDG is commonly used to detect cancer, Sodium fluoride#Medical imaging, NaF is widely used for detecting bone formation, and Isotopes of oxygen#Oxygen-15, oxygen-15 is sometimes used to measure blood flow. PET is a common medical imaging, imaging technique, a Scintigraphy#Process, medical scintillography technique used in nuclear medicine. A radiopharmaceutical, radiopharmaceutical — a radioisotope attached to a drug — is injected into the body as a radioactive tracer, tracer. When the radiopharmaceutical undergoes beta plus decay, a positron is ...
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Marc Laruelle
Marc or MARC may refer to: People * Marc (given name), people with the first name * Marc (surname), people with the family name Acronyms * MARC standards, a data format used for library cataloging, * MARC Train, a regional commuter rail system of the State of Maryland, serving Maryland, Washington, D.C., and eastern West Virginia * MARC (archive), a computer-related mailing list archive * M/A/R/C Research, a marketing research and consulting firm * Massachusetts Animal Rights Coalition, a non-profit, volunteer organization * Matador Automatic Radar Control, a guidance system for the Martin MGM-1 Matador cruise missile * Mid-America Regional Council, the Council of Governments and the Metropolitan Planning Organization for the bistate Kansas City region * Midwest Association for Race Cars, a former American stock car racing organization * Revolutionary Agrarian Movement of the Bolivian Peasantry (''Movimiento Agrario Revolucionario del Campesinado Boliviano''), a defunct right-w ...
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Primate
Primates are a diverse order of mammals. They are divided into the strepsirrhines, which include the lemurs, galagos, and lorisids, and the haplorhines, which include the tarsiers and the simians (monkeys and apes, the latter including humans). Primates arose 85–55 million years ago first from small terrestrial mammals, which adapted to living in the trees of tropical forests: many primate characteristics represent adaptations to life in this challenging environment, including large brains, visual acuity, color vision, a shoulder girdle allowing a large degree of movement in the shoulder joint, and dextrous hands. Primates range in size from Madame Berthe's mouse lemur, which weighs , to the eastern gorilla, weighing over . There are 376–524 species of living primates, depending on which classification is used. New primate species continue to be discovered: over 25 species were described in the 2000s, 36 in the 2010s, and three in the 2020s. Primates have large bra ...
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Beta-CIT
RTI(-''4229'')-55, also called RTI-55 or iometopane, is a phenyltropane-based psychostimulant used in scientific research and in some medical applications. This drug was first cited in 1991. RTI-55 is a non-selective dopamine reuptake inhibitor derived from methylecgonidine. However, more selective analogs are derived by conversion to "pyrrolidinoamido" RTI-229, for instance. Due to the large bulbous nature of the weakly electron withdrawing iodo halogen atom, RTI-55 is the most strongly serotonergic of the simple ''para''-substituted troparil based analogs. In rodents RTI-55 actually caused death at a dosage of 100 mg/kg, whereas RTI-51 and RTI-31 did not. Another notable observation is the strong propensity of RTI-55 to cause locomotor activity enhancements, although in an earlier study, RTI-51 was actually even stronger than RTI-55 in shifting baseline LMA. This observation serves to highlight the disparities that can arise between studies. RTI-55 is one of the most poten ...
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Iodine-123
Iodine-123 (123I) is a radioactive isotope of iodine used in nuclear medicine imaging, including single-photon emission computed tomography (SPECT) or SPECT/CT exams. The isotope's half-life is 13.2230 hours; the decay by electron capture to tellurium-123 emits gamma radiation with a predominant energy of 159 keV (this is the gamma primarily used for imaging). In medical applications, the radiation is detected by a gamma camera. The isotope is typically applied as iodide-123, the anionic form. Production Iodine-123 is produced in a cyclotron by proton irradiation of xenon in a capsule. Xenon-124 absorbs a proton and immediately loses a neutron and proton to form xenon-123, or else loses two neutrons to form caesium-123, which decays to xenon-123. The xenon-123 formed by either route then decays to iodine-123, and is trapped on the inner wall of the irradiation capsule under refrigeration, then eluted with sodium hydroxide in a halogen disproportionation reaction, similar to colle ...
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SSRI
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs increase the extracellular level of the neurotransmitter serotonin by limiting its reabsorption (reuptake) into the presynaptic cell. They have varying degrees of selectivity for the other monoamine transporters, with pure SSRIs having strong affinity for the serotonin transporter and only weak affinity for the norepinephrine and dopamine transporters. SSRIs are the most widely prescribed antidepressants in many countries. The efficacy of SSRIs in mild or moderate cases of depression has been disputed and may or may not be outweighed by side effects, especially in adolescent populations. Medical uses The main indication for SSRIs is major depressive disorder; however, they are frequently prescribed for anxiety disorders, such as social anxiety disorder, general ...
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Fluorine-18
Fluorine-18 (18F) is a fluorine radioisotope which is an important source of positrons. It has a mass of 18.0009380(6) u and its half-life is 109.771(20) minutes. It decays by positron emission 96% of the time and electron capture 4% of the time. Both modes of decay yield stable oxygen-18. Natural occurrence is a natural trace radioisotope produced by cosmic ray spallation of atmospheric argon as well as by reaction of protons with natural oxygen: 18O + p → 18F + n.18O">sup>18Oater with high energy protons (typically ~18 MeV). The fluorine produced is in the form of a water solution of 18F.html" ;"title="sup>18F">sup>18F luoride, which is then used in a rapid chemical synthesis of various radio pharmaceuticals. The organic oxygen-18 pharmaceutical molecule is not made before the production of the radiopharmaceutical, as high energy protons destroy such molecules ( radiolysis). Radiopharmaceuticals using fluorine must therefore be synthesized after the fluorine-18 has been p ...
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