11C-harmine as a tracer for monoamine oxidase A (MAO-A): in vitro and in vivo studies. 1997

M Bergström, and G Westerberg, and B Långström
Subfemtomole Biorecognition Project, Uppsala University, Sweden.

Frozen-section autoradiography in rat brain sections as well as in vivo positron emission tomography (PET) studies in monkey brain were used for the determination of binding characteristics of O-[methyl-11C]harmine in an attempt to validate this ligand for the assessment of monoamine oxidase A (MAO-A). In frozen sections, the binding of [11C]harmine showed an apparent KD of the binding of 2 nM. The specific binding was inhibited by nanomolar concentrations of clorgyline, esuprone, brofaromine, and Ro 41-1049. The in vivo kinetic pattern in the monkey brain indicated a significant trapping, which was inhibited by pretreatment with clorgyline, moclobemide, or harmine. Different approaches for a quantitative determination of MAO-A enzyme binding were attempted and demonstrated an IC50 dose of harmine in the range of 0.05-0.1 mg/kg. The studies give strong indications for the validity of [11C]harmine as an in vivo tracer for the assessment of MAO-A enzyme binding in the brain.

UI MeSH Term Description Entries
D008253 Macaca mulatta A species of the genus MACACA inhabiting India, China, and other parts of Asia. The species is used extensively in biomedical research and adapts very well to living with humans. Chinese Rhesus Macaques,Macaca mulatta lasiota,Monkey, Rhesus,Rhesus Monkey,Rhesus Macaque,Chinese Rhesus Macaque,Macaca mulatta lasiotas,Macaque, Rhesus,Rhesus Macaque, Chinese,Rhesus Macaques,Rhesus Macaques, Chinese,Rhesus Monkeys
D008297 Male Males
D008995 Monoamine Oxidase An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4. Amine Oxidase (Flavin-Containing),MAO,MAO-A,MAO-B,Monoamine Oxidase A,Monoamine Oxidase B,Type A Monoamine Oxidase,Type B Monoamine Oxidase,Tyramine Oxidase,MAO A,MAO B,Oxidase, Monoamine,Oxidase, Tyramine
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D006247 Harmine Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's. 9H-Pyrido(3,4-b)indole, 7-methoxy-1-methyl-,Banisterine,Leucoharmine,Telepathine,Yageine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001345 Autoradiography The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed) Radioautography
D014055 Tomography, Emission-Computed Tomography using radioactive emissions from injected RADIONUCLIDES and computer ALGORITHMS to reconstruct an image. CAT Scan, Radionuclide,CT Scan, Radionuclide,Computerized Emission Tomography,Radionuclide Tomography, Computed,Scintigraphy, Computed Tomographic,Tomography, Radionuclide-Computed,Computed Tomographic Scintigraphy,Emission-Computed Tomography,Radionuclide Computer-Assisted Tomography,Radionuclide Computerized Tomography,Radionuclide-Computed Tomography,Radionuclide-Emission Computed Tomography,Tomography, Computerized Emission,CAT Scans, Radionuclide,CT Scans, Radionuclide,Computed Radionuclide Tomography,Computed Tomography, Radionuclide-Emission,Computer-Assisted Tomographies, Radionuclide,Computer-Assisted Tomography, Radionuclide,Computerized Tomography, Radionuclide,Emission Computed Tomography,Emission Tomography, Computerized,Radionuclide CAT Scan,Radionuclide CAT Scans,Radionuclide CT Scan,Radionuclide CT Scans,Radionuclide Computed Tomography,Radionuclide Computer Assisted Tomography,Radionuclide Computer-Assisted Tomographies,Radionuclide Emission Computed Tomography,Scan, Radionuclide CAT,Scan, Radionuclide CT,Scans, Radionuclide CAT,Scans, Radionuclide CT,Tomographic Scintigraphy, Computed,Tomographies, Radionuclide Computer-Assisted,Tomography, Computed Radionuclide,Tomography, Emission Computed,Tomography, Radionuclide Computed,Tomography, Radionuclide Computer-Assisted,Tomography, Radionuclide Computerized,Tomography, Radionuclide-Emission Computed
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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