| pubmed-article:8535333 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C0035647 | lld:lifeskim |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C0205145 | lld:lifeskim |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C0026454 | lld:lifeskim |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C0030557 | lld:lifeskim |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C0040399 | lld:lifeskim |
| pubmed-article:8535333 | lifeskim:mentions | umls-concept:C1522485 | lld:lifeskim |
| pubmed-article:8535333 | pubmed:issue | 6 | lld:pubmed |
| pubmed-article:8535333 | pubmed:dateCreated | 1996-2-8 | lld:pubmed |
| pubmed-article:8535333 | pubmed:abstractText | Monoamine oxidases are important in the regulation of monoaminergic neurotransmission. An increase in monoamine oxidase B (MAO B) has been observed in some neurodegenerative diseases, and therefore quantification of cerebral MAO B activity by SPECT would be useful for the diagnosis and therapeutic follow-up of these disorders. We have developed an iodinated derivative of pargyline, a selective inhibitor of MAO B, in order to explore this enzyme by SPECT. Stable bromo and iodo derivatives of pargyline were synthesized and chemically characterized. The radioiodinated ligand [125I]-2-iodopargyline was obtained with high specific activity from the bromo precursor by nucleophilic exchange. Affinity and selectivity of 2-iodopargyline were tested in vitro. Biodistribution study of [125I]-2-iodopargyline was performed in rats. Radioiodinated ligand were obtained in a no-carrier-added form. 2-iodopargyline has a higher in vitro affinity for MAO B than pargyline. However, the in vitro selectivity for MAO B was better for pargyline than for 2-iodopargyline. Ex vivo autoradiographic studies and in vivo saturation studies with selective inhibitors of MAO showed that the cerebral biodistribution of [125I]-2-iodopargyline in the rat is consistent with high level binding to MAO B sites in the pineal gland and in the thalamus. In conclusion, 2-iodopargyline preferentially binds in vivo to MAO B sites with high affinity. However, its selectivity for MAO B in rats is not very high, whereas this ligand binds to a lesser extent to MAO A. It will be then of great value to evaluate the specificity of 2-iodopargyline in humans. This new ligand labeled with 123I should therefore be a suitable tool for SPECT exploration of MAO B in the human brain. | lld:pubmed |
| pubmed-article:8535333 | pubmed:language | eng | lld:pubmed |
| pubmed-article:8535333 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8535333 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:8535333 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8535333 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8535333 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8535333 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8535333 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:8535333 | pubmed:issn | 0969-8051 | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:BesnardJ CJC | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:HánaII | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:BaulieuJ LJL | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:ChalonSS | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:GuilloteauDD | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:GarreauLL | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:FranginYY | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:OmbettaJ EJE | lld:pubmed |
| pubmed-article:8535333 | pubmed:author | pubmed-author:DognonA MAM | lld:pubmed |
| pubmed-article:8535333 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8535333 | pubmed:volume | 22 | lld:pubmed |
| pubmed-article:8535333 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8535333 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8535333 | pubmed:pagination | 727-36 | lld:pubmed |
| pubmed-article:8535333 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:8535333 | pubmed:meshHeading | pubmed-meshheading:8535333-... | lld:pubmed |
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| pubmed-article:8535333 | pubmed:meshHeading | pubmed-meshheading:8535333-... | lld:pubmed |
| pubmed-article:8535333 | pubmed:year | 1995 | lld:pubmed |
| pubmed-article:8535333 | pubmed:articleTitle | Iododerivative of pargyline: a potential tracer for the exploration of monoamine oxidase sites by SPECT. | lld:pubmed |
| pubmed-article:8535333 | pubmed:affiliation | Laboratoire de Biophysique Médicale et Pharmaceutique, INSERM U316, Tours-France. | lld:pubmed |
| pubmed-article:8535333 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:8535333 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:8535333 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
