Stereoselectivity in the metabolism of 3H-noradrenaline during uptake into and efflux from the isolated rat vas deferens
| Autor: | K. H. Graefe, Salomon Z. Langer, F. J. E. Stefano |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Male
Phenoxybenzamine Monoamine oxidase Stereochemistry Metabolite In Vitro Techniques Norepinephrine chemistry.chemical_compound Vas Deferens Cocaine medicine Animals Neurons Pharmacology Catabolism Stereoisomerism General Medicine Metabolism Rats Biochemistry chemistry Amine gas treating Stereoselectivity Efflux Corticosterone Half-Life medicine.drug |
| Zdroj: | Naunyn-Schmiedeberg's Archives of Pharmacology. 299:225-238 |
| ISSN: | 1432-1912 0028-1298 |
| DOI: | 10.1007/bf00500315 |
| Popis: | 1. The metabolism of 3H-(-)- and 3H-(±)-noradrenaline (NA) was studied in the isolated rat vas deferens either under conditions of uptake or of efflux of the amine. Any differences obtained between 3H-(-)-and 3H-(±)NA as substrate were interpreted as being a reflection of differences between the two isomers of the amine. 2. Uptake experiments (0.13 μM; 7.5 min) showed that neuronal mechanisms of amine disposition prevail over extraneuronal ones. Thus, most of the metabolites of 3H-NA formed during incubation with the amine (including the O-methylated products) were of neuronal origin. The acid deaminated metabolite 3,4-dihydroxymandelic acid (DOMA), tended to be much better retained by the tissue than the neutral deaminated metabolite, 3,4-dihydroxyphenylethyleneglycol (DOPEG). While neuronal uptake exhibited no stereoselectivity, a pronounced stereoselectivity was found for monoamine oxidase (MAO) [(-)NA> (+)NA] as well as for the enzymes which are in series with MAO, namely, aldehyde reductase and aldehyde dehydrogenase [(-)DOPEG> (+)DOPEG; (-)DOMA |
| Databáze: | OpenAIRE |
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