Effects of (8beta)-8-[methylthio)methyl]-6-propylergoline on dopaminergic function and brain dopamine turnover in rats
| Autor: | Bach Nicholas J, E. Barry Smalstig, James A. Clemens, Kornfeld Edmund C, Ray W. Fuller, Harold D. Snoddy |
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| Rok vydání: | 1979 |
| Předmět: |
Agonist
Male medicine.medical_specialty Reserpine Time Factors medicine.drug_class Metabolite Dopamine General Biochemistry Genetics and Molecular Biology Receptors Dopamine chemistry.chemical_compound Hydroxydopamines In vivo Internal medicine medicine Animals Humans General Pharmacology Toxicology and Pharmaceutics Ergolines Receptor Brain Chemistry Dopaminergic Brain General Medicine Ergoline Rats Endocrinology chemistry Dopamine receptor 3 4-Dihydroxyphenylacetic Acid Stereotyped Behavior medicine.drug |
| Zdroj: | Life sciences. 24(4) |
| ISSN: | 0024-3205 |
| Popis: | (8β)-8-[(Methylthio)methyl]-6-propylergoline induced contralateral turning in rats with nigrostriatal lesions, lowered serum prolactin in reserpinized rats, and caused stereotyped hyperactivity. In addition to these functional effects typical of dopaminergic agonists, (8β)-8-[(methylthio)methyl]-6-propylergoline decreased dopamine turnover in rat brain. Decreased turnover was indicated by a diminished depletion of dopamine content after inhibition of its synthesis by α-methyltyrosine and by a decreased steady state concentration of the dopamine metabolite, 3, 4-dihydroxyphenylacetic acid (DOPAC). DOPAC concentration in whole brain was decreased after doses of (8β)-8-[(methylthio)methyl]-6-propylergoline as low as 0.003 mg/kg, and the lowering of DOPAC persisted for up to 16 hrs. after a 0.3 mg/kg dose. (8β)-8-[(Methylthio)-methyl]-6-propylergoline had less effect than a structurally-related compound, lergotrile, on 3-methoxy-4-hydroxy-phenyl-ethyleneglycol sulfate levels in whole brain and did not affect 5-hydroxy-indoleacetic acid levels over a dose range from .01–10 mg/kg. The behavioral and neuroendocrine effects of this new ergoline compound and its reduction of dopamine turnover in rat brain indicate that it is a potent dopamine receptor agonist in vivo . |
| Databáze: | OpenAIRE |
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