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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Keppens, S. De Wulf, H. |
| Description | Author Affiliation: Keppens S ( Afdeling Biochemie, Fakulteit Geneeskunde, Katholieke Universiteit Leuven, Belgium.) |
| Abstract | 1. In several tissues, 2-methylthio adenosine triphosphate (2MeSATP) is a very potent P2y-purine agonist. In rat hepatocytes, 2MeSATP half-maximally activated glycogen phosphorylase at 20 nM and was therefore about 25 times more effective than ATP (Ka 0.5-0.8 microM). This strong glycogenolytic potency of 2MeSATP suggests on its own the presence of P2Y-purinoceptors in liver. 2. Displacement of the radioligand ATP alpha[35S] from its receptor however occurred at much higher concentrations of 2MeSATP than was anticipated on the basis of its glycogenolytic potency. 3. The interaction of 2MeSATP with the receptor, characterized with ATP alpha[35S] as radioligand, cannot be considered as a pure competitive interaction. 4. 2MeSATP did not share the ability of ATP to counteract the effect of glucagon on the adenosine 3':5'-cyclic monophosphate levels. 5. 2MeSATP barely increased the levels of inositol trisphosphate (IP3). 6. The glycogenolytic effect of 2MeSATP was completely abolished by pretreatment of the hepatocytes with phorbol myristic acetate. 7. It is tentatively concluded that 2MeSATP and ATP are interacting with different P2 purinoceptors. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 2 |
| Volume Number | 104 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1991-10-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Adenosine Triphosphate Analogs & Derivatives Pharmacology Liver Drug Effects Thionucleotides Animals Cells, Cultured Enzyme Activation Chemistry Cytology Phosphorylases Radioligand Assay Rats, Inbred Strains Receptors, Purinergic Comparative Study Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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