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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Armstrong, R. A. Humphrey, P. P. Lumley, P. |
| Description | Author Affiliation: Armstrong RA ( Department of Pharmacology, University of Edinburgh Medical School.) |
| Abstract | 1. Exposure of human resuspended platelets in vitro for 30 min to the potent thromboxane A2 (TP)-receptor blocking drug GR32191, followed by its removal by dilution-dissociation, reduced the degree of subsequent binding to 2 nM [3H]-GR32191 by almost 50%. Exposure for longer periods (60 min) led to a further reduction. However, no change in the Kd of the radioligand was observed. 2. This effect of GR32191 could not be explained by persistent binding of drug to platelets since a dilution-dissociation stage, designed to remove all drug, was included prior to measurement of binding. 3. Using an alternative TP-receptor radioligand, [3H]-SQ29,548, to monitor receptor number, a reduction in Bmax was observed after GR32191 pre-treatment; the Kd value of the radioligand remained unchanged. 4. The effect was not a common property of TP-receptor blocking drugs since pre-exposure of platelets in vitro for 30 min to BM13.177 or SQ29,548 did not produce a fall in subsequent Bmax to [3H]-SQ29,548. 5. While the mechanism behind this apparent down-regulation of platelet TP-receptor is unknown, it may explain the long duration of action of GR32191 upon platelets in man which persists in the absence of detectable drug in the plasma. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 2 |
| Volume Number | 110 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1993-10-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Biphenyl Compounds Pharmacology Blood Platelets Metabolism Heptanoic Acids Receptors, Thromboxane Drug Effects Binding, Competitive Pharmacokinetics Down-Regulation Hydrazines In Vitro Techniques Ligands Platelet Aggregation Inhibitors Radioligand Assay Antagonists & Inhibitors Sulfonamides |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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