Interactions of heparin with alpha-2-adrenoceptors
| Autor: | F. Lübbecke, Volker Wizemann, V. Steudle |
|---|---|
| Rok vydání: | 1988 |
| Předmět: |
Pharmacology
Agonist Cerebral Cortex medicine.medical_specialty medicine.drug_class Heparin Anticoagulant Rats Inbred Strains Biology In Vitro Techniques Receptors Adrenergic alpha Binding Competitive Clonidine Cortex (botany) Rats Membrane Endocrinology Internal medicine medicine Animals Binding site IC50 medicine.drug |
| Zdroj: | Journal of receptor research. 8(5) |
| ISSN: | 0197-5110 |
| Popis: | The interactions of the anticoagulant Heparin with the alpha-2-adrenoceptor in rat brain cortex membranes were investigated. Binding experiments with 3H-Clonidine were performed in both the absence and presence of Heparin. 1 uM Na-Heparin caused a significant decrease in the maximal number of binding sites (Bmax) from 129.4 fmol/mg protein to 93.7 fmol/mg protein with an associated decrease in affinity (KD = 0.79 pM vs. KD= 1.53 pM) of these binding sites. Addition of Na+-Heparin to 3H-Clonidine (3.1 nM) labelled membranes inhibited 50% of specific 3H-Clonidine binding (IC50) at a concentration of 0.95 uM. Based on our findings we conclude that the simultaneous long term administration of Na-Heparin and the antihypertensive agonist Clonidine should be regarded under consideration of the inhibitory effect of Na-Heparin to the alpha-2-adrenoceptors. |
| Databáze: | OpenAIRE |
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