Heterogeneous mechanisms of endothelium-dependent relaxation for thrombin and peptide activators of protease-activated receptor-1 in porcine isolated coronary artery
| Autor: | Justin Raymond Hamilton, Thomas M. Cocks |
|---|---|
| Rok vydání: | 2000 |
| Předmět: |
Pharmacology
chemistry.chemical_classification medicine.medical_specialty Endothelium-derived hyperpolarizing factor Chemistry Calcium channel chemistry.chemical_element Peptide Calcium Trypsin Molecular biology Thrombin Endocrinology Nifedipine Internal medicine cardiovascular system medicine Verapamil medicine.drug |
| Zdroj: | British Journal of Pharmacology. 130:181-188 |
| ISSN: | 0007-1188 |
| DOI: | 10.1038/sj.bjp.0703146 |
| Popis: | 1. Mechanisms of protease-activated receptor-1 (PAR1)- and PAR2-induced relaxation were investigated in pre-contracted porcine coronary artery ring preparations. 2. Thrombin (0.01 - 0.3 u ml(-1)) and the PAR1-activating peptide SFLLRN (0.1 - 10 microM) caused concentration- and endothelium-dependent relaxation. pEC(50)s (-log u ml(-1) for enzymes, -log M for peptides) and maximum relaxations (R(max), %) for thrombin were 1.8+/-0.1 and 93.5+/-2.8% respectively, and for SFLLRN 6.8+/-0.1 and 90.8+/-1.3%. Similar concentration- and endothelium-dependent relaxations occurred with trypsin (pEC(50) 2.3+/-0.2; R(max) 94.1+/-1.9%) and the PAR2-activating peptide SLIGRL (pEC(50) 6.5+/-0.2; R(max) 92.4+/-1.6%). 3. Relaxations to thrombin, SFLLRN, trypsin and SLIGRL were significantly inhibited (P |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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