Tyrosine kinase inhibitors suppress alpha1-adrenoceptor mediated contraction in human radial, internal mammary arteries and saphenous vein.
The aim of this study is to determine whether the tyrosine kinase plays a role in the contractile response of human radial artery (RA), internal mammary artery (IMA) and saphenous vein (SV) to alpha(1)-adrenoceptor (AR) stimulation. The tyrosine kinase inhibitors, genistein and tyrphostin, significantly inhibited alpha(1)-AR mediated contractile response in a dose-dependent and non-competitive manner. Genistein at 10 microM inhibited 39%, 54% and 72% of PE-induced maximum contraction, and tyrphostin at 50 microM inhibited 41%, 68% and 39% of the contraction in the human RA, IMA and SV respectively. These results suggest that tyrosine kinases participate in regulation of signal transduction that is associated with alpha(1)-AR mediated contractile response in human blood vessels.
Yan
Ming
M
Cardiac Research Laboratory, National Heart Centre of Singapore, Singapore 168752. ming.yan@med.monash.edu.au
Liu
Dong Ling
DL
Chua
Yeow Leng
YL
Chen
Chen
C
Lim
Yean Leng
YL
D058668:Adrenergic alpha-1 Receptor Antagonists; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D019833:Genistein / Q000494:pharmacology; D006801:Humans; D008323:Mammary Arteries / Q000187:drug effects* / Q000502:physiology; D009119:Muscle Contraction / Q000187:drug effects* / Q000502:physiology; D010656:Phenylephrine / Q000494:pharmacology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D017534:Radial Artery / Q000187:drug effects* / Q000502:physiology; D012501:Saphenous Vein / Q000187:drug effects* / Q000502:physiology; D015398:Signal Transduction; D020032:Tyrphostins / Q000494:pharmacology
D058668:Adrenergic alpha-1 Receptor Antagonists; D000316:Adrenergic alpha-Agonists; D004791:Enzyme Inhibitors; D020032:Tyrphostins; D010656:Phenylephrine; D019833:Genistein; D011505:Protein-Tyrosine Kinases