Document Detail

Effects of AMP579 and adenosine on L-type Ca2+ current in isolated rat ventricular myocytes.
MedLine Citation:
PMID:  15842773     Owner:  NLM     Status:  MEDLINE    
AIM: To compare the effects of AMP579 and adenosine on L-type Ca2+ current (I(Ca-L)) in rat ventricular myocytes and explore the mechanism by which AMP579 acts on I(Ca-L). METHODS: I(Ca-L) was recorded by patch-clamp technique in whole-cell configuration. RESULTS: Adenosine (10 nmol/L to 50 micromol/L) showed no effect on basal I(Ca-L), but it inhibited the I(Ca-L) induced by isoproterenol 10 nmol/L in a concentration-dependent manner with the IC(50) of 13.06 micromol/L. Similar to adenosine, AMP579 also showed an inhibitory effect on the I(Ca-L) induced by isoproterenol. AMP579 and adenosine (both in 10 micromol/L) suppressed isoproterenol-induced ICa-L by 11.1% and 5.2%, respectively. In addition, AMP579 had a direct inhibitory effect on basal I(Ca-L) in a concentration-dependent manner with IC50 (1.17 micromol/L). PD116948 (30 micromol/L), an adenosine A1 receptor blocker, showed no action on the inhibitory effect of AMP579 on basal I(Ca-L). However, GF109203X (0.4 micromol/L), a special protein kinase C (PKC) blocker, could abolish the inhibitory effect of AMP579 on basal I(Ca-L). So the inhibitory effect of AMP579 on basal I(Ca-L) was induced through activating PKC, but not linked to adenosine A1 receptor. CONCLUSION: AMP579 shows a stronger inhibitory effect than adenosine on the I(Ca-L) induced by isoproterenol. AMP579 also has a strong inhibitory effect on basal I(Ca-L) in rat ventricular myocytes. Activation of PKC is involved in the inhibitory effect of AMP579 on basal I(Ca-L) at downstream-mechanism.
Xiong Wang; Bo-wei Wu; Dong-mei Wu
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Acta pharmacologica Sinica     Volume:  26     ISSN:  1671-4083     ISO Abbreviation:  Acta Pharmacol. Sin.     Publication Date:  2005 May 
Date Detail:
Created Date:  2005-04-21     Completed Date:  2005-10-26     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  100956087     Medline TA:  Acta Pharmacol Sin     Country:  China    
Other Details:
Languages:  eng     Pagination:  559-62     Citation Subset:  IM    
Department of Physiology, Shanxi Medical University, Taiyuan 030001, China.
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MeSH Terms
Adenosine / pharmacology*
Calcium Channels, L-Type / drug effects*,  metabolism
Cardiotonic Agents / pharmacology*
Cell Separation
Dose-Response Relationship, Drug
Heart Ventricles / cytology
Imidazoles / pharmacology*
Indoles / pharmacology
Maleimides / pharmacology
Myocytes, Cardiac / drug effects*
Protein Kinase C / antagonists & inhibitors
Pyridines / pharmacology*
Rats, Wistar
Receptor, Adenosine A1 / antagonists & inhibitors
Xanthines / pharmacology
Reg. No./Substance:
0/4-(7-((2-3-chloro-2-thienyl)-1-methyl-propylamino)-3H-imidazo(4,5-b)pyridyl-3-yl)cyclopentane carboxamide; 0/Calcium Channels, L-Type; 0/Cardiotonic Agents; 0/Imidazoles; 0/Indoles; 0/Maleimides; 0/Pyridines; 0/Receptor, Adenosine A1; 0/Xanthines; 102146-07-6/1,3-dipropyl-8-cyclopentylxanthine; 133052-90-1/bisindolylmaleimide I; 58-61-7/Adenosine; EC Kinase C

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