These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


PUBMED FOR HANDHELDS

Search MEDLINE/PubMed


  • Title: [Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig].
    Author: Li C, Guo J, Liu T.
    Journal: Zhonghua Yi Xue Za Zhi; 2002 Jan 10; 82(1):57-60. PubMed ID: 11953130.
    Abstract:
    OBJECTIVE: To investigate the effects of CPU86035, a recently synthesized tetrahydroberberine derivative, on the L-type calcium currents (I(Ca.L)) in single guinea pig ventricular myocytes. METHODS: The effect of CPU86035 of different concentrations (50 approximately 250 micromomol/L) on I(Ca.L) in enzymatically dispersed single guinea pig ventricular myocytes was investigated by using whole-cell patch-clamp technique. RESULTS: (1) CPU86035 concentration-dependently inhibited I(Ca.L), with the IC50 at 75 micromol/L. (2) The inhibition of CPU86035 on I(Ca.L) was dependent on the holding potential (HP). 75 micromol/L CPU86035 inhibited I(Ca.L) by 49% +/- 2% at HP = -40 mV, and 64% +/- 4% at HP = -80 mV. (3) The homeostatic activation curve of ICa.L shifted to the right toward more positive potentials in the presence of CPU86035, with a V(1/2) of 15.4 mV +/- 0.8 mV compared with that of 15.4 +/- 0.8 mV in the control. (4) The homeostatic inactivation curve of I(Ca.L) shifted to the right toward more positive potentials in the presence of CPU86035, with a V(1/2) of -12.6 mV +/- 2.7 mV compared with that of -19.1 mV +/- 2.5 mV in the control. (5) The recovery from inactivation became slower in the presence of CPU86035. CONCLUSION: CPU86035 strongly inhibits the calcium channel, probably by binding to the channel in resting stage.
    [Abstract] [Full Text] [Related] [New Search]