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[Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig].
Zhonghua Yi Xue Za Zhi. 2002 Jan 10; 82(1):57-60.ZY

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.

Authors+Show Affiliations

Li C
People's Hospital of Peking University, Beijing 100044, China.
Guo J
No affiliation info available
Liu T
No affiliation info available

MeSH

AnimalsBerberineCalcium Channel BlockersCalcium Channels, L-TypeGuinea PigsHeart VentriclesMyocardiumPatch-Clamp Techniques

Pub Type(s)

English Abstract
Journal Article

Language

chi

PubMed ID

11953130

Citation

Li, Chun, et al. "[Inhibitory Action of CPU86035 On L-type Calcium Current in Single Ventricular Myocyte of Guinea Pig]." Zhonghua Yi Xue Za Zhi, vol. 82, no. 1, 2002, pp. 57-60.
Li C, Guo J, Liu T. [Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig]. Zhonghua Yi Xue Za Zhi. 2002;82(1):57-60.
Li, C., Guo, J., & Liu, T. (2002). [Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig]. Zhonghua Yi Xue Za Zhi, 82(1), 57-60.
Li C, Guo J, Liu T. [Inhibitory Action of CPU86035 On L-type Calcium Current in Single Ventricular Myocyte of Guinea Pig]. Zhonghua Yi Xue Za Zhi. 2002 Jan 10;82(1):57-60. PubMed PMID: 11953130.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Inhibitory action of CPU86035 on L-type calcium current in single ventricular myocyte of guinea pig]. AU - Li,Chun, AU - Guo,Jihong, AU - Liu,Taifeng, PY - 2002/4/16/pubmed PY - 2002/5/15/medline PY - 2002/4/16/entrez SP - 57 EP - 60 JF - Zhonghua yi xue za zhi JO - Zhonghua Yi Xue Za Zhi VL - 82 IS - 1 N2 - 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. SN - 0376-2491 UR - https://www.unboundmedicine.com/medline/citation/11953130/[Inhibitory_action_of_CPU86035_on_L_type_calcium_current_in_single_ventricular_myocyte_of_guinea_pig]_ DB - PRIME DP - Unbound Medicine ER -