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[Effect of KB-R7943 on Na(+)-Ca2+ exchange current in guinea pig ventricular myocytes].
Yao Xue Xue Bao. 2001 Jan; 36(1):25-8.YX

Abstract

AIM

To study whether KB-R7943 has selective inhibitory effect on the inward and outward Na(+)-Ca2+ exchange current (INa-Ca) in guinea pig ventricular myocytes.

METHODS

Through setting up the model of intracellular Na(+)-overload during myocardial ischemia and reperfusion, the current-voltage relationship of INa-Ca was recorded using whole-cell patch clamp technique under bi-directional ionic conditions.

RESULTS

Currents were elicited by a declining ramp pulse depolarized immediately from holding potential of -40 mV to +60 mV, then repolarized to -100 mV at a speed of 80 mV.s-1 and returned to the holding potential under bi-directional ionic conditions, while the [Na+] was 25 mmol.L-1 in the pipette solution. The currents increased time-dependently and voltage-dependently which reached from (2.51 +/- 0.15) pA.pF-1 to (5.94 +/- 0.13) pA.pF-1 at mV and from (-1.92 +/- 0.13) pA.pF-1 to (-3.17 +/- 0.16) pA.pF-1 at -80 mV (n = 12) after 3 min and there is no significant run-down of the current. KB-R7943 10(-6) mol.L-1 was found to decrease the current to (4.62 +/- 0.05) pA.pF-1 by 29.4% at mV and to (-2.30 +/- 0.18) pA.pF-1 by 22.1% at -80 mV (n = 5) after 5 min. While 10(-5) mol.L-1 KB-R7943 was shown to decrease the current to (3.13 +/- 0.03) pA.pF-1 by 61.7% at mV and to (-1.62 +/- 0.03) pA.pF-1 by 56.9% at -80 mV (n = 7).

CONCLUSION

KB-R7943 can block INa-Ca in guinea pig ventricular myocytes. But, it did not show selective inhibition effect on inward and outward currents.

Authors+Show Affiliations

Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.No affiliation info availableNo affiliation info available

Pub Type(s)

English Abstract
Journal Article
Research Support, Non-U.S. Gov't

Language

chi

PubMed ID

12579855

Citation

Lu, J, et al. "[Effect of KB-R7943 On Na(+)-Ca2+ Exchange Current in Guinea Pig Ventricular Myocytes]." Yao Xue Xue Bao = Acta Pharmaceutica Sinica, vol. 36, no. 1, 2001, pp. 25-8.
Lu J, Xu XH, Wang XL. [Effect of KB-R7943 on Na(+)-Ca2+ exchange current in guinea pig ventricular myocytes]. Yao Xue Xue Bao. 2001;36(1):25-8.
Lu, J., Xu, X. H., & Wang, X. L. (2001). [Effect of KB-R7943 on Na(+)-Ca2+ exchange current in guinea pig ventricular myocytes]. Yao Xue Xue Bao = Acta Pharmaceutica Sinica, 36(1), 25-8.
Lu J, Xu XH, Wang XL. [Effect of KB-R7943 On Na(+)-Ca2+ Exchange Current in Guinea Pig Ventricular Myocytes]. Yao Xue Xue Bao. 2001;36(1):25-8. PubMed PMID: 12579855.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Effect of KB-R7943 on Na(+)-Ca2+ exchange current in guinea pig ventricular myocytes]. AU - Lu,J, AU - Xu,X H, AU - Wang,X L, PY - 2003/2/13/pubmed PY - 2003/8/9/medline PY - 2003/2/13/entrez SP - 25 EP - 8 JF - Yao xue xue bao = Acta pharmaceutica Sinica JO - Yao Xue Xue Bao VL - 36 IS - 1 N2 - AIM: To study whether KB-R7943 has selective inhibitory effect on the inward and outward Na(+)-Ca2+ exchange current (INa-Ca) in guinea pig ventricular myocytes. METHODS: Through setting up the model of intracellular Na(+)-overload during myocardial ischemia and reperfusion, the current-voltage relationship of INa-Ca was recorded using whole-cell patch clamp technique under bi-directional ionic conditions. RESULTS: Currents were elicited by a declining ramp pulse depolarized immediately from holding potential of -40 mV to +60 mV, then repolarized to -100 mV at a speed of 80 mV.s-1 and returned to the holding potential under bi-directional ionic conditions, while the [Na+] was 25 mmol.L-1 in the pipette solution. The currents increased time-dependently and voltage-dependently which reached from (2.51 +/- 0.15) pA.pF-1 to (5.94 +/- 0.13) pA.pF-1 at mV and from (-1.92 +/- 0.13) pA.pF-1 to (-3.17 +/- 0.16) pA.pF-1 at -80 mV (n = 12) after 3 min and there is no significant run-down of the current. KB-R7943 10(-6) mol.L-1 was found to decrease the current to (4.62 +/- 0.05) pA.pF-1 by 29.4% at mV and to (-2.30 +/- 0.18) pA.pF-1 by 22.1% at -80 mV (n = 5) after 5 min. While 10(-5) mol.L-1 KB-R7943 was shown to decrease the current to (3.13 +/- 0.03) pA.pF-1 by 61.7% at mV and to (-1.62 +/- 0.03) pA.pF-1 by 56.9% at -80 mV (n = 7). CONCLUSION: KB-R7943 can block INa-Ca in guinea pig ventricular myocytes. But, it did not show selective inhibition effect on inward and outward currents. SN - 0513-4870 UR - https://www.unboundmedicine.com/medline/citation/12579855/[Effect_of_KB_R7943_on_Na_+__Ca2+_exchange_current_in_guinea_pig_ventricular_myocytes]_ DB - PRIME DP - Unbound Medicine ER -