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Effects of RP58866 on transmembrane K+ currents in mammalian ventricular myocytes.
Zhongguo Yao Li Xue Bao. 1999 Nov; 20(11):961-9.ZY

Abstract

AIM

To determine effects of RP58866 on inward rectifier K+ current (IKl), transient outward K+ current (Ito) and delayed outward rectifier K+ current (IK) in isolated cardiac myocytes.

METHODS

In isolated ventricular myocytes of guinea pig and dog, the effect of RP58866 on IKl, Ito, and IK were observed by the whole cell voltage-clamp technique.

RESULTS

RP58866 decreased IKl in a concentration-dependent manner, with an IC50 of (3.4 +/- 0.8) micromol.L-1 (n = 6) at -100 mV in guinea pig ventricular cells. In dog ventricular myocytes, RP58866 inhibited Ito with IC50 of (2.3 +/- 0.5) micromol.L-1 at +40 mV. In guinea pig ventricular cells, RP58866 at 100 micromol.L-1 decreased IK: IKstep by (58 +/- 13)% at +40 mV, and IKtail by (86 +/- 17)%, respectively. RP58866 inhibited IKstep with an IC50 of (7.5 +/- 0.8) micromol.L-1, and IKtail with an IC50 of (3.5 +/- 0.9) micromol.L-1. The envelope of tail analysis suggested that both IKr and IKs were inhibited.

CONCLUSION

RP58866 inhibits IKl, Ito, and IK in cardiac myocytes with a similar potency, and is not a specific IKl inhibitor.

Authors+Show Affiliations

Department of Pharmacology, Harbin Medical University, Harbin 150086, China. Yangbf@ems.hrbmu.edu.cnNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

11270975

Citation

Yang, B F., et al. "Effects of RP58866 On Transmembrane K+ Currents in Mammalian Ventricular Myocytes." Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, vol. 20, no. 11, 1999, pp. 961-9.
Yang BF, Li GR, Xu CQ, et al. Effects of RP58866 on transmembrane K+ currents in mammalian ventricular myocytes. Zhongguo Yao Li Xue Bao. 1999;20(11):961-9.
Yang, B. F., Li, G. R., Xu, C. Q., & Nattel, S. (1999). Effects of RP58866 on transmembrane K+ currents in mammalian ventricular myocytes. Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, 20(11), 961-9.
Yang BF, et al. Effects of RP58866 On Transmembrane K+ Currents in Mammalian Ventricular Myocytes. Zhongguo Yao Li Xue Bao. 1999;20(11):961-9. PubMed PMID: 11270975.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of RP58866 on transmembrane K+ currents in mammalian ventricular myocytes. AU - Yang,B F, AU - Li,G R, AU - Xu,C Q, AU - Nattel,S, PY - 2001/3/29/pubmed PY - 2001/4/3/medline PY - 2001/3/29/entrez SP - 961 EP - 9 JF - Zhongguo yao li xue bao = Acta pharmacologica Sinica JO - Zhongguo Yao Li Xue Bao VL - 20 IS - 11 N2 - AIM: To determine effects of RP58866 on inward rectifier K+ current (IKl), transient outward K+ current (Ito) and delayed outward rectifier K+ current (IK) in isolated cardiac myocytes. METHODS: In isolated ventricular myocytes of guinea pig and dog, the effect of RP58866 on IKl, Ito, and IK were observed by the whole cell voltage-clamp technique. RESULTS: RP58866 decreased IKl in a concentration-dependent manner, with an IC50 of (3.4 +/- 0.8) micromol.L-1 (n = 6) at -100 mV in guinea pig ventricular cells. In dog ventricular myocytes, RP58866 inhibited Ito with IC50 of (2.3 +/- 0.5) micromol.L-1 at +40 mV. In guinea pig ventricular cells, RP58866 at 100 micromol.L-1 decreased IK: IKstep by (58 +/- 13)% at +40 mV, and IKtail by (86 +/- 17)%, respectively. RP58866 inhibited IKstep with an IC50 of (7.5 +/- 0.8) micromol.L-1, and IKtail with an IC50 of (3.5 +/- 0.9) micromol.L-1. The envelope of tail analysis suggested that both IKr and IKs were inhibited. CONCLUSION: RP58866 inhibits IKl, Ito, and IK in cardiac myocytes with a similar potency, and is not a specific IKl inhibitor. SN - 0253-9756 UR - https://www.unboundmedicine.com/medline/citation/11270975/Effects_of_RP58866_on_transmembrane_K+_currents_in_mammalian_ventricular_myocytes_ L2 - http://www.chinaphar.com/1671-4083/20/961.pdf DB - PRIME DP - Unbound Medicine ER -