Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017

De Zai Dai, Huijuan Hu, Jing Zhao, Xue Mei Hao, Dong Mei Yang, Pei Ai Zhou, Cai Hong Wu

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

AIM: To assess the blockade by CPU 86017 on the L-type calcium channels in the myocardium and on the Ca2+-related contractions of vascular smooth muscle. METHODS: The whole-cell patch-clamp was applied to investigate the blocking effect of CPU 86017 on the L-type calcium current in isolated guinea pig myocytes and contractions by KCl or phenylephrine (Phe) of the isolated rat tail arteries were measured. RESULTS: Suppression of the L-type current of the isolated myocytes by CPU 86017 was moderate, in time- and concentration-dependent manner and with no influence on the activation and inactivation curves. The IC50 was 11.5 μmol/L. Suppressive effect of CPU 86017 on vaso-contractions induced by KCl 100 mmol/L, phenylephrine 1 μmol/L in KH solution (phase 1), Ca2+ free KH solution (phase 2), and by addition of CaCl2 into Ca2+-free KH solution (phase 3) were observed. The IC50 to suppress vaso-contractions by calcium entry via the receptor operated channel (ROC) and voltage-dependent channel (VDC) was 0.324 μmol/L and 16.3 μmol/L, respectively. The relative potency of CPU 86017 to suppress vascular tone by Ca2+ entry through ROC and VDC is 1/187 of prazosin and 1/37 of verapamil, respectively. CONCLUSION: The blocking effects of CPU 86017 on the L-type calcium channel of myocardium and vessel are moderate and non-selective. CPU 86017 is approximately 50 times more potent in inhibiting ROC than VDC.

Original languageEnglish (US)
Pages (from-to)416-423
Number of pages8
JournalActa Pharmacologica Sinica
Volume25
Issue number4
StatePublished - Apr 1 2004
Externally publishedYes

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L-Type Calcium Channels
Vascular Smooth Muscle
Myocardium
Calcium
Phenylephrine
Muscle Cells
Inhibitory Concentration 50
Prazosin
Verapamil
4-chlorobenzyltetrahydroberberine
Blood Vessels
Tail
Guinea Pigs
Arteries

All Science Journal Classification (ASJC) codes

  • Pharmacology (medical)
  • Pharmacology

Cite this

Dai, De Zai ; Hu, Huijuan ; Zhao, Jing ; Hao, Xue Mei ; Yang, Dong Mei ; Zhou, Pei Ai ; Wu, Cai Hong. / Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017. In: Acta Pharmacologica Sinica. 2004 ; Vol. 25, No. 4. pp. 416-423.
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abstract = "AIM: To assess the blockade by CPU 86017 on the L-type calcium channels in the myocardium and on the Ca2+-related contractions of vascular smooth muscle. METHODS: The whole-cell patch-clamp was applied to investigate the blocking effect of CPU 86017 on the L-type calcium current in isolated guinea pig myocytes and contractions by KCl or phenylephrine (Phe) of the isolated rat tail arteries were measured. RESULTS: Suppression of the L-type current of the isolated myocytes by CPU 86017 was moderate, in time- and concentration-dependent manner and with no influence on the activation and inactivation curves. The IC50 was 11.5 μmol/L. Suppressive effect of CPU 86017 on vaso-contractions induced by KCl 100 mmol/L, phenylephrine 1 μmol/L in KH solution (phase 1), Ca2+ free KH solution (phase 2), and by addition of CaCl2 into Ca2+-free KH solution (phase 3) were observed. The IC50 to suppress vaso-contractions by calcium entry via the receptor operated channel (ROC) and voltage-dependent channel (VDC) was 0.324 μmol/L and 16.3 μmol/L, respectively. The relative potency of CPU 86017 to suppress vascular tone by Ca2+ entry through ROC and VDC is 1/187 of prazosin and 1/37 of verapamil, respectively. CONCLUSION: The blocking effects of CPU 86017 on the L-type calcium channel of myocardium and vessel are moderate and non-selective. CPU 86017 is approximately 50 times more potent in inhibiting ROC than VDC.",
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Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017. / Dai, De Zai; Hu, Huijuan; Zhao, Jing; Hao, Xue Mei; Yang, Dong Mei; Zhou, Pei Ai; Wu, Cai Hong.

In: Acta Pharmacologica Sinica, Vol. 25, No. 4, 01.04.2004, p. 416-423.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Blockade of L-type calcium channel in myocardium and calcium-induced contractions of vascular smooth muscle by CPU 86017

AU - Dai, De Zai

AU - Hu, Huijuan

AU - Zhao, Jing

AU - Hao, Xue Mei

AU - Yang, Dong Mei

AU - Zhou, Pei Ai

AU - Wu, Cai Hong

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N2 - AIM: To assess the blockade by CPU 86017 on the L-type calcium channels in the myocardium and on the Ca2+-related contractions of vascular smooth muscle. METHODS: The whole-cell patch-clamp was applied to investigate the blocking effect of CPU 86017 on the L-type calcium current in isolated guinea pig myocytes and contractions by KCl or phenylephrine (Phe) of the isolated rat tail arteries were measured. RESULTS: Suppression of the L-type current of the isolated myocytes by CPU 86017 was moderate, in time- and concentration-dependent manner and with no influence on the activation and inactivation curves. The IC50 was 11.5 μmol/L. Suppressive effect of CPU 86017 on vaso-contractions induced by KCl 100 mmol/L, phenylephrine 1 μmol/L in KH solution (phase 1), Ca2+ free KH solution (phase 2), and by addition of CaCl2 into Ca2+-free KH solution (phase 3) were observed. The IC50 to suppress vaso-contractions by calcium entry via the receptor operated channel (ROC) and voltage-dependent channel (VDC) was 0.324 μmol/L and 16.3 μmol/L, respectively. The relative potency of CPU 86017 to suppress vascular tone by Ca2+ entry through ROC and VDC is 1/187 of prazosin and 1/37 of verapamil, respectively. CONCLUSION: The blocking effects of CPU 86017 on the L-type calcium channel of myocardium and vessel are moderate and non-selective. CPU 86017 is approximately 50 times more potent in inhibiting ROC than VDC.

AB - AIM: To assess the blockade by CPU 86017 on the L-type calcium channels in the myocardium and on the Ca2+-related contractions of vascular smooth muscle. METHODS: The whole-cell patch-clamp was applied to investigate the blocking effect of CPU 86017 on the L-type calcium current in isolated guinea pig myocytes and contractions by KCl or phenylephrine (Phe) of the isolated rat tail arteries were measured. RESULTS: Suppression of the L-type current of the isolated myocytes by CPU 86017 was moderate, in time- and concentration-dependent manner and with no influence on the activation and inactivation curves. The IC50 was 11.5 μmol/L. Suppressive effect of CPU 86017 on vaso-contractions induced by KCl 100 mmol/L, phenylephrine 1 μmol/L in KH solution (phase 1), Ca2+ free KH solution (phase 2), and by addition of CaCl2 into Ca2+-free KH solution (phase 3) were observed. The IC50 to suppress vaso-contractions by calcium entry via the receptor operated channel (ROC) and voltage-dependent channel (VDC) was 0.324 μmol/L and 16.3 μmol/L, respectively. The relative potency of CPU 86017 to suppress vascular tone by Ca2+ entry through ROC and VDC is 1/187 of prazosin and 1/37 of verapamil, respectively. CONCLUSION: The blocking effects of CPU 86017 on the L-type calcium channel of myocardium and vessel are moderate and non-selective. CPU 86017 is approximately 50 times more potent in inhibiting ROC than VDC.

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