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Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells.
Pharmazie. 2008 Jun; 63(6):470-4.P

Abstract

OBJECTIVE

Amlodipine (Aml) has R- and S-isomers with different pharmacological effects. However, no data are available on the influence of (S)-Aml and (R)-Aml on L-type calcium channel current (I(Ca-L)) or cytosolic calcium (Ca2+). This study is to investigate effects on I(Ca-L) and cytosolic Ca2+.

METHODS

I(Ca-L), peak currents, I-V curves, steady state activation curves, steady state inactivation curves and recovery curves from inactivation with (S)-Aml and (R)-Aml were recorded by whole-cell patch clamp configuration. Cytosolic Ca2+ of smooth muscle cells was assayed by Fura-2/AM.

RESULTS

At the concentrations of 0.1, 0.5, 1, 5, and 10 micromol/L, 1.5 +/- 0.2%, 25.4 +/- 5.3%, 65.2 +/- 7.3%, 78.4 +/- 8.1%, and 94.2 +/- 5.0% of I(Ca-L) were blocked by (S)-Aml. I-V curves were shifted upward. Half-activation voltages were -16.01 +/- 1.65 mV, -17.61 +/- 1.60 mV, -20.17 +/- 1.46 mV, -21.87 +/- 1.69 mV and -24.09 +/- 1.87 mV (P < 0.05). Half-inactivation voltages were -27.16 +/- 4.48 mV, -28.69 +/- 4.52 mV, -31.19 +/- 4.17 mV, -32.63 +/- 4.34 mV and -35.16 +/- 4.46 mV (P < 0.05). Recovery time were prolonged gradually (P < 0.05). 10.3 +/- 1.2%, 35.2 +/- 3.5%, 60.1 +/- 5.0%, 78.9 +/- 6.1%, and 91.2 +/- 7.6% of cytosolic Ca2+ were reduced at different concentrations (P < 0.05). However, (R)-Aml at different concentrations had no effect on I(Ca-L) and cytosolic Ca2+ (P > 0.05).

CONCLUSION

Only (S)-Aml has calcium channel blockade activity, while (R)-Aml has none of the pharmacologic actions associated with CCBs.

Authors+Show Affiliations

Wang RX
Department of Cardiology, First Affiliated Hospital of Nanjing Medical University in Wuxi, China.
Jiang WP
No affiliation info available
Li XR
No affiliation info available
Lai LH
No affiliation info available

MeSH

AmlodipineAnimalsAortaCalciumCalcium Channel BlockersCalcium Channels, L-TypeCytosolFemaleIn Vitro TechniquesIndicators and ReagentsKineticsMaleMyocytes, CardiacMyocytes, Smooth MusclePatch-Clamp TechniquesRatsRats, Sprague-DawleySolutionsStereoisomerism

Pub Type(s)

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

Language

eng

PubMed ID

18604992

Citation

Wang, Ru-Xing, et al. "Effects of (S)-amlodipine and (R)-amlodipine On L-type Calcium Channel Current of Rat Ventricular Myocytes and Cytosolic Calcium of Aortic Smooth Muscle Cells." Die Pharmazie, vol. 63, no. 6, 2008, pp. 470-4.
Wang RX, Jiang WP, Li XR, et al. Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells. Pharmazie. 2008;63(6):470-4.
Wang, R. X., Jiang, W. P., Li, X. R., & Lai, L. H. (2008). Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells. Die Pharmazie, 63(6), 470-4.
Wang RX, et al. Effects of (S)-amlodipine and (R)-amlodipine On L-type Calcium Channel Current of Rat Ventricular Myocytes and Cytosolic Calcium of Aortic Smooth Muscle Cells. Pharmazie. 2008;63(6):470-4. PubMed PMID: 18604992.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells. AU - Wang,Ru-Xing, AU - Jiang,Wen-Ping, AU - Li,Xiao-Rong, AU - Lai,Li-Hong, PY - 2008/7/9/pubmed PY - 2008/7/23/medline PY - 2008/7/9/entrez SP - 470 EP - 4 JF - Die Pharmazie JO - Pharmazie VL - 63 IS - 6 N2 - OBJECTIVE: Amlodipine (Aml) has R- and S-isomers with different pharmacological effects. However, no data are available on the influence of (S)-Aml and (R)-Aml on L-type calcium channel current (I(Ca-L)) or cytosolic calcium (Ca2+). This study is to investigate effects on I(Ca-L) and cytosolic Ca2+. METHODS: I(Ca-L), peak currents, I-V curves, steady state activation curves, steady state inactivation curves and recovery curves from inactivation with (S)-Aml and (R)-Aml were recorded by whole-cell patch clamp configuration. Cytosolic Ca2+ of smooth muscle cells was assayed by Fura-2/AM. RESULTS: At the concentrations of 0.1, 0.5, 1, 5, and 10 micromol/L, 1.5 +/- 0.2%, 25.4 +/- 5.3%, 65.2 +/- 7.3%, 78.4 +/- 8.1%, and 94.2 +/- 5.0% of I(Ca-L) were blocked by (S)-Aml. I-V curves were shifted upward. Half-activation voltages were -16.01 +/- 1.65 mV, -17.61 +/- 1.60 mV, -20.17 +/- 1.46 mV, -21.87 +/- 1.69 mV and -24.09 +/- 1.87 mV (P < 0.05). Half-inactivation voltages were -27.16 +/- 4.48 mV, -28.69 +/- 4.52 mV, -31.19 +/- 4.17 mV, -32.63 +/- 4.34 mV and -35.16 +/- 4.46 mV (P < 0.05). Recovery time were prolonged gradually (P < 0.05). 10.3 +/- 1.2%, 35.2 +/- 3.5%, 60.1 +/- 5.0%, 78.9 +/- 6.1%, and 91.2 +/- 7.6% of cytosolic Ca2+ were reduced at different concentrations (P < 0.05). However, (R)-Aml at different concentrations had no effect on I(Ca-L) and cytosolic Ca2+ (P > 0.05). CONCLUSION: Only (S)-Aml has calcium channel blockade activity, while (R)-Aml has none of the pharmacologic actions associated with CCBs. SN - 0031-7144 UR - https://www.unboundmedicine.com/medline/citation/18604992/Effects_of__S__amlodipine_and__R__amlodipine_on_L_type_calcium_channel_current_of_rat_ventricular_myocytes_and_cytosolic_calcium_of_aortic_smooth_muscle_cells_ DB - PRIME DP - Unbound Medicine ER -