TY - JOUR
T1 - Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791
AU - Kongsamut, Sathapana
AU - Kamp, Timothy J.
AU - Miller, Richard J.
AU - Sanguinetti, Michael C.
PY - 1985/7/16
Y1 - 1985/7/16
N2 - The effects of the pure stereoisomers of the novel dihydropyridine 202-791 on voltage sensitive calcium channels in nerve and cardiac muscle were examined. The (-)-isomer blocked depolarization-induced uptake of 45Ca2+ into NG108-15 neuroblastoma x glioma cells, blocked the depolarization-induced release of [3H]-norepinephrine from PC12 cells and reduced the Vmax of the slow response action potential recorded from guinea pig papillary muscle. In contrast, the (+)-isomer enhanced these same processes. In papillary muscle, greater enhancement of the slow responses was observed at lower stimulation frequencies. Thus, the (-) and (+) stereoisomers of 202-791 can be shown to be calcium channel antagonist and agonist respectively.
AB - The effects of the pure stereoisomers of the novel dihydropyridine 202-791 on voltage sensitive calcium channels in nerve and cardiac muscle were examined. The (-)-isomer blocked depolarization-induced uptake of 45Ca2+ into NG108-15 neuroblastoma x glioma cells, blocked the depolarization-induced release of [3H]-norepinephrine from PC12 cells and reduced the Vmax of the slow response action potential recorded from guinea pig papillary muscle. In contrast, the (+)-isomer enhanced these same processes. In papillary muscle, greater enhancement of the slow responses was observed at lower stimulation frequencies. Thus, the (-) and (+) stereoisomers of 202-791 can be shown to be calcium channel antagonist and agonist respectively.
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U2 - 10.1016/0006-291X(85)90393-6
DO - 10.1016/0006-291X(85)90393-6
M3 - Article
C2 - 2411259
AN - SCOPUS:0022260861
SN - 0006-291X
VL - 130
SP - 141
EP - 148
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 1
ER -
