TY - JOUR
T1 - The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats
AU - Ehlert, Frederick J.
AU - Itoga, Eiko
AU - Roeske, William R.
AU - Yamamura, Henry I.
PY - 1982/2/11
Y1 - 1982/2/11
N2 - The binding properties of the calcium antagonist, [3H]nitrendipine, were investigated in homogenates of the rat cerebral cortex and myocardium. The specific component of [3H]nitrendipine binding was consistent with mass action behavior and was described by a high affinity dissociation constant in the range of 0.1 - 0.3 nM. [3H]nitrendipine binding was sensitive to inhibition by other calcium antagonists and by the cations Ca+2 and La+3. The inhibition of [3H]nitrendipine binding by verapamil was not of the simple competitive type but resembled allosteric inhibition, suggesting that there are at least two binding sites for calcium antagonists.
AB - The binding properties of the calcium antagonist, [3H]nitrendipine, were investigated in homogenates of the rat cerebral cortex and myocardium. The specific component of [3H]nitrendipine binding was consistent with mass action behavior and was described by a high affinity dissociation constant in the range of 0.1 - 0.3 nM. [3H]nitrendipine binding was sensitive to inhibition by other calcium antagonists and by the cations Ca+2 and La+3. The inhibition of [3H]nitrendipine binding by verapamil was not of the simple competitive type but resembled allosteric inhibition, suggesting that there are at least two binding sites for calcium antagonists.
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U2 - 10.1016/0006-291X(82)91339-0
DO - 10.1016/0006-291X(82)91339-0
M3 - Article
C2 - 7073736
AN - SCOPUS:0020004693
SN - 0006-291X
VL - 104
SP - 937
EP - 943
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 3
ER -