Abstract
The binding properties of the 1,4-dihydropyridine calcium channel antagonist, [3H](+)PN 200-110, were studied in rat cerebral cortical and cardiac homogenates (37°C, Krebs phosphate buffer). Specific binding of [3H](+)PN 200-110 was saturable, reversible, and of high affinity (Kd values are 35 and 64 pM for the cerebral cortex and heart, respectively). In parallel studies with [3H](+)PN 200-110, the dissociation constant of [3H]nitrendipine was 10-12 times higher. Substituted dihydropyridine calcium channel antagonists and agonists competitively inhibited specific [3H](+)PN 200-110 binding, but d-cis diltiazem enhanced and verapamil incompletely inhibited [3H](+)PN 200-110 binding in both the cerebral cortex and the heart. The effects of diltiazem and verapamil on [3H](+)PN 200-110 binding were due mainly to alterations in the dissociation constant (Kd), without alterations in the binding density (Bmax). The new [3H](+)PN 200-110 receptor binding assay is remarkable for its low degree of nonspecific binding as compared to [3H]nitrendipine at physiological temperatures. [3H(+)PN 200-110 is a useful ligand for the further analysis of the dihydropyridine binding sites associated with calcium channels.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 721-732 |
| Number of pages | 12 |
| Journal | Life Sciences |
| Volume | 35 |
| Issue number | 7 |
| DOIs | |
| State | Published - Aug 13 1984 |
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ASJC Scopus subject areas
- Pharmacology
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High affinity specific [3H] (+)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart. / Lee, Howard R.; Roeske, William R; Yamamura, Henry I.
In: Life Sciences, Vol. 35, No. 7, 13.08.1984, p. 721-732.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - High affinity specific [3H] (+)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart
AU - Lee, Howard R.
AU - Roeske, William R
AU - Yamamura, Henry I.
PY - 1984/8/13
Y1 - 1984/8/13
N2 - The binding properties of the 1,4-dihydropyridine calcium channel antagonist, [3H](+)PN 200-110, were studied in rat cerebral cortical and cardiac homogenates (37°C, Krebs phosphate buffer). Specific binding of [3H](+)PN 200-110 was saturable, reversible, and of high affinity (Kd values are 35 and 64 pM for the cerebral cortex and heart, respectively). In parallel studies with [3H](+)PN 200-110, the dissociation constant of [3H]nitrendipine was 10-12 times higher. Substituted dihydropyridine calcium channel antagonists and agonists competitively inhibited specific [3H](+)PN 200-110 binding, but d-cis diltiazem enhanced and verapamil incompletely inhibited [3H](+)PN 200-110 binding in both the cerebral cortex and the heart. The effects of diltiazem and verapamil on [3H](+)PN 200-110 binding were due mainly to alterations in the dissociation constant (Kd), without alterations in the binding density (Bmax). The new [3H](+)PN 200-110 receptor binding assay is remarkable for its low degree of nonspecific binding as compared to [3H]nitrendipine at physiological temperatures. [3H(+)PN 200-110 is a useful ligand for the further analysis of the dihydropyridine binding sites associated with calcium channels.
AB - The binding properties of the 1,4-dihydropyridine calcium channel antagonist, [3H](+)PN 200-110, were studied in rat cerebral cortical and cardiac homogenates (37°C, Krebs phosphate buffer). Specific binding of [3H](+)PN 200-110 was saturable, reversible, and of high affinity (Kd values are 35 and 64 pM for the cerebral cortex and heart, respectively). In parallel studies with [3H](+)PN 200-110, the dissociation constant of [3H]nitrendipine was 10-12 times higher. Substituted dihydropyridine calcium channel antagonists and agonists competitively inhibited specific [3H](+)PN 200-110 binding, but d-cis diltiazem enhanced and verapamil incompletely inhibited [3H](+)PN 200-110 binding in both the cerebral cortex and the heart. The effects of diltiazem and verapamil on [3H](+)PN 200-110 binding were due mainly to alterations in the dissociation constant (Kd), without alterations in the binding density (Bmax). The new [3H](+)PN 200-110 receptor binding assay is remarkable for its low degree of nonspecific binding as compared to [3H]nitrendipine at physiological temperatures. [3H(+)PN 200-110 is a useful ligand for the further analysis of the dihydropyridine binding sites associated with calcium channels.
UR - http://www.scopus.com/inward/record.url?scp=0021144377&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0021144377&partnerID=8YFLogxK
U2 - 10.1016/0024-3205(84)90340-0
DO - 10.1016/0024-3205(84)90340-0
M3 - Article
C2 - 6088927
AN - SCOPUS:0021144377
VL - 35
SP - 721
EP - 732
JO - Life Sciences
JF - Life Sciences
SN - 0024-3205
IS - 7
ER -