High affinity specific (/sup 3/H)(/sup +/)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart

Journal Article · Mon Aug 13 04:00:00 EDT 1984 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(84)90340-0· OSTI ID:6271877

Lee, H R; Roeske, W R; Yamamura, H I

The binding properties of the 1,4-dihydropyridine calcium channel antagonist, (/sup 3/H)(/sup +/)PN 200-110, were studied in rat cerebral cortical and cardiac homogenates (37/sup 0/C, Krebs phosphate buffer). Specific binding of (/sup 3/H)(/sup +/)PN 200-110 was saturable, reversible, and of high affinity (K/sub d/ values are 35 and 64 pM for the cerebral cortex and heart, respectively). In parallel studies with (/sup 3/H)(/sup +/)PN 200-110, the dissocation constant of (/sup 3/H)nitrendipine was 10-12 times higher. Substituted dihydropyridine calcium channel antagonists and agonists competively inhibited specific (/sup 3/H)(/sup +/)PN 200-110 binding, but d-cis diltiazem enhanced and verapamil incompletely inhibited (/sup 3/H)(/sup +/)PN 200-110 binding in both the cerebral cortex and the heart. The effects of diltiazem and verapamil on

• Research Organization: Univ. of Arizona Coll. of Medicine, Tucson
• OSTI ID: 6271877
• Journal Information: Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 35:7; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES