Faculty Collaboration Database

High affinity binding of the calcium channel blocker, (+)-[methyl-3H]PN200-110(3HPN) in rat brain. Physiol Behav 1989 Jul;46(1):101-4

Date

07/01/1989

Pubmed ID

2554350

DOI

10.1016/0031-9384(89)90330-2

Scopus ID

2-s2.0-0024386952 (requires institutional sign-in at Scopus site)   4 Citations

Abstract

PN200-110 is a recently introduced 1,4-dihydropyridine which has been demonstrated to be a potent calcium channel blocker. 3HPN has been shown to bind in a specific saturable manner to P2 fractions obtained from brain homogenates from male Sprague-Dawley rats. 3HPN binding was found to be temperature-dependent. Specific 3HPN binding was maximal at 25 degrees C; binding decreased at 2 degrees C and 37 degrees C. The KD calculated from Scatchard analysis was 0.0943 +/- 0.0038 nM while the Bmax was found to be 109.1 +/- 2.3 fmol/mg protein. A concentration dependent inhibition of 3HPN binding by various cations was determined and found to be as follows: ZN2+ greater than La3+ greater than Rh3+, Al3+ greater than Co2+, Ni2+, Mn2+ greater than Ca2+, Mg2+ greater than Ba2+ greater than Sr2+. These results provide evidence for the existence of central high affinity dihydropyridine receptor sites in rat brain.

Author List

Magill SB, Stone JS, Parmar SS

Author

Steven B. Magill MD, PhD Staff Physician in the Medicine department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Animals
Brain
Calcium Channel Blockers
Calcium Channels
Isradipine
Male
Nifedipine
Oxadiazoles
Radioligand Assay
Rats
Rats, Inbred Strains
Receptors, Nicotinic
Synaptosomes