High affinity binding of the calcium channel blocker, (+)-[methyl-3H]PN200-110(3HPN) in rat brain.

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.

journal_name

Physiol Behav

journal_title

Physiology & behavior

authors

Magill SB,Stone JS,Parmar SS

doi

10.1016/0031-9384(89)90330-2

subject

Has Abstract

pub_date

1989-07-01 00:00:00

pages

101-4

issue

1

eissn

0031-9384

issn

1873-507X

pii

0031-9384(89)90330-2

journal_volume

46

pub_type

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