Faculty Collaboration Database

The dihydropyridine nitrendipine inhibits [3H]MK 801 binding to mouse brain sections. Eur J Pharmacol 1994 Nov 15;269(3):325-30

Date

11/15/1994

Pubmed ID

7534709

DOI

10.1016/0922-4106(94)90040-x

Scopus ID

2-s2.0-0028172966 (requires institutional sign-in at Scopus site)   15 Citations

Abstract

The L-type Ca2+ channel antagonist nitrendipine inhibits N-methyl-D-aspartate (NMDA)-activated Ca2+ flux into cerebellar granule cells, and [3H]dibenzocyclohepteneimine ([3H]MK 801) binding to mouse cerebral cortical and hippocampal membranes. To further study this interaction between nitrendipine and NMDA-activated channels, the effects of several L-channel active agents on [3H]MK 801 binding to mouse brain were investigated in an autoradiographic assay. Serial slide-mounted sagittal sections of mouse brain were labeled with [3H]MK 801 in the presence of varying concentrations of the L-channel active agents nitrendipine, nimodipine, nifedipine, Bay K 8644, and verapami. Nitrendipine potently displaced 2 nM [3H]MK 801 binding to mouse brain sections (IC50 = 89.8 nM). Dose-dependent inhibition of [3H]MK 801 binding by nitrendipine was demonstrated in most brain regions examined. 10(-5) M and 10(-8) M concentrations of the other dihydropyridines studied, and of verapamil, were without effect. The data supports a unique, direct interaction between nitrendipine and the NMDA-activated ion channel.

Author List

Filloux FM, Fitts RC, Skeen GA, White HS

Author

Robert Fitts PhD Professor in the Biological Sciences department at Marquette University

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

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
Analysis of Variance
Animals
Autoradiography
Binding, Competitive
Brain
Calcium
Dizocilpine Maleate
Dose-Response Relationship, Drug
Male
Mice
N-Methylaspartate
Nifedipine
Nimodipine
Nitrendipine
Software
Verapamil