Abstract
An in vitro autoradiographic technique has been used for the quantitative mapping of calcium antagonist binding sites (CABS) in the rat brain, using the 1,4-dihydropyridines [3H]PN 200-110 and [3H]PY 108-068 as ligands. CABS were distributed throughout the brain in a highly heterogeneous fashion. The highest densities of CABS were observed in the olfactory bulb, hippocampus and parts of the amygdala. The neocortex was also rich in CABS. The basal ganglia, thalamus and hypothalamus presented intermediate levels of CABS while low densities of sites were seen in areas such as the cerebellum, pons and white matter tracts. The distributions of CABS in brain does not correlate with indexes of brain blood flow, regional glucose utilization or the distributions of receptor binding sites for drugs and neurotransmitters analyzed until now. No correlation exists between CABS distribution and that of any neurotransmitter or brain enzyme described so far. The heterogeneous distributions of CABS is suggestive of a neuronal localization, an idea supported by lesion experiments.
MeSH Terms
Animals
Autoradiography
Binding Sites
Brain/metabolism
Calcium Channel Blockers/metabolism
Isradipine
Male
Nifedipine/analogs & derivatives,metabolism
Oxadiazoles/metabolism
Rats
Rats, Inbred Strains
Chemicals
Calcium Channel Blockers
Oxadiazoles
Nifedipine
darodipine
Isradipine
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Cortés R
Supavilai P
Karobath M
Palacios J M
References (16)
16 references, click to expand
-
Intraperitoneal administration and other modifications of the 2-deoxy-D-glucose technique.
Brain Res. 1980 Aug 11;195(1):167-76
PMID: 7397493
-
Autoradiographic localization of a calcium channel antagonist, [3H]nitrendipine, binding site in rat brain.
Neurosci Lett. 1983 Apr 29;36(3):267-71
PMID: 6866333
-
A unitary mechanism of calcium antagonist drug action.
Proc Natl Acad Sci U S A. 1983 Feb;80(3):860-4
PMID: 6572372
-
Autoradiographic visualization of [3H]nitrendipine binding sites in rat brain: localization to synaptic zones.
Eur J Pharmacol. 1982 Jul 16;81(3):517-9
PMID: 7117385
-
The [14C]deoxyglucose method for the measurement of local cerebral glucose utilization: theory, procedure, and normal values in the conscious and anesthetized albino rat.
J Neurochem. 1977 May;28(5):897-916
PMID: 864466
-
[3H]-Nimodipine and [3H]-nitrendipine as tools to directly identify the sites of action of 1,4-dihydropyridine calcium antagonists in guinea-pig tissues. Tissue-specific effects of anions and ionic strength.
Arzneimittelforschung. 1982;32(4):361-3
PMID: 7201804
-
The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats.
Biochem Biophys Res Commun. 1982 Feb 11;104(3):937-43
PMID: 7073736
-
The effects of lesions in the rat hippocampus suggest the association of calcium channel blocker binding sites with specific neuronal population.
Neurosci Lett. 1983 Dec 11;42(3):249-54
PMID: 6320069
-
Evidence of multiple receptor sites within the putative calcium channel.
Naunyn Schmiedebergs Arch Pharmacol. 1982 Oct;321(1):80-3
PMID: 6292744
-
Connections of the cerebral cortex; the albino rat; topography of the cortical areas.
J Comp Neurol. 1946 Apr;84:221-75
PMID: 20982805
-
Connections of the cerebral cortex; the albino rat; structure of the cortical areas.
J Comp Neurol. 1946 Jun;84:277-323
PMID: 20991808
-
Quantitative receptor autoradiography using [3H]ultrofilm: application to multiple benzodiazepine receptors.
J Neurosci Methods. 1982 Jul;6(1-2):59-73
PMID: 6126619
-
The interaction of [3H]PY 108-068 and of [3H]PN 200-110 with calcium channel binding sites in rat brain.
J Neural Transm. 1984;60(3-4):149-67
PMID: 6098633
-
Measurement of regional cerebral blood flow with antipyrine-14C in awake cats.
J Appl Physiol. 1969 Aug;27(2):296-300
PMID: 5796327
-
Behavioral effects of nimodipine in animals.
Arzneimittelforschung. 1982;32(4):347-60
PMID: 7201803
-
High affinity binding of a calcium channel antagonist to smooth and cardiac muscle.
Biochem Biophys Res Commun. 1982 Feb 26;104(4):1604-9
PMID: 7073757