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Quantitative autoradiographic analysis of the new radioligand [3H](2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid ([3H]NCS-382) at γ-hydroxybutyric acid (GHB) binding sites in rat brain
- Source :
- Brain Research. 979:51-56
- Publication Year :
- 2003
- Publisher :
- Elsevier BV, 2003.
-
Abstract
- (2E)-(5-Hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene) ethanoic acid (NCS-382) is an antagonist for gamma-hydroxybutyric acid (GHB) at GHB receptor sites. Advantages of using [(3)H]NCS-382 over [(3)H]GHB in radioligand binding studies are that unlike GHB, NCS-382 does not appear to bind to, activate, or interfere with the functioning of GABA(B) or GABA(A) receptors, either directly or indirectly. Herein we establish a protocol for use of [(3)H]NCS-382 by quantitative autoradiography. GHB was used to define non-specific binding, since it displaced [(3)H]NCS-382 to an extent equivalent to NCS-382. Among many areas of brain examined, two regions in which high specific binding of [(3)H]NCS-382 occurred were the hippocampus and cerebral cortex. Areas such as the striatum and nucleus accumbens exhibited intermediate levels of specific binding. No or very low binding was observed in other areas such as the cerebellum and dorsal raphe nucleus. The distribution of GHB binding sites as defined by [(3)H]NCS-382 suggests that GHB may play a role in neuromodulation or neurotransmission in frontal brain areas.
- Subjects :
- Male
Stereochemistry
NCS-382
Hydroxybutyrates
Receptors, Cell Surface
Striatum
Nucleus accumbens
Tritium
Binding, Competitive
behavioral disciplines and activities
Rats, Sprague-Dawley
Radioligand Assay
chemistry.chemical_compound
Dorsal raphe nucleus
Receptors, GABA
mental disorders
Radioligand
Animals
Molecular Biology
GABAA receptor
General Neuroscience
GHB receptor
Brain
Rats
Benzocycloheptenes
chemistry
Biochemistry
Autoradiography
Neurology (clinical)
Developmental Biology
Subjects
Details
- ISSN :
- 00068993
- Volume :
- 979
- Database :
- OpenAIRE
- Journal :
- Brain Research
- Accession number :
- edsair.doi.dedup.....92b5d3d05198a898f522333768c763f6
- Full Text :
- https://doi.org/10.1016/s0006-8993(03)02865-8