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Studies on the neurotransmitter binding to pig brain microvessels
Journal of Neural Transmission. Supplementum
|January 1, 1983
Summary
This study investigated the binding of 3H-flunitrazepam in pig brain microvessels. Results indicate differences in binding kinetics compared to synaptosomal membranes, suggesting distinct receptor populations.
Area of Science:
- Neuroscience
- Biochemistry
- Pharmacology
Background:
- Brain microvessels play a crucial role in regulating the brain microenvironment.
- Understanding the molecular composition of microvessels is essential for studying drug delivery and neurological disorders.
Purpose of the Study:
- To characterize the binding properties of 3H-flunitrazepam in isolated pig brain microvessels.
- To compare these properties with those of a synaptosomal membrane fraction (P2-fraction).
Main Methods:
- Isolation of microvessels from pig brain using differential centrifugation.
- Assay of fraction purity and structural integrity via marker enzymes and microscopy.
- Kinetic studies of 3H-flunitrazepam binding.
- GABA kinetic studies.
Main Results:
- 3H-flunitrazepam binding in microvessels showed BMax of 0.42 ± 0.3 pmol/mg protein and KD of 1.26 ± 0.6 nM.
- Synaptosomal membranes (P2-fraction) exhibited higher BMax (2.68 ± 0.5 pmol/mg protein) and similar KD (1.95 ± 0.3 nM).
- GABA studies revealed IC50 values of 250 nM in microvessels versus 40 nM in the P2-fraction.
Conclusions:
- Pig brain microvessels possess distinct benzodiazepine binding characteristics compared to synaptosomal membranes.
- These findings suggest the presence of specific receptor sites within the brain microvasculature.
- Further research is warranted to elucidate the functional implications of these microvessel-associated receptors.