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Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding.
- C. Braestrup, R. Squires
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 1 September 1977
Specific [3H]diazepam binding to membranes appears to be restricted to brain, where it is unevenly distributed: the density of diazepam receptors is about five times higher in cortex (the highest density) than in pons-meddula (lowest density).
[35S]t-butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to gamma-aminobutyric acid-A and ion recognition sites.
High densities of benzodiazepine receptors in human cortical areas
It is reported here that benzodiazepine receptors are also present in the human brain, that the cerebral and cerebellar cortical regions contain the highest densities of binding sites and that the receptors in human brain are very similar to those in rat brain.
Benzodiazepine receptors in rat brain
Experiments suggest that another important group of psychoactive drugs, the benzodiazepines, bind to specific receptors on the membranes of rat brain cells, and this suggests that there may be an unknown endogenous neurotransmitter which is the natural ligand for the Benzodiazepine receptor.
EVIDENCE THAT 5‐METHOXY‐N, N‐DIMETHYL TRYPTAMINE IS A SPECIFIC SUBSTRATE FOR MAO‐A IN THE RAT: IMPLICATIONS FOR THE INDOLEAMINE DEPENDENT BEHAVIOURAL SYNDROME
- R. Squires
- Biology, ChemistryJournal of neurochemistry
- 1 January 1975
It is concluded that very little 5‐MeODMT or other 5‐methoxyindoleamines are formed endogenously in rat brain, and that the stereotyped syndrome of hyperactivity and tremors produced in rats by pretreatment with MAO inhibitors and L‐tryptophan is dependent on the formation of an N‐substituted derivative of 5‐HT which is at least partly deaminated by MAO‐B to 5‐HIAA.
Pharmacological characterization of benzodiazepine receptors in the brain.
Some properties of brain specific benzodiazepine receptors: New evidence for multiple receptors
Brain Specific Benzodiazepine Receptors
Brain membranes from rat and human contain a single class of brain specific binding sites for pharmacologically and clinically active benzodiazepines, which indicate that the in vitro 3H-diazepam and3H-flunitrazepam binding sites are the receptors which in vivo mediate various pharmacological and clinical effects of Benzodiazepine.
Enhancement of 3H-diazepam binding by SQ 65,396: A novel anti-anxiety agent