Identification and Characterisation of 5‐Hydroxytryptamine3 Recognition Sites in Human Brain Tissue

  title={Identification and Characterisation of 5‐Hydroxytryptamine3 Recognition Sites in Human Brain Tissue},
  author={Janine M. Barnes and Nicholas M Barnes and Brenda Costall and James W. Ironside and Robert J. Naylor},
  journal={Journal of Neurochemistry},
Abstract: [3H]Zacopride displayed regional saturable specific binding to homogenates of human brain tissues, as defined by the inclusion of BRL43694 [endo‐N‐(9‐methyl‐9‐azabicyclo[3.3.1]non‐3‐yl)‐l‐methylindazole‐3‐carboxamide] in the incubation media. Scatchard analysis of the saturation data obtained from amygdaloid and hippocampal tissues identified the binding as being of high affinity and to a homogeneous population of binding sites (KD= 2.64 ± 0.75 and 2.93 ± 0.41 nmol/L and Bmax= 55 ± 7… 
Pharmacological and Regional Characterization of [3H]LY278584 Binding Sites in Human Brain
It is concluded that 5‐HT3 receptors labeled by [3H]LY278584 are present in both limbic and striatal areas in human brain, suggesting that 5-HT3 receptor antagonists may be able to influence the dopamine system in humans, similarly to their effects in rodent studies.
Identification and distribution of 5‐HT3 recognition sites in the rat gastrointestinal tract
It is demonstrated that there are regional variations in the density of 5‐HT3 recognition sites within the rat gastrointestinal tract, relevant to the potential use of 5-HT3 receptor ligands to modify secretory and contraction responses in the gastrointestinal system.
Labelling of 5‐Hydroxytryptamine3 Receptors with a Novel 5‐HT3 Receptor Ligand, [3H]RS‐42358–197
Differences in 5‐HT3 receptors of different tissues and species were detected on the basis of statistically significant differences in the affinities of phenylbiguanide, and 1‐(m‐chlorophenyl) biguanide when displacing [3H]RS‐42358‐197 binding.
Agonist interactions with 5‐HT3 receptor recognition sites in the rat entorhinal cortex labelled by structurally diverse radioligands
1 The pharmacological properties of 5‐HT3 receptor recognition sites labelled with [3H]‐(S)‐zacopride, [3H]‐LY278,584, [3H]‐granisetron and [3H]‐GR67330 in membranes prepared from the rat entorhinal
5‐Hydroxytryptamine (5‐HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases
A heterogeneous distribution of 5‐HT4 receptors in human brain, with high to moderate densities in basal ganglia and limbic structures is suggested, given the lack of change observed in Parkinson's disease.
Characterization of a human 5‐hydroxytryptamine3 receptor type A (h5‐HT3R‐AS) subunit stably expressed in HEK 293 cells
The construction of a stable cell line expressing a high density of recombinant human 5‐ HT3 receptors which display appropriate pharmacology and function will assist in the further characterization of this receptor subtype and the exploration of species differences in 5‐HT3 receptor pharmacology.
Membrane‐Bound and solubilized brain 5HT3 receptors: Improved radioligand binding assays using bovine area postrema or rat cortex and the radioligands 3H‐Gr65630C, 3H‐BRl43694, and 3H‐LY278584
Bovine area postrema tissue was used as a convenient source of tissue for studies of brain 5HT3 receptor density was determined to be 97 ± 5 fmol/mg and 124 ± 10 fmol/mg of protein using the
Molecular modeling of 5-HT3 receptor ligands


[3H]Zacopride: Ligand for the Identification of 5‐HT3 Recognition Sites
It is concluded that [3H]zacopride may prove a useful ligand for the study of 5‐HT3 recognition sites.
Identification of 5‐HT3 recognition sites in human brain tissue using [3H]zacopride
The first direct evidence for the existence of 5- HT3 recognition sites in human brain tissue is reported using the tritiated derivative of the potent and selective 5-HT3 receptor antagonist zacopride (US. Patent Number 465791 1 assigned to Delalande; Smith et al 1988).
Biochemical characterization of the muscarinic cholinergic receptor in human brain: alterations in Huntington's disease.
It was revealed that the decreases in ligand binding were due to receptor loss rather than to changes in receptor affinity, and Huntington’s diseased brains had significant decreases in muscarinic receptor binding in the caudate nucleus and putamen.
Pharmacological properties of GR38032F, a novel antagonist at 5‐HT3 receptors
R,S‐GR38032F is highly selective for 5‐HT3 receptors, and at concentrations of 3 × 10‐6‐3 × 10−5m, had negligible agonist or antagonist activity on other 5‐ HT or non‐5‐HT receptor‐containing tissues on which it was tested.
Species variations in 5-HT3 recognition sites labeled by 3H-quipazine in the central nervous system
  • S. Peroutka
  • Biology
    Naunyn-Schmiedeberg's Archives of Pharmacology
  • 1988
The data indicate that marked species variations exist in the presence and/or density of 5-HT3 membrane recognition sites in the central nervous system and no significant specific binding of 3H-quipazine could be detected in human or animal brain membranes.
Identification of 5‐HT3 recognition sites in the ferret area postrema
The results indicate that 5‐HT3 recognition sites are present within the area postrema and may afford an antiemetic site of action for zacopride and other 5‐ HT3 receptor antagonists.
Identification and distribution of 5-HT3 receptors in rat brain using radioligand binding
Direct evidence for the existence of 5-HT3 receptors in rat brain tissue and their distribution is reported, based on high affinity binding of the potent 5- HT3 receptor antagonist 3H-GR65630 to homogenates of rat entorhinal cortex.