Identification of 5‐hydroxytryptamine1D binding sites in human brain membranes

@article{Peroutka1989IdentificationO5,
  title={Identification of 5‐hydroxytryptamine1D binding sites in human brain membranes},
  author={Stephen J. Peroutka and Jeffrey A. Switzer and Anne Hamik},
  journal={Synapse},
  year={1989},
  volume={3}
}
High‐affinity, specific 3H‐5‐hydroxytryptamine (5‐HT) binding was analyzed in membrane homogenates of human frontal cortex, caudate, and globus pallidus. 5‐HT1A and 5‐HT1C binding sites were pharmacologically blocked using 100 nM 8‐hydroxy‐N,N‐dipropyl‐2‐aminotetralin (8‐OH‐DPAT) and 100 nM mesulergine, respectively. The majority of 5‐HT1 sites remained in each of the three brain regions under these conditions. The pattern of nucleotide interactions with these binding sites (GppNHp = GTP = GDP… 
Binding studies with the 5‐HT1B receptor agonist [3H]CP‐96,501 in brain tissues
TLDR
Negligible specific binding of [3H]CP‐96,501 was found in membranes of guinea pig brain, dog hypothalamus, bovine caudate, pig choroid plexus, and several human brain tissues, consistent with the reported absence of the 5‐HT1B receptor subtype in these species.
Identification of 5-hydroxytryptamine1D binding sites in sheep caudate nucleus membranes.
TLDR
The present results indicate that sheep caudate nucleus is a valid tissue for studying interaction of compounds with 5- HT1D binding sites in the relative absence of 5-HT1E binding sites.
L‐694,247: a potent 5‐HT1D receptor agonist
TLDR
The excellent agreement observed for L‐694,247 between the 5‐HT1D radioligand binding affinity and the functional potency confirm that the two functional models (the inhibition of forskolin‐stimulated adenylyl cyclase in guinea‐pig substantia nigra and the inhibition of K+‐evoked [3H]‐5‐HT release from guinea-pig frontal cortex) do indeed reflect 5‐ HT1D‐mediated events.
An investigation of the 5-HT1D receptor binding affinity of 5-hydroxytryptamine, 5-carboxyamidotryptamine and sumatriptan in the central nervous system of seven species.
TLDR
Data indicate that under these experimental conditions the high affinity component labelled by [3H]5-HT is the same receptor subtype, previously denoted the 5-HT1D receptor, in all seven species.
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References

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TLDR
This putative novel 5‐HT receptor has a similar pharmacology to the “5‐HT1D” site detected in bovine brain by Heuring and Peroutka and is also detectable in human caudate.
Identification of Multiple Binding Sites for [3H]5‐Hydroxytryptamine in the Rat CNS
TLDR
The present data suggest the presence of three independent 5‐HT1 binding sites having different affinities for mianserin and spiperone and having different regional distributions.
Discrimination of Multiple [3H]5‐Hydroxytryptamine Binding Sites by the Neuroleptic Spiperone in Rat Brain
TLDR
Saturation studies of [3H]5‐HT binding assayed in the absence or presence of 1 μM‐spiperone reveal a parallel shift in the Scatchard plot with no change in the dissociation constant of [2‐12 nM], but a significant decrease in the number of specific binding sites.
Pharmacological Differentiation and Characterization of 5‐HT1A, 5‐HT1B, and 5‐HT1C Binding Sites in Rat Frontal Cortex
  • S. Peroutka
  • Chemistry, Medicine
    Journal of neurochemistry
  • 1986
TLDR
Computer‐assisted iterative curve fitting suggests that these drugs can discriminate two distinct subpopulations of non‐5‐ HT1A binding sites, each representing ∼35% of the total [3H]5‐HT binding in the rat frontal cortex.
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TLDR
The postsynaptic hippocampal [3H]8‐OH‐DPAT binding sites are probably identical to the 5‐HT1A, subsites, but the relationship between the presynaptic binding sites and the Presynaptic autoreceptors controlling 5‐ HT release deserves further investigation.
[3H]5‐Hydroxytryptamine Binding Sites: Species and Tissue Variation
TLDR
The present data are consistent with the concept of multiple 5‐HT1 binding sites and suggest the presence of at least two, and perhaps as many as three, groups of sites in the mammalian brain.
Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes
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  • Chemistry, Medicine
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TLDR
The data demonstrate the presence of a homogeneous class of 5- HT1 binding sites in bovine caudate that is pharmacologically distinct from previously defined 5-HT1A, 5-ht1B, 5 - HT1C, 4-HT2, 3-HT3 receptor subtypes.
Effect of Age on Human Brain Serotonin (S‐1) Binding Sites
The effect of age on the binding of [3H]5‐hydroxytryptamine ([3H]5‐HT, serotonin) to postmortem human frontal cortex, hippocampus, and putamen from individuals between the ages of 19 and 100 years
Ca2+‐Guanine Nucleotide Interactions in Brain Membranes. I. Modulation of Central 5‐Hydroxytryptamine Receptors in the Rat
TLDR
It is indicated that central 5‐hydroxytryptamine (5‐HT; serotonin) receptors can be modulated in opposite directions by Ca2+ and guanine nucleotides and compatible with the hypothesis of a possible coupling of some–but not all–[3H]5‐ HT binding sites to adenylate cyclase in the rat brain.
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