Functional and Radioligand Binding Characterization of Rat 5-HT6 Receptors Stably Expressed in HEK293 Cells

@article{Boess1997FunctionalAR,
  title={Functional and Radioligand Binding Characterization of Rat 5-HT6 Receptors Stably Expressed in HEK293 Cells},
  author={Frank Boess and Frederick J. Monsma and C Carolo and V. Meyer and Alain Rudler and Catherine Zwingelstein and Andrew J. Sleight},
  journal={Neuropharmacology},
  year={1997},
  volume={36},
  pages={713-720}
}
Characterization of 5-ht6 receptor and expression of 5-ht6 mRNA in the rat brain during ontogenetic development
TLDR
The hypothesis that 5-ht6 receptors may correspond to an important target for atypical antipsychotics and reveal an original pharmacological profile for this receptor is confirmed and its role in the early growth process involving the serotonergic system is suggested.
Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue.
TLDR
High affinity, selective radioligand which can be used to label both recombinant and native 5-HT(6) receptors and will facilitate further characterization of this receptor subtype in animal and human tissues is found.
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
TLDR
The affinities of 14 5-HT6 receptor ligands at this binding site were similar to those found for the recombinant rat and human 5- HT6 receptor, which suggested the presence of 5-hydroxytryptamine6 receptors in porcine striatum.
Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor.
TLDR
The ligand-binding site of the 5-hydroxytryptamine6 (5-HT6) receptor was examined using site-directed mutagenesis and it was indicated that in wild-type 5- HT6 receptor, Thr196 interacts with the N1 of N1-unsubstituted ergolines and tryptamines, probably forming a hydrogen bond.
5-Hydroxytryptamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
TLDR
Unique amongst the GPCRs, RNA editing produces 5-HT2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to Gq/11 and also pharmacology [40, 482].
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The pharmacological profile of this receptor, characterized by both radioligand binding and functional coupling to adenylyl cyclase, does not correspond to that of any of the currently classified subtypes of 5- HT receptor, but is similar to the 5-HT receptor cloned recently from rat striatum and referred to as the5-HT6 receptor.
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TLDR
The authors examined the affinities of 36 typical and atypical antipsychotic agents for the cloned rat 5-hydroxytryptamine-6 and rat5-HT7 receptors in transiently expressed COS-7 cells or stably transfected HEK-293 cells to identify those with high affinity for the newly discovered 5-HT6 receptor.
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TLDR
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