SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4′-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain

@article{Thomas2006SB699551AD,
  title={SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4′-\{[(2-phenylethyl)amino]methyl\}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain},
  author={David R. Thomas and Ellen M. Soffin and Claire Roberts and James N. C. Kew and Ra{\'u}l de la Flor and Lee A. Dawson and Victoria A H Fry and Sara A. Coggon and Stefania Faedo and Philip David Hayes and David F. Corbett and Ceri H. Davies and Jim J. Hagan},
  journal={Neuropharmacology},
  year={2006},
  volume={51},
  pages={566-577}
}
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49 Citations
Highly Influential Citations
4
Background Citations
9
Methods Citations
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49 Citations

Citation Type

Citation Type

Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats
Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors.
TLDR
The present data suggest that 5-HT may release GH through a pituitary site of action, and that the 5-HTR2B, 5- HTR7 and 5-hTR1B mediate this response, with possibly an inhibitory component of the 5.HTR1D.
GR-127935-sensitive Mechanism Mediating Hypotension in Anesthetized Rats: Are 5-HT5B Receptors Involved?
TLDR
It is suggested that the GR-127935-sensitive mechanism mediating hypotension in rats is unrelated to 5-HT1B, 5- HT1D, 3-HT5A, 4-HT6, and5-HT7 receptors; this mechanism, however, resembles putative 5-ht5B receptors.
The Native Serotonin 5-HT5A Receptor: Electrophysiological Characterization in Rodent Cortex and 5-HT1A-Mediated Compensatory Plasticity in the Knock-Out Mouse
TLDR
Electrophysiologically identify and characterize a native 5-HT5A receptor current in acute ex vivo brain slices of adult rodent prefrontal cortex and observe that genetic deletion of the inhibitory 5- HT5A receptors results in an unexpected, large increase in the inhibitors of this receptor in the healthy prefrontal cortex.
Differential influence of selective 5-HT5A vs 5-HT1A, 5-HT1B, or 5-HT2C receptor blockade upon light-induced phase shifts in circadian activity rhythms: Interaction studies with citalopram
Involvement of 5-HT1 and 5-HT5A Receptors in Modulation of Synaptic Transmission and Intrinsic Membrane Properties of Spinal Motoneurons of the Frog (Rana ridibunda)
TLDR
The results indicate the involvement of 5- HT 5A receptors, along with 5-HT 1 receptors, in the modulation of motor output of frog spinal motoneurons.
Role of 5-HT5A and 5-HT1B/1D receptors in the antinociception produced by ergotamine and valerenic acid in the rat formalin test.
Identification and functional significance of N-glycosylation of the 5-ht5A receptor
Role of 5-HT5A receptors in the consolidation of memory
The serotonin 5-HT7 receptor agonist LP-44 microinjected into the dorsal raphe nucleus suppresses REM sleep in the rat
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References

SHOWING 1-10 OF 37 REFERENCES
WAY-100635 and GR127935: effects on 5-hydroxytryptamine-containing neurones.
5-HT1D as well as 5-HT1A autoreceptors modulate 5-HT release in the guinea-pig dorsal raphénucleus
Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.
TLDR
Two serotonin (5-hydroxytryptamine, 5-HT) receptors, MR22 and REC17, that belong to the G-protein-associated receptor superfamily are reported and it is proposed that REC17 and MR22 represent a distinct subfamily of 5- HT receptors.
The human 5-ht5A receptor couples to Gi/Go proteins and inhibits adenylate cyclase in HEK 293 cells.
Cloning and pharmacological characterisation of the guinea pig 5-ht5A receptor.
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
[3H]‐SB‐269970 – A selective antagonist radioligand for 5‐HT7 receptors
TLDR
The data suggest that, in each tissue, both radioligands labelled the same population of receptors, which appear to be present in an agonist high affinity state in both tissues.
Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
TLDR
The 5-HT5A gene colocalized with the mouse mutation reeler and the human mutation holoprosencephaly type 3, which both result in abnormal brain development, raising the possibility that the 5- HT5A receptor plays a role in brain development.
Ligands for the investigation of 5-HT autoreceptor function
Enhancement of 5-HT1B and 5-HT1D receptor antagonist effects on extracellular 5-HT levels in the guinea-pig brain following concurrent 5-HT1A or 5-HT re-uptake site blockade
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