• Publications
  • Influence
5-HT7 receptors.
TLDR
Findings suggest that 5-HT(7) receptor-selective ligands might prove therapeutically useful for the treatment of psychiatric disorders and that the receptor may play a role in other CNS disorders including, anxiety, cognitive disturbances and also migraine probably via both peripheral and central mechanisms. Expand
Role of 5-HT receptor mechanisms in sub-chronic PCP-induced reversal learning deficits in the rat
TLDR
These studies implicate the role of 5-HT7, 5- HT2C, and5-HT1A receptors in the improvement of cognitive dysfunction of relevance to schizophrenia. Expand
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
TLDR
The structure-activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11, a potent and selective 5-ht5A receptor antagonist. Expand
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
A focused SAR study around the previously reported selective 5-HT(7) receptor antagonist, SB-269970-A has resulted in the identification of a structurally related analogue having an improvedExpand
5‐CT stimulation of adenylyl cyclase activity in guinea‐pig hippocampus: evidence for involvement of 5‐HT7 and 5‐HT1A receptors
TLDR
5‐HT7 receptor‐mediated stimulation of adenylyl cyclase activity in guinea‐pig hippocampus appears to be augmented by a mechanism involving 5‐HT1A receptor activation. Expand
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
TLDR
Evidence is provided for an autoreceptor role for the 5-ht5A receptor in guinea pig brain and a failure to affect both electrically-evoked 5-HT release and 5-CT-induced inhibition of evoked release measured using fast cyclic voltammetry in vitro. Expand
Distribution of 5-HT7 receptors in the human brain: a preliminary autoradiographic study using [ 3 H ]SB-269970
TLDR
The distribution pattern obtained in this study supports the involvement of this receptor subtype in affective behavior and cognition. Expand
5-ht5A receptors as a therapeutic target.
  • David R. Thomas
  • Biology, Medicine
  • Pharmacology & therapeutics
  • 1 September 2006
TLDR
It can be speculated that 5-ht5A receptor-selective ligands might show utility in psychiatric disorders such as schizophrenia and unipolar depression in which cognitive or mood disturbances are a feature. Expand
GABAergic modulation of 5-HT7 receptor-mediated effects on 5-HT efflux in the guinea-pig dorsal raphe nucleus
TLDR
5-HT(7) receptor antagonist-induced inhibition of 5-HT efflux occurs indirectly via activation of GABA(A) receptors, which may be located on GABA interneurones and when activated decrease GABA release and hence decrease the inhibitory tone on 5-ht neurones, increasing 5- HT efflux in the DRN. Expand
Cloning and pharmacological characterisation of the guinea pig 5-ht5A receptor.
TLDR
The data suggest that the guinea pig 5-hydroxytryptamine(5A) receptor couples to G(i)-proteins in this expression system and shows a similar pharmacological profile to that for the human 5-ht(5a) receptor. Expand
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