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Orexin A activates locus coeruleus cell firing and increases arousal in the rat.
  • J. Hagan, R. Leslie, +18 authors N. Upton
  • Medicine, Biology
    Proceedings of the National Academy of Sciences…
  • 14 September 1999
TLDR
It is shown that the brain region receiving the densest innervation from orexinergic nerves is the locus coeruleus, a key modulator of attentional state, where application of orexIn A increases cell firing of intrinsic noradrenergic neurones and modulates neuroendocrine function.
Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
TLDR
The effect of SB-277011-A on isolation-induced prepulse inhibition deficit suggests that blockade of dopamine D(3) receptors may benefit the treatment of schizophrenia.
Characterization of [125I]‐SB‐258585 binding to human recombinant and native 5‐HT6 receptors in rat, pig and human brain tissue
SB‐258585 (4‐Iodo‐N‐[4‐methoxy‐3‐(4‐methyl‐piperazin‐1‐yl)‐phenyl]‐benzenesulphonamide) is a high affinity ligand at 5‐HT6 receptors. It displays over 100 fold selectivity for the 5‐HT6 receptor over
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine]
TLDR
This paper describes how, using computational chemistry models as a guide, the nonselective 5- HT1B/5-HT1D receptor antagonist 4 was structurally modified to produce the selective 5-HT 1B receptor inverse agonist 5.
Characterization of SB‐271046: A potent, selective and orally active 5‐HT6 receptor antagonist
TLDR
It is demonstrated that SB‐271046 is a potent and selective 5‐HT6 receptor antagonist and is orally active in the rat MEST test and represents a valuable tool for evaluating the in vivo central function of 5‐ HT6 receptors.
Functional MRI detection of pharmacologically induced memory impairment
TLDR
It is suggested that pharmacologic effects can be detected with fMRI by using a reproducible experimental paradigm and that medications that impair memory also diminish activation in specific brain regions thought to subserve complex memory processes.
Effects of centrally administered orexin-B and orexin-A: a role for orexin-1 receptors in orexin-B-induced hyperactivity
TLDR
The present study has demonstrated a number of behavioural, neuroendocrine and neurochemical effects of orexin-B that distinguish it from oxin-A, and demonstrated a role for OX1 receptors in the actions of oX1-B upon motor activity.
Importance of h5-HT1B Receptor Selectivity for 5-HT Terminal Autoreceptor Activity: an In Vivo Microdialysis Study in the Freely-moving Guinea-pig
TLDR
The lack of effect of the above h5-HT1B receptor selective compounds and the decrease in extracellular 5-HT elicited by the non-selective compounds GR 127935, GR125743 and methiothepin suggest that antagonism of 5- HT1D receptors may mediate this decrease in 5-ht levels.
The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist [(125)I]SB-258585.
TLDR
The striatal binding sites seen in this study may be on intrinsic GABAergic or cholinergic neurones, or on terminals of projection neurones from the thalamus or cerebral cortex, and suggest a possible involvement of 5-HT(6) receptors in locomotor control, cognition, memory, and control of affect.
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