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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, BiologyProceedings of the National Academy of Sciences…
- 14 September 1999
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.
- C. Reavill, S. Taylor, +23 authors J. Hagan
- Chemistry, MedicineThe Journal of pharmacology and experimental…
- 1 September 2000
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]…
- L. Gaster, F. Blaney, +18 authors P. Slade
- Chemistry, MedicineJournal of medicinal chemistry
- 9 April 1998
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
- C. Routledge, S. Bromidge, +10 authors D. Middlemiss
- Chemistry, MedicineBritish journal of pharmacology
- 1 August 2000
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.
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
Functional MRI detection of pharmacologically induced memory impairment
- R. Sperling, D. Greve, +10 authors M. Albert
- MedicineProceedings of the National Academy of Sciences…
- 26 December 2001
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
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
- C. Roberts, G. W. Price, L. Gaster, B. Jones, D. Middlemiss, C. Routledge
- Medicine, ChemistryNeuropharmacology
- 1 April 1997
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.
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.