The effects of pharmacological blockade of the 5-HT(6) receptor on formalin-evoked nociceptive behaviour, locomotor activity and hypothalamo-pituitary-adrenal axis activity in rats.

Abstract	5-hydroxytryptamine (5-HT) mediates behavioural and neuroendocrine responses to noxious or stressful stimuli. 5-HT(6) receptors are expressed in brain regions involved in nociceptive processing, however, their role in nociception is unknown. Here we demonstrate that acute, systemic administration of the 5-HT(6) receptor antagonist, 5-chloro-N-(4-methoxy-3-benzothio-phenesulfonamide (SB-271046), reduces formalin-evoked nociceptive behaviour and increases plasma corticosterone. SB-271046 dose-dependently reduced pre-formalin distance moved, rearing, grooming and defecation. These data provide the first evidence for 5-HT(6) receptor-mediated regulation of nociception and hypothalamo-pituitary-adrenal axis activity in a model of persistent pain although effects on locomotor activity demand that the putative antinociceptive effect of SB-271046 be interpreted with some caution.
Authors	David P Finn, Kevin C F Fone, Simon R G Beckett, Jonathan A Baxter, Lucy Ansell, Charles A Marsden, Victoria Chapman
Journal	European journal of pharmacology (Eur J Pharmacol) Vol. 569 Issue 1-2 Pg. 59-63 (Aug 13 2007) ISSN: 0014-2999 [Print] Netherlands
PMID	17599826 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Receptors, Serotonin Serotonin Antagonists Sulfonamides Thiophenes serotonin 6 receptor Formaldehyde SB 271046 Corticosterone
Topics	Analysis of Variance Animals Behavior, Animal (drug effects) Corticosterone (blood) Defecation (drug effects) Dose-Response Relationship, Drug Formaldehyde (toxicity) Grooming (drug effects) Hypothalamo-Hypophyseal System (drug effects, physiology) Injections, Intraperitoneal Male Motor Activity (drug effects, physiology) Pain (chemically induced, physiopathology, prevention & control) Pain Measurement (methods) Pituitary-Adrenal System (drug effects, physiology) Radioimmunoassay Rats Receptors, Serotonin (physiology) Serotonin Antagonists (administration & dosage, pharmacology) Stress, Physiological (blood, chemically induced) Sulfonamides (administration & dosage, pharmacology) Thiophenes (administration & dosage, pharmacology) Time Factors

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