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The time-course for up- and down-regulation of the cortical 5-hydroxytryptamine (5-HT)2A receptor density predicts 5-HT2A receptor-mediated behavior in the rabbit
Journal article   Peer reviewed

The time-course for up- and down-regulation of the cortical 5-hydroxytryptamine (5-HT)2A receptor density predicts 5-HT2A receptor-mediated behavior in the rabbit

Kuldip D Dave, John A Harvey and Vincent J Aloyo
The Journal of pharmacology and experimental therapeutics, v 323(1), pp 327-335
Oct 2007
DOI: https://doi.org/10.1124/jpet.107.121707
PMID: 17640952
Featured in Collection :   UN Sustainable Development Goals @ Drexel

Abstract

Amphetamines - administration & dosage Amphetamines - pharmacology Animals Behavior, Animal - drug effects Cerebral Cortex - drug effects Cerebral Cortex - metabolism Down-Regulation Injections, Intraventricular Male Piperidines - administration & dosage Piperidines - pharmacology Rabbits Receptor, Serotonin, 5-HT2A - administration & dosage Serotonin 5-HT2 Receptor Antagonists Serotonin Receptor Agonists - administration & dosage Serotonin Receptor Agonists - pharmacology Up-Regulation
5-Hydroxytryptamine (serotonin; 5-HT)2 receptor agonists such as (+/-)-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) injected systemically or directly into frontal cortex, elicit stereotyped head movements that are mediated by 5-HT2A receptors. Chronic administration of 5-HT2A receptor antagonists can produce either a down-regulation, e.g., d-2-bromolysergic acid diethylamide (BOL) or an up-regulation, e.g., alpha-phenyl-10(2-phenylethyl)-4-piperidinemethanol (MDL11,939) of cortical 5-HT2A receptors in the rabbit with no change in the density of the 5-HT2C receptor. We examined the degree to which the time course for the onset and offset of changes in cortical 5-HT2A receptor density was correlated with functional changes as measured by the magnitude of DOI elicited, 5-HT2A receptor-mediated head movements (head bobs). First, the magnitude of DOI-elicited head bobs was measured over 1 to 8 days after chronic BOL (5.8 micromol/kg), MDL11,939 (10 micromol/kg), or vehicle administration. Second, rabbits were injected with BOL, MDL11,939, or vehicle once daily for 8 days, and then, 1 to 8 days after the cessation of drug or vehicle, DOI-elicited head bobs were determined. Samples of frontal cortex were obtained for each animal immediately following behavioral testing, and 5-HT2A receptor density was measured using [3H]ketanserin. Thus, each animal provided a value for receptor density and number of head bobs, and these two measures showed a high degree of correlation between 0.94 for BOL and 0.95 for MDL11,939. This study establishes that the density of 5-HT2A receptors in cortex reflects their functional status.

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Web of Science research areas
Pharmacology & Pharmacy
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