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Research ArticleNEUROPHARMACOLOGY

Selective and Divergent Regulation of Cortical 5-HT2AReceptors in Rabbit

Vincent J. Aloyo, Kuldip D. Dave, Tariq Rahman and John A. Harvey
Journal of Pharmacology and Experimental Therapeutics December 2001, 299 (3) 1066-1072;
Vincent J. Aloyo
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Kuldip D. Dave
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Tariq Rahman
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John A. Harvey
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Abstract

It is well established that repeated administration of both 5-hydroxytryptamine2 (5-HT2) receptor agonists and antagonists decreases the density of 5-HT2A and 5-HT2C receptors. However, the regulation of these two receptors has not been studied in the same tissue. Therefore, we examined the effects of repeated daily injections of the 5-HT2 receptor agonists (±)-2,5-dimethoxy-4-iodoamphetamine (DOI) and d-lysergic acid diethylamide (LSD) and the antagonistsd-2-bromolysergic acid diethylamide hydrogen tartrate (BOL) and α-phenyl-2-(2-phenylethyl)-4-piperidinemethanol (MDL 11,939) on rabbit cortical 5-HT2A and 5-HT2Creceptors. Repeated administration of DOI, LSD, or BOL decreased cortical 5-HT2A receptor density but had no effect on the density of cortical 5-HT2C receptors. Repeated administration of the selective 5-HT2A receptor antagonist MDL 11,939 significantly increased 5-HT2A receptor density. This unexpected outcome also occurred without any change in cortical 5-HT2C receptor density. The down-regulation of 5-HT2A receptors produced by chronic administration of BOL was associated with a decrease in DOI-elicited head bobs, whereas 5-HT2A receptor up-regulation produced by MDL 11,939 was associated with an increase in DOI-elicited head bobs compared with controls. These studies demonstrate that 5-HT2A receptor antagonists can both down- and up-regulate the density of cortical 5-HT2A receptors and these changes in receptor density have functional consequences for 5-HT2A receptor-mediated behaviors. Furthermore, because DOI, LSD, and BOL have approximately equal affinities for the 5-HT2A and 5-HT2Creceptors, these results suggest that different mechanisms regulate 5-HT2A and 5-HT2C receptor density, in that chronic occupation of 5-HT2C receptors does not modulate their density in rabbit frontal cortex.

Footnotes

  • This research was supported by U.S. Public Health Service Grant MH16841 from the National Institute for Mental Health and by Grant DA11164 from the National Institute on Drug Abuse.

  • Abbreviations:
    5-HT2
    5-hydroxytryptamine2
    DOI
    (±)-2,5-dimethoxy-4-iodoamphetamine
    BOL
    d-2-bromolysergic acid diethylamide hydrogen tartrate
    LSD
    d-lysergic acid diethylamide
    SR 46349B
    trans-4-[(3Z)3-(2-dimethylaminoethyl) oxyimino-3-(2-fluorophenyl) propen-1-yl] phenol
    MDL 11,939
    α-phenyl-2-(2-phenylethyl)-4-piperidinemethanol
    RS 102221
    α-benzenesulfonamide of 8-[5-(5-amino-2,4-dimethoxyphenyl) 5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione
    Gpp(NH)p
    5-guanylylimidodiphosphate
    • Received July 25, 2001.
    • Accepted September 7, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 299 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 299, Issue 3
1 Dec 2001
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Research ArticleNEUROPHARMACOLOGY

Selective and Divergent Regulation of Cortical 5-HT2AReceptors in Rabbit

Vincent J. Aloyo, Kuldip D. Dave, Tariq Rahman and John A. Harvey
Journal of Pharmacology and Experimental Therapeutics December 1, 2001, 299 (3) 1066-1072;

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Research ArticleNEUROPHARMACOLOGY

Selective and Divergent Regulation of Cortical 5-HT2AReceptors in Rabbit

Vincent J. Aloyo, Kuldip D. Dave, Tariq Rahman and John A. Harvey
Journal of Pharmacology and Experimental Therapeutics December 1, 2001, 299 (3) 1066-1072;
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