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British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1990 Feb;99(2):221–222. doi: 10.1111/j.1476-5381.1990.tb14683.x

Effects of a selective 5-HT2 agonist, DOI, on 5-HT neuronal firing in the dorsal raphe nucleus and 5-HT release and metabolism in the frontal cortex.

I K Wright 1, J C Garratt 1, C A Marsden 1
PMCID: PMC1917392  PMID: 1691671

Abstract

Systemic administration of the 5-HT2 agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) (50 and 100 micrograms kg-1, i.v.) inhibited dorsal raphe neuronal firing. DOI (100 micrograms kg-1, i.v.) also produced a decrease in extracellular 5-hydroxytryptamine (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA) in the frontal cortex measured by microdialysis. However, local administration of DOI into the frontal cortex produced no change in extracellular 5-HT and 5-HIAA at any dose given (1, 10 and 100ng). The results demonstrate that DOI is a potent inhibitor of 5-HT neuronal firing and terminal release and that the effects on release are not mediated by an action within the terminal region. The site of action and the receptor involved in the inhibition remains to be determined.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Aghajanian G. K., Foote W. E., Sheard M. H. Lysergic acid diethylamide: sensitive neuronal units in the midbrain raphe. Science. 1968 Aug 16;161(3842):706–708. doi: 10.1126/science.161.3842.706. [DOI] [PubMed] [Google Scholar]
  2. Glennon R. A. Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1–12. doi: 10.1021/jm00384a001. [DOI] [PubMed] [Google Scholar]
  3. Hoyer D., Pazos A., Probst A., Palacios J. M. Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition sites. Brain Res. 1986 Jun 18;376(1):97–107. doi: 10.1016/0006-8993(86)90903-0. [DOI] [PubMed] [Google Scholar]
  4. Marsden C. A., Sleight A. J., Fone K. C., Jonson J. V., Crespi F., Martin K. F., Garrett J. C., Bennett G. W. Functional identification of 5HT receptor subtypes. Comp Biochem Physiol A Comp Physiol. 1989;93(1):107–114. doi: 10.1016/0300-9629(89)90197-7. [DOI] [PubMed] [Google Scholar]
  5. McKenna D. J., Nazarali A. J., Hoffman A. J., Nichols D. E., Mathis C. A., Saavedra J. M. Common receptors for hallucinogens in rat brain: a comparative autoradiographic study using [125I]LSD and [125I]DOI, a new psychotomimetic radioligand. Brain Res. 1989 Jan 2;476(1):45–56. doi: 10.1016/0006-8993(89)91535-7. [DOI] [PubMed] [Google Scholar]
  6. Verge D., Daval G., Patey A., Gozlan H., el Mestikawy S., Hamon M. Presynaptic 5-HT autoreceptors on serotonergic cell bodies and/or dendrites but not terminals are of the 5-HT1A subtype. Eur J Pharmacol. 1985 Jul 31;113(3):463–464. doi: 10.1016/0014-2999(85)90099-8. [DOI] [PubMed] [Google Scholar]

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