QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

HOME  |   SEARCH  |   ARCHIVE  |   SUBSCRIBE  |   CONTACT  |   HELP

This Article Full Text (PDF) Submit an eLetter Alert me when this article is cited Alert me when eLetters are posted Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Conn, P. J. Articles by Sanders-Bush, E. Search for Related Content PubMed PubMed Citation Articles by Conn, P. J. Articles by Sanders-Bush, E.

 Previous Article  |  Next Article 

Journal of Neuroscience, Vol 6, 3669-3675, Copyright © 1986 by Society for Neuroscience

ARTICLE

Regulation of serotonin-stimulated phosphoinositide hydrolysis: relation to the serotonin 5-HT-2 binding site

PJ Conn and E Sanders-Bush

The hypothesis that serotonin (5-HT)-stimulated phosphoinositide hydrolysis is mediated by the 5-HT-2 binding site in cerebral cortex was tested by comparing antagonist Kd values determined by Schild analyses with Ki values at the 5-HT-2 binding site. A significant correlation was found between Kd values and Ki values at competing for 3H-ketanserin binding (R = 0.98), suggesting that the phosphoinositide- linked receptor and the 5-HT-2 site are identical. The 5-HT-2-mediated phosphoinositide response was then used as a measure of 5-HT-2 receptor sensitivity after in vivo treatments that alter the availability of 5- HT. Chronic treatment with the 5-HT-2 antagonist mianserin resulted in a significant decrease (52%) in the density of 5-HT-2 binding sites and a significant decrease (49%) in the maximal phosphoinositide hydrolysis response to 5-HT. Depletion of 5-HT levels with para- chlorophenylalanine or chemical denervation of serotonergic neurons with 5,7-dihydroxytryptamine had no significant effect upon 5-HT-2 receptor density or upon the phosphoinositide response to 5-HT. These data suggest that changes or lack of changes in 5-HT-2 receptor density following in vivo manipulations reflect the functional state of the receptor.

This article has been cited by other articles:

				L. A. Hazelwood and E. Sanders-Bush His452Tyr Polymorphism in the Human 5-HT2A Receptor Destabilizes the Signaling Conformation Mol. Pharmacol., November 1, 2004; 66(5): 1293 - 1300. [Abstract] [Full Text] [PDF]

				L. McGrew, M. S. S. Chang, and E. Sanders-Bush Phospholipase D Activation by Endogenous 5-Hydroxytryptamine 2C Receptors Is Mediated by Galpha 13 and Pertussis Toxin-Insensitive Gbeta gamma Subunits Mol. Pharmacol., December 1, 2002; 62(6): 1339 - 1343. [Abstract] [Full Text] [PDF]

Home  |   Search  |   Archive  |   Subscribe  |   Contact  |   Help