Pleiotropic behavior of 5-HT2A
and 5-HT2C receptor agonists
by
Berg KA, Maayani S, Goldfarb J, Clarke WP
Department of Pharmacology,
University of Texas Health Science Center,
San Antonio 78284-7764, USA.
Br J Psychiatry 1997 Nov; 171:444-8

ABSTRACT

There is now considerable evidence that a single receptor subtype can couple to multiple effector pathways within a cell. Recently, Kenakin proposed a new concept, termed "agonist-directed trafficking of receptor stimulus", that suggests that agonists may be able to selectively activate a subset of multiple signaling pathways coupled to a single receptor subtype. 5-HT2A and 5-HT2C receptors couple to phospholipase C-(PLC) mediated inositol phosphate (IP) accumulation and PLA2-mediated arachidonic acid (AA) release. Relative efficacies of agonists (referenced to 5-HT) differed depending upon whether IP accumulation or AA release was measured. For the 5-HT2C receptor system, some agonists (e.g. TFMPP) preferentially activated the PLC-IP pathway, whereas others (e.g. LSD) favored PLA2-AA. As expected, EC50's of agonists did not differ between pathways. For the 5-HT2A receptor system, all agonists tested had greater relative efficacy for PLA2-AA than for PLC-IP. In contrast, relative efficacies were not different for 5-HT2A agonists when sequential effects in a pathway were measured (IP accumulation vs. calcium mobilization). These data strongly support the agonist-directed trafficking hypothesis.

LSD
SSRIs
5-HT2
5-HT3
5-HT4
5-H2c
5-HT1a
5-HT2a
5-HT1d
Serotonin
Agomelatine
5-HT2a antagonists
New antidepressants
Serotonin 5-HT2C receptors
Serotonergic genes and suicide
5-HT7 receptor antagonists as antidepressants
Depression, SSRIs and the serotonin 5-HT2 receptors

Refs
and further reading

HOME
HedWeb
Nootropics
cocaine.wiki
Future Opioids
BLTC Research
MDMA/Ecstasy
Superhapiness?
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family