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Vol. 282, Issue 2, 699-706, 1997
Department of Psychiatry, Case Western Reserve University, School
of Medicine, Cleveland, Ohio
The serotonin (5-HT)2A/2c agonist
1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), the
5-HT2C agonist 6-chloro-2-[1-piperazinyl]-pyrazine and
the 5-HT2A partial agonist m-chloro-phenylpiperazine (mCPP) were injected bilaterally into the medial prefrontal cortex of male
rats. DOI and mCPP, but not 6-chloro-2-[1-piperazinly]-pyrazine, elicited a dose-dependent head-twitch response (HTR). DOI-induced HTR
had an ED50 of 12.8 nmoles/0.5 µl/side and was inhibited
by the 5-HT2A antagonists ketanserin and MDL 100,907 but
was not blocked by pretreatment with the selective
5-HT2C/2B antagonist SDZ SER 082. The HTR to mCPP
demonstrated a bell-shaped dose-response curve with an ED50
of 1.5 nmoles/0.5 µl/side and a peak effect after 3 nmoles/side. The
response to mCPP was greatly diminished by both ketanserin and MDL
100,907 and was partially reversed by SDZ SER 082. These findings
suggest that the HTR produced by the direct injection of serotonergic
agonists into the medial prefrontal cortex is, in part, mediated by the
activation of 5-HT2A receptors. Pretreatment of rats with
the 5-HT1A agonist (±)-8-hydroxy-dipropylaminotetralin hydrobromide inhibited the HTR to DOI. This is consistent with other
evidence that suggests a functional antagonism between
5-HT1A and 5-HT2A receptor activation. The HTR
to DOI was potentiated by the novel 5-HT1A selective
antagonist WAY 100,635, which suggests that 5-HT1A
receptors tonically regulate this behavioral response to stimulation of
cortical 5-HT2A receptors.
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