The highly selective 5‐hydroxytryptamine (5‐HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test

@article{Patel2004TheHS,
  title={The highly selective 5‐hydroxytryptamine (5‐HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test},
  author={Jignesh G Patel and Gerd D. Bartoszyk and E Edwards and Charles R. Ashby},
  journal={Synapse},
  year={2004},
  volume={52}
}
We examined the effect of the highly selective 5‐hydroxytryptamine (5‐HT)2A receptor antagonist 7‐{4‐[2‐(4‐fluoro‐phenyl)‐ethyl]‐piperazine‐1‐carbonyl}‐1H‐indole‐3‐carbonitrile HCl (EMD 281014) in congenital learned helpless male rats in the forced swim test. The administration of EMD‐281014 (0.3–30 mg/kg i.p.) to congenital learned helpless rats dose‐dependently and significantly (at 10 and 30 mg/kg) decreased immobility and increased swimming compared to vehicle‐treated animals. Thus, EMD… 
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TLDR
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TLDR
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TLDR
C. ferruginea exerts its antidepressant-like action through interaction with α-adrenoceptor, dopamine D2,5-HT2B, 5-HT6 and muscarinic cholinergi1c receptors as well as L-arginine-nitric oxide systems and could be used as adjuvant with conventional antidepressants in the treatment of major depressive disorder.
5-HT2 ligands in the treatment of anxiety and depression
TLDR
This review synthesizes the current literature about the behavioral, electrophysiological and neurochemical effects of 5-HT2 receptors ligands on the monoaminergic systems but also on adult hippocampal neurogenesis to shed some light on the preclinical evidence supporting the use of 5 -HT2A and/or 5- HT2C receptor antagonists such as antipsychotics, as potential effective adjuncts in SSRIs-resistant depression.
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References

SHOWING 1-9 OF 9 REFERENCES
In vitro autoradiography of serotonin 5‐HT2A/2C receptor‐activated G protein: Guanosine‐5′‐(γ‐[35S]thio)triphosphate binding in rat brain
TLDR
Autoradiography revealed a similar localization of DOI‐ and 5‐HT‐stimulated binding of [35S]GTPγS in distinct areas of prefrontal and parietal cortex, consistent with previously reported 5‐ HT2A receptor distribution.
EMD 281014, a new selective serotonin 5-HT2A receptor antagonist.
Antisense inhibition of 5-hydroxytryptamine2a receptor induces an antidepressant-like effect in mice.
TLDR
It is reported that down-regulation of the 5-HT2A receptor by intracerebroventricular injection of antisense oligonucleotides resulted in an antidepressant-like effect in mice and suggested that receptor down- regulation may be an essential part of the antidepressant drug action.
Active behaviors in the rat forced swimming test differentially produced by serotonergic and noradrenergic antidepressants
TLDR
This study demonstrated that distinct patterns of active behaviors are produced by antidepressants that selectively inhibit norepinephrine (NE) or serotonin (5-HT) uptake in the rat forced swimming test (FST), and showed that SSRIs are not false negatives in the FST.
Modulation of learned helplessness by 5-hydroxytryptamine2A receptor antisense oligodeoxynucleotides
Increased serotonin2 and beta-adrenergic receptor binding in the frontal cortices of suicide victims.
TLDR
The hypothesis that suicide completed by violent methods is associated with reduced presynaptic serotonergic activity that has generated compensatory upregulation of the postsynaptic serotonin2 receptor sites is supported and antidepressant pharmacotherapies specifically downregulate cortical beta-adrenergic and/or serotonin2 receptors in depressed subjects are investigated.
Behavioural despair in rats: a new model sensitive to antidepressant treatments.
Imaging of the serotonergic system: interactions of neuroanatomical and functional abnormalities of depression
Autoradiographic demonstration of increased serotonin 5-HT2 and beta-adrenergic receptor binding sites in the brain of suicide victims.
TLDR
It is concluded that suicide is associated with a localized increase in 5-HT2 binding sites, which is linked to a deficiency in serotonin neurotransmission.