The role and therapeutic potential
of 5-HT-moduline in psychiatry

by
Moret C, Grimaldi B, Massot O, Fillion G.
NeuroBiz Consulting and Communications,
Castres, France, and Neuromoduline Pharma, Paris, France.
Semin Clin Neuropsychiatry 2003 Apr;8(2):137-46


ABSTRACT

The endogenous neuropeptide, 5-HT-moduline, selectively and allosterically interacts with 5-HT(1B) receptors. By binding at a site distinct from that bound by 5-HT, 5-HT-moduline induces structural changes in 5-HT(1B) receptors or stabilizes a particular conformation of these receptors. These conformational changes ultimately lead to the prevention of 5-HT binding resulting in desensitization of these receptors and reduction of the serotonergic function. The efficacy of 5-HT(1B) receptor agonists, for example, has been shown to be reduced by this peptide in vitro and behaviorally. In addition, 5-HT-moduline increases 5-HT release, which is regulated by presynaptic 5-HT(1B) autoreceptors. The release of 5-HT-moduline itself is increased after acute restraint stress in rats, whereas deactivation of 5-HT-moduline by specific antibodies in mice prevents the development of anxiety in a classic behavioral model, suggesting a potential role of the peptide in the control of anxiety. It is thus hypothesized that agents inhibiting the effect of 5-HT-moduline could have anxiolytic activity. Because the serotonergic activity is known to play a key role in psychiatric disorders such as depression and anxiety, compounds capable of mimicking or inhibiting the activity of 5-HT-moduline can represent novel antidepressants or anxiolytics.
TCAs
SSRIs
5-HT1
5-HT2
5-HT3
5-HT1a
5-HT1b
5-HT2c
Anpirtoline
Eltoprazine
Zolmitriptan
Knockout mice
5-HT-moduline
5-HT2c/5-HT2b
5-HT1a v 5-HT1b
MDMA and 5-HT1a
5-HT1b and reward
Aggression and serotonin
5-HT1b, 5-HT-moduline and anxiety
Presynaptic and postsynaptic 5-HT1b receptors


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