Triptan analog inhibits NF-kappaB

A triptan analog, a non-specific 5-HT1 agonist, is shown to reduce the production of pro-inflammatory cytokines via inhibition of NF-kappaB.

The triptans are an effective class of acute anti-migraine medications. Their mechanism of action has yet to be entirely determined, though they are known to be bind at 5-HT1b/d (serotonin) receptors.

In the study below, the effect of a similar molecule was investigated. m-CPP binds non-specifically to both 5-HT1 and 5-HT2  receptors. It may be that the anti-inflammatory effects of m-CPP are mediated through binding sites that are not effected by triptans. However, the triptans do exhibit certain anti-inflammatory effects that are similar to those observed for m-CPP. One possibility is that triptans also inhibit NF-kB and that some portion of their efficacy in the treatment of migraine is thereby accounted for.

The publication:

December, 2008

Anti-inflammatory effects of m-chlorophenylpiperazine in brain glia cells.

Summary of the abstract

Glia cells are regarded as a mediator of neuroinflammation releasing pro-inflammatory cytokines and nitric oxide in the central nervous system.

m-Chlorophenylpiperazine (m-CPP) is used clinically to manipulate serotonergic function, though its precise mechanisms of actions are not well understood. m-CPP alters synaptic transmission and neuronal function in vertebrates by non-selective agonistic actions on 5-HT1 and 5-HT2 receptors.

In the present study, the anti-inflammatory effect of m-CPP was investigated.

Rresults showed that m-CPP significantly decreased the production of nitric oxide, TNF, and IL-1beta in microglia and astrocyte cultures. m-CPP also attenuated the expression of inducible nitric oxide synthase and pro-inflammatory cytokines such as IL-1beta and TNF-alpha at mRNA levels. In addition, m-CPP inhibited NF-kB activation, providing molecular mechanisms of the anti-inflammatory effects.


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