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It Might Be a Big Family but the Pain Remains-Last Chance Saloon for Selective 5-HT Receptor Ligands?

It Might Be a Big Family but the Pain Remains-Last Chance Saloon for Selective 5-HT Receptor Ligands?

Nick Andrews, Michael F O'Neill

Curr Opin Pharmacol. 2011 Feb;11(1):39-44.

PMID: 21377931

Abstract:

The following brief overview reflects our own opinion of where the most likely advances to treating pain (unrelated to IBS and migraine) may come from with respect to ligands directly interacting with specific 5-HT receptors. It is fully appreciated, and possibly more likely, that 5-HT plays a modulatory role in the mediation of analgesic effects of certain compounds, for example tricyclic antidepressants and the newer, safer class of serotonin/noradrenaline re-uptake inhibitors, for example duloxetine and milnacipran. However, we find that recent pre-clinical findings highlight the potential of peripherally acting 5-HT(1) and 5-HT(2A) receptor agonists and centrally penetrating 5-HT(7) receptor agonists to reduce chronic pain. We encourage experimentation using human tissues and healthy volunteers to improve the confidence in rationale of targeting such receptors for treatment of pain in humans. However for this to happen the available pharmacological toolbox will also need to be further improved and any safety concerns understood to provide the necessary impetus to go to the clinic.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
CS31042344	Milnacipran Related Compound A			Price

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