International Myopain Society Meeting 2013 Cyclobenzaprine Abstract

INTERNATIONAL MYOPAIN SOCIETY MEETING
SEATTLE, WA, AUGUST 15-17, 2013
SCIENTIFIC POSTER REPORT #2

Cyclobenzaprine (CBP) inhibits Serotonin (5HT) Receptor Type 2A, Adrenergic Receptor
and the 5HT and Norepinephrine (NE) Reuptake Transporters:
Mechanistic Implications for Treating Fibromyalgia Syndrome and
Post-Traumatic Stress Disorder (PTSD) by Improving Sleep Quality

Bruce Daugherty, with Tonix Pharmaceuticals, gave a podium presentation on a new form of an old drug that has shown good efficacy in the treatment of fibromyalgia. He reported that a bedtime Cyclobenzaprine (CBP) is under development as a treatment for fibromyalgia symptoms that targets sleep quality. The interactions of CBP with neurotransmitter receptors and transporters have not been fully characterized. This led to the company’s study on binding and functional activity of CBP and its primary metabolite, norcyclobenzaprine (nCBP) on a set of central nervous system targets with potential relevance to sleep and pain effects.

Continue here from NFMCPA Advocate Voice Newsletter, August 2013

The study method included performance of equilibrium receptor binding on cell line membranes expressing select recombinant human receptors and transporters. Cell based functional assays were performed by ligand-induced CA2+flux.

It was determined that CPB is a potent antagonist of 5HT2A and î+1A receptors as well as 5HT and NE reuptake. Trazodone, widely used off label for sleep effects, inhibits 5HT2A and 5HT reuptake has been designated a Serotonin receptor Antagonist and Reuptake Inhibitor. The end result is that taken together, at the level of synaptic monoamine receptors, bedtime cyclobenzaprine combines some activities of trazodone and prazosin, (a drug used off label to prevent night terrors) and may have similar effects on sleep and sleep quality.

Tonix is working with the University of Michigan to fulfill the Stage 2B levels of the study. If the results of this round of discovery are consistent with the other phases of the investigation, a Stage 3 study will be launched to finalize the results. The University of Michigan will oversee the study in several locations around the country. If you are interested in being a study participant, please keep checking the research area of the NFMCPA website for further information.