Salvinorin Compounds and Uses Thereof

McLean Hospital
posted on 05/18/2011

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Depression is a mental condition that affects millions of people worldwide. Although there are various medications available, many of these have unacceptable side effects. Stressors that cause symptoms of depression increase the activation of cAMP response element-binding protein (CREB) in the nucleus accumbens. CREB activation results in over-expression of the opioid peptide dynorphin, which is an agonist of the kappa opioid receptors in the brain, and enhances symptoms of depression. It has been shown in animal models that kappa receptor antagonists produce antidepressant-like effects, possibly by mediating a disinhibition of dopamine release in the nucleus accumbens, thereby facilitating monoamine activity. The invention features novel chemical compounds based on a naturally occurring molecule that is known to be a high affinity and selective kappa receptor agonist. The chemical structure of the natural compound has been modified in specific ways, to alter its binding properties against the kappa receptor.
Potential Commercial Uses: The compounds of the invention show high affinity and specificity for the kappa opioid receptor. One derivative in particular was 7-fold more potent (as measured by EC50) than the naturally-occurring starting compound, with efficacy against the receptor of 98% compared to a known kappa agonist. The compounds of the invention can therefore be used in methods of treating depression, or can be the starting point for additional chemistry and drug design to develop antidepressive drugs.
Patent Status: McLean Hospital is the owner of U.S. Patent No. 7,629,475 and other pending U.S. patent applications claiming this invention. The research has been published in numerous scientific articles.
Licenses Available: McLean Hospital is offering a worldwide exclusive license to this technology.