Invention Summary: The Sigma-1 receptor (S1R) is a ligand-gated molecular chaperone protein, found in the endoplasmic reticulum and plasma membranes, which modulates mu-opioid and NMDA receptors. S1R antagonists can reduce the amplification of messages coming from pain sensors without impacting non-pain sensors that transmit other types of stimuli. Rutgers researchers have developed a new class of compounds, with the lead molecule named PW507, that exhibit: (1) potent S1R binding affinity and antagonism, (2) high selectivity for S1R over S2R, (3) favorable in vitro and in vivo metabolic stability, (4) good brain permeability (B/P ratio ≥ 14) and oral bioavailability (F=26%), (4) no CNS toxicity or general toxicity in rats, (5) dose-dependent analgesia in vivo in rodent models of neuropathic pain such as chemotherapy-induced pain models, and (6) significant potentiation effect (3 fold) of opioids’ analgesic effects in a mouse of acute pain. Market Applications: Treatment for pain Treatment for substance abuse Combination with opioids to reduce opioid dosage Advantages: Potent analgesic effect No addictive potential Negligible side effects Excellent metabolic stability High CNS penetration and oral bioavailability Intellectual Property & Development Status: Patent pending. Available for licensing and/or research collaboration.
|Original language||English (US)|
|State||Published - Apr 2019|