NS16085 / Saniona - LARVOL DELTA

Antinociceptive effects of α2/α3-subtype selective GABAA receptor positive allosteric modulators KRM-II-81 and NS16085 in rats: behavioral specificity. (PubMed, J Pharmacol Exp Ther) - "The benzodiazepine midazolam was used as a comparator in these studies. Significance Statement This study demonstrates that α2/α3-subtype selective GABAA PAMs KRM-II-81 and NS16085 produce selective antinociceptive effects devoid of sedation, myorelaxation, cognitive impairment in two rat models of persistent pain. Unlikely classical benzodiazepines, this study supports the development of α2/α3-subtype selective GABAA PAMs as safe and novel analgesics for pain management."

Journal • Preclinical • Alzheimer's Disease • Anesthesia • Cognitive Disorders • Neuralgia • Pain

Antinociceptive effects of α /α -selective GABA receptor positive allosteric modulators on opioid-induced hyperalgesia. (PubMed, FASEB J) - "This study systematically examined the antinociceptive effects of α /α -selective GABA receptor PAMs alone and in combination with acetaminophen in an OIH rat model wherein repeated treatment with the opioid fentanyl induces mechanical hyperalgesia...Duration of actions of α /α -selective GABA receptor PAMs (KRM-II-81, NS16085, HZ-166) alone were studied, and combinations of KRM-II-81 and acetaminophen were also studied at fixed ratios (1:1, 1:3, 3:1)...Furthermore, KRM-II-81/acetaminophen combinations produced additive to supra-additive interactions depending on the drug mixture ratios. These findings support the idea that α /α -selective GABA receptor PAMs could serve as novel analgesics for treating OIH, and may interact favorably with other non-opioid analgesics."

Journal • Immunology • Neuralgia • Pain

Antinociceptive effects of α 2 /α 3 -selective GABA A receptor positive allosteric modulators on opioid-induced hyperalgesia (Neuroscience 2021) - "This study systematically examined the antinociceptive effects of α 2 /α 3 -selective GABA A receptor PAMs alone and in combination with acetaminophen in an OIH rat model wherein repeated treatment with the opioid fentanyl induces mechanical hyperalgesia...Duration of actions of α 2 /α 3 -selective GABA A receptor PAMs (KRM-II-81, NS16085, HZ-166) alone were studied, and combinations of KRM-II-81 and acetaminophen were also studied at fixed ratios (1:1, 1:3, 3:1)...Furthermore, KRM-II-81/acetaminophen combinations produced additive to supra-additive interactions depending on the drug mixture ratios. These findings support the idea that α 2 /α 3 -selective GABA A receptor PAMs could serve as novel analgesics for treating OIH, and may interact favorably with other non-opioid analgesics.; Grant Support: NIH Grant DA047967"

CNS Disorders • Neuralgia • Pain