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Journal: Inhibition of Nav1.7 channel by a novel blocker QLS-81 for alleviation of neuropathic pain. (Pubmed Central) - Nov 4, 2021
Ralfinamide has shown anti-nociceptive activity in animal models of inflammatory and neuropathic pain and is currently under phase III clinical trial for neuropathic pain...In addition, QLS-81 (10 μM) did not significantly affect ECG in guinea pig heart ex vivo; and administration of QLS-81 (10, 20 mg/kg, i.p.) in mice had no significant effect on spontaneous locomotor activity. Taken together, our results demonstrate that QLS-81, as a novel Nav1.7 inhibitor, is efficacious on chronic pain in mice, and it may hold developmental potential for pain therapy.
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Trial completion: Efficacy and Safety of Ralfinamide in Patients With Chronic Neuropathic Low Back Pain (clinicaltrials.gov) - Sep 15, 2017
P3, N=411, Completed,
Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Na targets, could serve as new leads for the development of analgesic medicines. Active, not recruiting --> Completed
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