Unlike most subtype-selective modulators, NCT10001 potentiates certain GABAAR subtypes as strongly as diazepam. As a result, it is highly effective in animal models of epilepsy, pain and anxiety. Furthermore, NCT10001 does not potentiate the α1 or α5 subtypes. Therefore, it should not cause side effects commonly seen with non-selective benzodiazepines such as drowsiness, lethargy, dizziness, and cognitive dysfunction.
In preclinical studies, NCT10001 was superior or equivalent to diazepam (a commonly prescribed anticonvulsant) in multiple epilepsy models. It has a significantly wider margin of effect vs both motor-impairment and sedation than diazepam. This should translate to an effective treatment that has fewer and less severe side effects than existing therapies. Furthermore, we are uncovering evidence that our compound can treat refractory epilepsy, and unlike many treatments – tolerance to our compound does not develop.
NCT10001 demonstrates superiority to the first line therapeutic gabapentin in the rat spinal nerve ligation assay. This compound is also highly effective in the Complete Freund’s Adjuvant induced hyperalgesia model, and elicits nearly 100% of the maximum potential effect consistently over 12 days of dosing. Furthermore, NCT10001 outperforms tramadol (an opioid analgesic) in the formalin-induced allodynia model.