We have:
• First-in-class positive allosteric modulators (PAMs) highly selective to the α6 subunit-containing GABAA receptors (α6GABAARs).
• Proof of Concept in animal models for
• Migraine2
• Orofacial pain3,4
• Temporomandibular joint (TMJ) pain5
• Mode of action
• Enhancing α6GABAAR-mediated inhibition in trigeminal ganglia.
• Non-opioid mechanism for pain relief.
• Effective for both prophylaxis and abortion of migraine.
• Silent at the BDZ sites: no sedative, addictive, motor-impairing activity.