Potent, brain penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1; IC50 value 3.3 nM and 14 nM and 320 nM for the closely related BIKE and GAK enzymes, repsectively). LP-935509 is antinociceptive in multiple rat models of neuropathic pain, but not acute pain. The AAK1 inhibitor-induced antinociception and inhibition of spontaneous neural activity can be blocked by α2 adrenergic antagonists.

KEYWORDS: LP-935509 | supplier | AAK1 inhibitor | LP935509 | CAS [1454555-29-3] | AAK | neuropathic pain | adapter protein-2 | AP-2 | antinociceptive | nociception | SNF1 family | endocytosis | clathrin | Notch