Description
ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11beta-HSD1 with Ki of 5.3, 2.6 and 23nM for human, mouse and rat 11beta-HSD1, does not inhibit human 11beta-HSD2 at 30uM; demonstrates no appreciable binding affinity to or inhibition against 87 off-targets (adenosine receptors, adrenergic receptors, angiotensin receptors, calcium channels, 5-HT receptors etc.); inhibits the in vitro conversion of glucocorticoid from its inactive to active form in the brain and spinal cord; ameliorates mechanical allodynia in spinal nerve ligation (SNL) and streptozotocin-induced diabetic rats and thermal hyperalgesia in chronic constriction nerve injury rats. Alzheimer Disease Phase 2 Discontinued