DKR-1677 (DKR1677) is a potent, selective σ2R/TMEM97 modulator with Ki value of 5.1 nM, 45-fold selectivity over σ1R (Ki=230 nM).
DKR-1677 generally exhibits greater than 100-fold selectivity against a panel of more than 50 proteins relevant to the central nervous system (CNS), with the exception of histamine-1 (20-fold) and the alpha-2A adrenergic (68-fold) receptors.
DKR-1677 is neuroprotective after blast-induced and controlled cortical impact (CCI) TBI in mice.
DKR-1677 decreases axonal degeneration after blast-induced TBI and enhances survival of cortical neurons and oligodendrocytes after CCI injury.
DKR-1677 preserves cognition in the Morris water maze after blast TBI.
