The novel σ-receptor ligands eurotransmitter antagonists.

TargetValue σ1R (Cell-free assay) 4.43 nM(Ki)

BD1063 dose-dependently reduces ethanol self-administration in sP rats (3.3-11 mg/kg) and withdrawn, dependent Wistar rats (4-11 mg/kg) at doses that does not modify mean ethanol self-administration in non-dependent Wistar controls. BD1063 also reduces the breakpoints of sP rats to work for ethanol under a progressive-ratio reinforcement schedule. BD1063 dose-dependently reduces binge-like eating and the regularity of food responding, and blocks the increased eating rate in Palatable rats. In the light/dark conflict test, BD1063 antagonizes the increased time spent in the aversive compartment and the increased intake of the palatable diet, without affecting motor activity. The administration of BD1063 30 minutes before each paclitaxel dose prevents the development of cold and mechanical allodynia in WT mice. Moreover, the acute administration of BD1063 dose dependently reverses both types of paclitaxel-induced allodynia.

BD1063 2HCL (BD1063 dihydrochloride)是一种有效的选择性 sigma-1 receptor (σ1R) 拮抗剂，对应的Ki值为4.43 nM。