OPC-14523 dihydrochloride

OPC-14523 dihydrochloride is the dihydrochloride form of the free base OPC-14523. OPC-14523 dihydrochloride is an orally active dual agonist of sigma receptors and 5-HT₁A receptors that also inhibits the 5-HT transporter, with IC₅₀ values of 47/56 nM for sigma receptors σ1/2, 5-HT₁A receptor IC₅₀ = 2.3 nM, and 5-HT transporter IC₅₀ = 80 nM. OPC-14523 dihydrochloride exhibits antidepressant-like activity. OPC-14523 dihydrochloride can be used in neuroscience research, including studies on antidepressants and neuroprotection.

5-HT1A receptor:2.3 nM, σ1 receptor:47 nM, σ2 receptor:56 nM

Methods: To investigate the effects of OPC-14523 dihydrochloride on 5-HT biosynthesis, ICR mice were administered OPC-14523 dihydrochloride orally (0.3–10 mg/kg). The mice were sacrificed 1 hour after dosing, and 5-HTP accumulation was measured by HPLC.
Results: OPC-14523 dihydrochloride at doses ≥3 mg/kg significantly inhibited 5-HT synthesis. [1]
Methods: To investigate the antidepressant effects of OPC-14523 dihydrochloride, Wistar rats underwent a forced swimming test. Rats were administered OPC-14523 dihydrochloride orally for 1, 2, 4, and 7 consecutive days at doses of 1–100 mg/kg, with testing conducted 1 hour after the final dose.
Results: The ED₅₀ for a single dose was 27 mg/kg; after 7 days, the ED₅₀ was 18 mg/kg. OPC-14523 dihydrochloride demonstrated significant antidepressant effects.[1]