OPC-14523 free base
Names
[ CAS No. ]:
145969-30-8
[ Name ]:
OPC-14523 free base
[Synonym ]:
1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2(1H)-quinolone
5-methoxy-1-{3-[4-(3-chlorophenyl)-1-piperazinyl]propyl}-3,4-dihydrocarbostyril
Biological Activity
[Description]:
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity[1][2].
[Related Catalog]:
[Target]
5-HT1A Receptor:2.3 nM (IC50)
sigma 1:47 nM (IC50)
sigma 2:56 nM (IC50)
[In Vivo]
OPC-14523 free base (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity[1]. Animal Model: Wistar strain of rats (140-245 g)[1] Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single doses of 1 mg/kg and higher of OPC-14523 reduced immobility time in the FST with an ED50 value of 27 mg/kg. The ED50 value for OPC-14523 on day 7 was 18 mg/kg. Animal Model: ICR strain of mice (25-45 g)[1] Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single oral dose of OPC-14523 produced a marked reduction in immobility time during the FST at oral doses of 1 mg/kg and higher, with an ED50 value of 20 mg/kg. The potency of OPC-14523 in decreasing immobility time was greater after treatment for seven consecutive days, producing an ED50 value of 2 mg/kg.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C23H28ClN3O2
[ Molecular Weight ]:
413.94000
[ Exact Mass ]:
413.18700
[ PSA ]:
36.02000
[ LogP ]:
3.90800