| Identification | Back Directory | [Name]
4H-1-Benzothiopyran-4-one, 2,3-dihydro-2-[1-(phenylMethyl)-4-piperidinyl]- | [CAS]
1204401-49-9 | [Synonyms]
WQ 1
σ1 Receptor antagonist-1
2-(1-Benzylpiperidin-4-yl)thiochroman-4-one
2-(1-Benzylpiperidin-4-yl)-2,3-dihydro-4H-thiochromen-4-one
4H-1-Benzothiopyran-4-one, 2,3-dihydro-2-[1-(phenylMethyl)-4-piperidinyl]-
anti-nociceptive,Sigma Receptor,cycle,σ1 Receptor antagonist1,σ1 Receptor antagonist 1,MCF-7,ADR,inhibit,phase,σ1 Receptor antagonist-1,Inhibitor,cells | [Molecular Formula]
C21H23NOS | [MDL Number]
MFCD18206882 | [MOL File]
1204401-49-9.mol | [Molecular Weight]
337.48 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (296.31 mM; Need ultrasonic) | [form ]
Solid | [color ]
Light yellow to light brown |
| Hazard Information | Back Directory | [Uses]
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1]. | [in vivo]
Pretreatment withσ1 Receptor antagonist-1 (compound 9;1 mg/kg; s.c.) significantly increases the anti-nociceptive effect produces by morphine over the entire time course starting at 60 min[1]. | Animal Model: | Male CD-1 mice[1] | | Dosage: | 1 mg/kg | | Administration: | S.c. | | Result: | Significantly increased the anti-nociceptive effect produced by morphine over the entire time course starting at 60 min.
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| [IC 50]
Sigma 1 Receptor | [storage]
Store at -20°C | [References]
[1] Piergentili A, et al. Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. J Med Chem. 2010;53(3):1261-1269. DOI:10.1021/jm901542q |
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