Name | 2-(1-Benzyl-4-piperidinyl)-2,3-dihydro-4H-thiochromen-4-one |
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Description | 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]. |
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Related Catalog | |
In Vitro | σ1 Receptor antagonist-1 (compound 9) (10 μM; 48 hours) inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1]. Cell Cycle Analysis[1] Cell Line: MCF-7/ADR, MCF-7 cells Concentration: 10 μM Incubation Time: 48 hours Result: Increased the number of cells in G0/G1 (27.8%) and decreased those in S phase (46.7%), in a sigma 1-dependent manner. It selectively affects the high sigma 1 receptor expressing MCF-7/ADR but not the low sigma 1 receptor expressing MCF-7 cells. |
In Vivo | Pretreatment withσ1 Receptor antagonist-1 (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. |
References |
Molecular Formula | C21H23NOS |
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Molecular Weight | 337.47800 |
Exact Mass | 337.15000 |
PSA | 45.61000 |
LogP | 4.58380 |
HS Code | 2934999090 |
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~74% 1204401-49-9 |
Literature: Piergentili, Alessandro; Amantini, Consuelo; Del Bello, Fabio; Giannella, Mario; Mattioli, Laura; Palmery, Maura; Perfumi, Marina; Pigini, Maria; Santoni, Giorgio; Tucci, Paolo; Zotti, Margherita; Quaglia, Wilma Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1261 - 1269 |
Precursor 2 | |
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DownStream 0 |
HS Code | 2934999090 |
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Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |