WQ 1

WQ 1 is an antagonist of sigma non-opioid intracellular receptor 1 (σ₁ receptor; K_i = 0.01 nM).¹ It is selective for the σ₁ receptor over the σ₂ receptor and dopamine transporter (DAT; K_is = 295.12 and 1,585 nM, respectively). WQ 1 (10 µM) decreases proliferation of MCF-7 breast cancer and MCF-7/adr multidrug-resistant breast cancer cells.² It induces cell cycle arrest at the G₀/G₁ phase in MCF-7 and MCF-7/adr cancer cells and apoptosis in MCF-7/adr cancer cells. WQ 1 (1 mg/kg) increases the duration of morphine-induced latency to tail withdrawal in the tail-flick test in mice when administered 30 minutes prior to the test. WQ 1 (3 or 7 mg/kg) reduces stress-induced food consumption in rats.¹

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1. Del Bello, F., Micioni Di Bonaventura, M.V., Bonifazi, A., et al. Investigation of the role of chirality in the interaction with σ receptors and effect on binge eating episode of a potent σ1 antagonist analogue of spipethiane. ACS Chem. Neurosci. 10(8), 3391-3397 (2019).

2. Piergentili, A., Amantini, C., Del Bello, F., et al. Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane. J. Med. Chem. 53(3), 1261-1269 (2010).