Bioactivity | Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer[1][2][3][4]. |
Target | sigma (σ) receptordopamine transporter |
Invitro | Rimcazole (1-50 μM; 24-48 h) concentration-dependently decreases the number HCT-116p53+/+ cells[2].Rimcazole (50 μM; 1-24 h) dihydrochloride induces a transient accumulation of HIF-1α protei in cancer cells (HCT-116p53+/+ and MDA MB 231 cells) but not in normal human dermal fibroblasts[2]. Western Blot Analysis[2] Cell Line: |
Name | Rimcazole dihydrochloride |
CAS | 75859-03-9 |
Formula | C21H29Cl2N3 |
Molar Mass | 394.38 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
Reference | [1]. Gilmore DL, et, al. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Rev. Spring 2004;10(1):1-22. [2]. Achison M, et, al. HIF-1alpha contributes to tumour-selective killing by the sigma receptor antagonist rimcazole. Oncogene. 2007 Feb 22;26(8):1137-46. [3]. Matsumoto RR, et, al. Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology. 2001 Dec;41(7):878-86. [4]. Job MO, et, al. A behavioral economic analysis of the effects of rimcazole on reinforcing effects of cocaine injection and food presentation in rats. Psychopharmacology (Berl). 2019 Dec;236(12):3601-3612. |