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Rimcazole (BW 234U) is a small molecule carbazole derivative that acts as a sigma receptor antagonist and dopamine reuptake inhibitor. Developed by Wellcome Research Laboratories (now part of GSK) in the 1980s, it was initially investigated as a novel antipsychotic for the treatment of schizophrenia. The drug was hypothesized to offer a better side-effect profile than traditional antipsychotics by targeting sigma receptors rather than primarily dopamine D2 receptors. However, clinical trials failed to demonstrate sufficient efficacy in patients with schizophrenia, leading to the termination of its development for this indication. Rimcazole also binds to the dopamine transporter (DAT) and has been studied for its potential to attenuate the reinforcing effects of cocaine. It is currently utilized primarily as a pharmacological research tool and as a lead compound for the development of novel dopamine transporter ligands.
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