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Rimcazole is an antagonist of the sigma receptor as well as a dopamine reuptake inhibitor. Sigma receptors are thought to be involved in the drug psychosis that can be induced by some drugs such as phencyclidine and cocaine, and rimcazole was originally researched as a potential antipsychotic with a different mechanism of action to traditional antipsychotic drugs. Trials proved inconclusive and rimcazole was not pursued for this application, but other sigma antagonists continue to be researched for a variety of potential applications. Rimcazole has been shown to reduce the effects of cocaine, and analogues of rimcazole have been shown to be highly effective at blocking the convulsions caused by cocaine overdose in animal models.
- Gilmore DL, Liu Y, Matsumoto RR. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Reviews. 2004 Spring;10(1):1-22.
- Eaton MJ, Lookingland KJ, Moore KE (1996). "The sigma ligand rimcazole activates noradrenergic neurons projecting to the paraventricular nucleus and increases corticosterone secretion in rats". Brain Res. 733 (2): 162–6. doi:10.1016/0006-8993(96)00290-9. PMID 8891298.
- Husbands, S. M.; Izenwasser, S; Loeloff, R. J.; Katz, J. L.; Bowen, W. D.; Vilner, B. J.; Newman, A. H. (1997). "Isothiocyanate derivatives of 9-3-(cis-3,5-dimethyl-1-piperazinyl)propylcarbazole (rimcazole): Irreversible ligands for the dopamine transporter". Journal of Medicinal Chemistry 40 (26): 4340–46. doi:10.1021/jm9705519. PMID 9435903.
- Volz HP, Stoll KD. Clinical trials with sigma ligands. Pharmacopsychiatry. 2004 Nov;37 Suppl 3:S214-20.
- Katz JL, Libby TA, Kopajtic T, Husbands SM, Newman AH. Behavioral effects of rimcazole analogues alone and in combination with cocaine. European Journal of Pharmacology. 2003 May 9;468(2):109-19.
- Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Hauck Newman A. 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.
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