Chemistry:Rimcazole
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| Formula | C21H27N3 |
| Molar mass | 321.459 g·mol−1 |
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Rimcazole is an antagonist[1] of the sigma receptor[2] as well as a dopamine reuptake inhibitor.[3] 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.[4] Rimcazole has been shown to reduce the effects of cocaine,[5] and analogues of rimcazole have been shown to be highly effective at blocking the convulsions caused by cocaine overdose in animal models.[6]
References
- ↑ "Review of the pharmacological and clinical profile of rimcazole". CNS Drug Reviews 10 (1): 1–22. 2004. doi:10.1111/j.1527-3458.2004.tb00001.x. PMID 14978511.
- ↑ "The sigma ligand rimcazole activates noradrenergic neurons projecting to the paraventricular nucleus and increases corticosterone secretion in rats". Brain Research 733 (2): 162–166. September 1996. doi:10.1016/0006-8993(96)00290-9. PMID 8891298.
- ↑ "Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter". Journal of Medicinal Chemistry 40 (26): 4340–4346. December 1997. doi:10.1021/jm9705519. PMID 9435903.
- ↑ "Clinical trials with sigma ligands". Pharmacopsychiatry 37 (Suppl 3): S214–S220. November 2004. doi:10.1055/s-2004-832680. PMID 15547788.
- ↑ "Behavioral effects of rimcazole analogues alone and in combination with cocaine". European Journal of Pharmacology 468 (2): 109–119. May 2003. doi:10.1016/s0014-2999(03)01638-8. PMID 12742518.
- ↑ "Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters". Neuropharmacology 41 (7): 878–886. December 2001. doi:10.1016/s0028-3908(01)00116-2. PMID 11684152.
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