Rimcazole
 | |
| Clinical data | |
|---|---|
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| Chemical and physical data | |
| Formula | C21H27N3 |
| Molar mass | 321.468g·mol−1 |
| 3D model (JSmol) | |
| |
| |
  (what is this?)(verify) | |
Rimcazoleis anantagonist[1]of thesigma receptor[2]as well as adopamine reuptake inhibitor.[3]Sigma receptors are thought to be involved in the drugpsychosisthat can be induced by some drugs such asphencyclidineandcocaine,and rimcazole was originally researched as a potentialantipsychoticwith 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 theconvulsionscaused by cocaineoverdosein animal models.[6]
References
[edit]- ^Gilmore DL, Liu Y, Matsumoto RR (2004)."Review of the pharmacological and clinical profile of rimcazole".CNS Drug Reviews.10(1): 1–22.doi:10.1111/j.1527-3458.2004.tb00001.x.PMC6741722.PMID14978511.
- ^Eaton MJ, Lookingland KJ, Moore KE (September 1996). "The sigma ligand rimcazole activates noradrenergic neurons projecting to the paraventricular nucleus and increases corticosterone secretion in rats".Brain Research.733(2): 162–166.doi:10.1016/0006-8993(96)00290-9.PMID8891298.S2CID42885767.
- ^Husbands SM, Izenwasser S, Loeloff RJ, Katz JL, Bowen WD, Vilner BJ, Newman AH (December 1997). "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.doi:10.1021/jm9705519.PMID9435903.
- ^Volz HP, Stoll KD (November 2004). "Clinical trials with sigma ligands".Pharmacopsychiatry.37(Suppl 3): S214–S220.doi:10.1055/s-2004-832680.PMID15547788.S2CID260238757.
- ^Katz JL, Libby TA, Kopajtic T, Husbands SM, Newman AH (May 2003). "Behavioral effects of rimcazole analogues alone and in combination with cocaine".European Journal of Pharmacology.468(2): 109–119.doi:10.1016/s0014-2999(03)01638-8.PMID12742518.
- ^Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Newman AH (December 2001). "Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters".Neuropharmacology.41(7): 878–886.doi:10.1016/s0028-3908(01)00116-2.PMID11684152.S2CID44328858.
 | Thisdrugarticle relating to thenervous systemis astub.You can help Wikipedia byexpanding it. |