Rimcazole

Drugbox
IUPAC_name = 9- [3- [(3S,5R) -3,5-dimethylpiperazin-1-yl] propyl] carbazole


width = 140
CAS_number=75859-04-0
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PubChem=53389
DrugBank=
C=21 | H=27 | N=3
molecular_weight = 321.459
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Rimcazole is an antagonist [Gilmore DL, Liu Y, Matsumoto RR. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Reviews. 2004 Spring;10(1):1-22.] of the sigma receptor. [cite journal |author=Eaton MJ, Lookingland KJ, Moore KE |title=The sigma ligand rimcazole activates noradrenergic neurons projecting to the paraventricular nucleus and increases corticosterone secretion in rats |journal=Brain Res. |volume=733 |issue=2 |pages=162–6 |year=1996 |pmid=8891298 |doi=] Sigma receptors are thought to be involved in the drug psychosis that can be induced by some drugs such as PCP 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. [ Volz HP, Stoll KD. Clinical trials with sigma ligands. Pharmacopsychiatry. 2004 Nov;37 Suppl 3:S214-20. ] Rimcazole has been shown to reduce the effects of cocaine, [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.] and analogues of rimcazole have been shown to be highly effective at blocking the convulsions caused by cocaine overdose in animal models. [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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