Rimcazole: Difference between revisions

'''Rimcazole''' is an [[Receptor antagonist|antagonist]]<ref>Gilmore DL, Liu Y, Matsumoto RR. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Reviews. ~~2004~~ ~~Spring;~~10~~(1):~~1-22.</ref> of the [[sigma receptor]].<ref>{{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=10.1016/0006-8993(96)00290-9}}</ref> Sigma receptors are thought to be involved in the drug [[psychosis]] that can be induced by some drugs such as [[~~Phencyclidine|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.<ref> Volz HP, Stoll KD. Clinical trials with sigma ligands. Pharmacopsychiatry. ~~2004~~ ~~Nov;~~37 Suppl 3~~:S214-20~~. </ref> Rimcazole has been shown to reduce the effects of cocaine,<ref>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.~~</ref> and analogues of rimcazole have been shown to be highly effective at blocking the [[convulsions]] caused by cocaine [[overdose]] in animal models.<ref>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.~~</ref>

'''Rimcazole''' is an [[Receptor antagonist|antagonist]]<ref name="Gilmore_2004">{{cite journal | vauthors = Gilmore DL, Liu Y, Matsumoto RR | title = Review of the pharmacological and clinical profile of rimcazole | journal = CNS Drug Reviews | volume = 10 | issue = 1 | pages = 1–22 | date = 2004 | pmid = 14978511 | pmc = 6741722 | doi = 10.1111/j.1527-3458.2004.tb00001.x }}</ref> of the [[sigma receptor]]<ref>{{cite journal | vauthors = 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 Research | volume = 733 | issue = 2 | pages = 162–166 | date = September 1996 | pmid = 8891298 | doi = 10.1016/0006-8993(96)00290-9 | s2cid = 42885767 }}</ref> as well as a [[dopamine reuptake inhibitor]].<ref>{{cite journal | vauthors = Husbands SM, Izenwasser S, Loeloff RJ, Katz JL, Bowen WD, Vilner BJ, Newman AH | title = Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter | journal = Journal of Medicinal Chemistry | volume = 40 | issue = 26 | pages = 4340–4346 | date = December 1997 | pmid = 9435903 | doi = 10.1021/jm9705519 }}</ref> 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.<ref name="pmid15547788">{{cite journal | vauthors = Volz HP, Stoll KD | title = Clinical trials with sigma ligands | journal = Pharmacopsychiatry | volume = 37 | issue = Suppl 3| pages = S214–S220 | date = November 2004 | pmid = 15547788 | doi = 10.1055/s-2004-832680 | s2cid = 260238757 }}</ref> Rimcazole has been shown to reduce the effects of cocaine,<ref name="pmid12742518">{{cite journal | vauthors = Katz JL, Libby TA, Kopajtic T, Husbands SM, Newman AH | title = Behavioral effects of rimcazole analogues alone and in combination with cocaine | journal = European Journal of Pharmacology | volume = 468 | issue = 2 | pages = 109–119 | date = May 2003 | pmid = 12742518 | doi = 10.1016/s0014-2999(03)01638-8 }}</ref> and analogues of rimcazole have been shown to be highly effective at blocking the [[convulsions]] caused by cocaine [[overdose]] in animal models.<ref name="pmid11684152">{{cite journal | vauthors = Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Newman AH | title = Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters | journal = Neuropharmacology | volume = 41 | issue = 7 | pages = 878–886 | date = December 2001 | pmid = 11684152 | doi = 10.1016/s0028-3908(01)00116-2 | s2cid = 44328858 }}</ref>

==References==

== References ==

[[Category:Piperazines]]

[[Category:Carbazoles]]

[[Category:Dopamine reuptake inhibitors]]

[[Category:Sigma antagonists]]

[[Category:Anticonvulsants]]