Rimkazol

Rimkazol
(IUPAC) ime
	93-[(3R,5S)-3,5-dimethylpiperazin-1-yl]propyl9H-carbazole
Klinički podaci
Identifikatori
CAS broj	75859-04-0
ATC kod	nije dodeljen
PubChem	53389
Hemijski podaci
Formula	C21H27N3
Mol. masa	321.459
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C21H27N3/c1-16-14-23(15-17(2)22-16)12-7-13-24-20-10-5-3-8-18(20)19-9-4-6-11-21(19)24/h3-6,8-11,16-17,22H,7,12-15H2,1-2H3/t16-,17+ ; Key: GUDVQJXODNJRIJ-CALCHBBNSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Rimkazol je antagonist^[3] sigma receptora.^[4] Za sigma receptore se smatra da učestvuju u psihozi koja može da bude indukovana lekovima kao što su PCP i kokain. Rimkazol je originalno bio istraživan kao potencijalni antipsihotik sa različitim mehanizmom dejstva od tradicionalnih antipsihotičkih lekova. To nije u dovoljnoj meri potvrđeno kliničkim ispitivanjima tako da se rimkazol ne primenjuje za tu indikaciju.^[5]

Za rimkazol je utvrđeno da redukuje dejstvo kokaina,^[6] a za analoge rimkazola je pokazano da su veoma efektivni u blokiranju konvulzija uzrokovanih kokainskim predoziranjem u modelima na životinjama.^[7]

Literatura

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Gilmore DL, Liu Y, Matsumoto RR (2004). „Review of the pharmacological and clinical profile of rimcazole”. CNS Drug Reviews 10 (1): 1–22. PMID 14978511.
↑ 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.
↑ Volz HP, Stoll KD (November 2004). „Clinical trials with sigma ligands”. Pharmacopsychiatry 37 Suppl 3: S214–20. DOI:10.1055/s-2004-832680. PMID 15547788. Pristupljeno 2011-04-27. ^{[mrtav link]}
↑ 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): 109–19. PMID 12742518. Pristupljeno 2011-04-27.
↑ Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Hauck Newman A (December 2001). „Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters”. Neuropharmacology 41 (7): 878–86. PMID 11684152. Pristupljeno 2011-04-27.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Gilmore DL, Liu Y, Matsumoto RR (2004). „Review of the pharmacological and clinical profile of rimcazole”. CNS Drug Reviews 10 (1): 1–22. PMID 14978511.

[4] 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.

[5] Volz HP, Stoll KD (November 2004). „Clinical trials with sigma ligands”. Pharmacopsychiatry 37 Suppl 3: S214–20. DOI:10.1055/s-2004-832680. PMID 15547788. Pristupljeno 2011-04-27. ^{[mrtav link]}

[pmid12742518-6] 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): 109–19. PMID 12742518. Pristupljeno 2011-04-27.

[pmid11684152-7] Matsumoto RR, Hewett KL, Pouw B, Bowen WD, Husbands SM, Cao JJ, Hauck Newman A (December 2001). „Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters”. Neuropharmacology 41 (7): 878–86. PMID 11684152. Pristupljeno 2011-04-27.

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