Chemical Name:9-[3-(cis-3,5-Dimethyl-1-piperazinyl)propyl]-9H-carbazo
le dihydrochloride
Biological Activity:
Antagonist at σ receptors
(IC50 values are 1480 and 386 nM at σ1
and σ2
receptors respectively). Also binds to the dopamine transporter (IC50
= 57.6 nM) and inhibits dopamine uptake. Reduces the stimulatory effects of
cocaine in vivo.
Ferriset al (1986) Evidence that
the potential antipsychotic agent rimcazole (BW 234U) is a specific,
competitive antagonist of sigma sites in brain. Life Sci. 38
2329. Husbandset al (1997) Isothiocyanate derivatives of
9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]-carbazole (Rimcazole):
irreversible ligands for the dopamine transporter. J.Med.Chem. 40
4340. Matsumotoet al (2001) Rimcazole analogs attenuate the
convulsive effects of cocaine: correlation with binding to sigma receptors
rather than dopamine transporters. Neuropharmacology 41 878.
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