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.
Technical Data
| M. Wt | 394.39 |
| Formula | C21H27N3.2HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 75859-03-9 |
| PubChem ID | 53388 |
| InChI Key | ZWHRZGHGYMUSRM-VWDRLOGHSA-N |
| Smiles | C[C@H](N[C@H](C)C4)CN4CCCN1C3=C(C=CC=C3)C2=C1C=CC=C2.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 39.44 | 100 | |
| water | 3.94 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 394.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.54 mL | 12.68 mL | 25.36 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.07 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ferris et 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 PMID: 2873494
Husbands et 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 PMID: 9435903
Matsumoto et al (2001) Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology 41 878 PMID: 11684152
Keywords: Rimcazole dihydrochloride, supplier, σ2, sigma2, antagonists, DAT, reuptake, inhibitors, inhibits, Receptors, Dopamine, Transporters, Monoamine, Neurotransmitter, BW234U, BW, 234U, Sigma2, Receptors, Dopamine, Transporters, Sigma2, Receptors, Tocris Bioscience
