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Submit ReviewRimcazole dihydrochloride is an 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.
分子量 | 394.39 |
公式 | C21H27N3.2HCl |
储存 | Store at +4°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 3.94 | 10 |
以下数据基于产品分子量 394.39。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 25.36 mL | 126.78 mL | 253.56 mL |
0.5 mM | 5.07 mL | 25.36 mL | 50.71 mL |
1 mM | 2.54 mL | 12.68 mL | 25.36 mL |
5 mM | 0.51 mL | 2.54 mL | 5.07 mL |
参考文献是支持产品生物活性的出版物。
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 DA 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 DA transporters. Neuropharmacology 41 878 PMID: 11684152
If you know of a relevant reference for Rimcazole dihydrochloride, please let us know.
关键词: Rimcazole dihydrochloride, Rimcazole dihydrochloride supplier, σ2, sigma2, antagonists, DAT, reuptake, inhibitors, inhibits, Receptors, Dopamine, Transporters, Monoamine, Neurotransmitter, BW234U, BW, 234U, Sigma2, 1497, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Rimcazole dihydrochloride 的部分引用包括:
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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