4-IODO-N-[4-METHOXY-3-(4-METHYL-1-PIPERAZINYL)PHENYL]BENZENESULFONAMIDE HYDROCHLORIDE

4-IODO-N-[4-METHOXY-3-(4-METHYL-1-PIPERAZINYL)PHENYL]BENZENESULFONAMIDE HYDROCHLORIDE Property

storage temp. 

2-8°C

solubility 

DMF: 15 mg/mL
DMSO: 20 mg/mL
Ethanol: 0.25 mg/mLPBS (pH 7.2): 10 mg/mL

form 

solid

color 

off-white

Safety

Hazard Codes 

Xn

Risk Statements 

36/37/38-42/43

Safety Statements 

26-36/37-45

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

4-IODO-N-[4-METHOXY-3-(4-METHYL-1-PIPERAZINYL)PHENYL]BENZENESULFONAMIDE HYDROCHLORIDE Chemical Properties,Usage,Production

Uses

SB 258585 is a selective and potent SR-6 and 5-HT6R antagonist.

Biological Activity

Potent and selective 5-HT 6 receptor antagonist (pK i = 8.6); displays > 160-fold selectivity over other 5-HT receptor subtypes.

References

[1] WARREN D HIRST. Characterization of [125I]-SB-258585 binding to human recombinant and native 5-HT6 receptors in rat, pig and human brain tissue[J]. British Journal of Pharmacology, 2009, 130 7: 1597-1605. DOI: 10.1038/sj.bjp.0703458
[2] CAROL ROUTLEDGE. Characterization of SB-271046: A potent, selective and orally active 5-HT6 receptor antagonist[J]. British Journal of Pharmacology, 2009, 130 7: 1606-1612. DOI: 10.1038/sj.bjp.0703457
[3] AYAKA TATARA. Modulation of antipsychotic-induced extrapyramidal side effects by medications for mood disorders[J]. Progress in Neuro-Psychopharmacology & Biological Psychiatry, 2012, 38 2: Pages 252-259. DOI: 10.1016/j.pnpbp.2012.04.008
[4] FANNY DUHR. Cdk5 induces constitutive activation of 5-HT6 receptors to promote neurite growth[J]. Nature chemical biology, 2014, 10 7: 590-597. DOI: 10.1038/nchembio.1547
[5] SAKI SHIMIZU. Interaction between anti-Alzheimer and antipsychotic drugs in modulating extrapyramidal motor disorders in mice[J]. Journal of pharmacological sciences, 2015, 127 4: Pages 439-445. DOI: 10.1016/j.jphs.2015.03.004