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SB 258585 hydrochloride

Potent, selective 5-HT6 antagonist CAS# 1216468-02-8

SB 258585 hydrochloride

Catalog No. BCC7216----Order now to get a substantial discount!

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Chemical structure

SB 258585 hydrochloride

3D structure

Chemical Properties of SB 258585 hydrochloride

Cas No. 1216468-02-8 SDF Download SDF
PubChem ID 53429667 Appearance Powder
Formula C18H23ClIN3O3S M.Wt 523.82
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in water and to 50 mM in DMSO
Chemical Name 4-iodo-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamide;hydrochloride
SMILES CN1CCN(CC1)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)I)OC.Cl
Standard InChIKey BFGOZFXMAJBFGI-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H22IN3O3S.ClH/c1-21-9-11-22(12-10-21)17-13-15(5-8-18(17)25-2)20-26(23,24)16-6-3-14(19)4-7-16;/h3-8,13,20H,9-12H2,1-2H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SB 258585 hydrochloride

DescriptionPotent and selective 5-HT6 receptor antagonist (pKi = 8.6); displays > 160-fold selectivity over other 5-HT receptor subtypes.

SB 258585 hydrochloride Dilution Calculator

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SB 258585 hydrochloride Molarity Calculator

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Preparing Stock Solutions of SB 258585 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9091 mL 9.5453 mL 19.0905 mL 38.1811 mL 47.7263 mL
5 mM 0.3818 mL 1.9091 mL 3.8181 mL 7.6362 mL 9.5453 mL
10 mM 0.1909 mL 0.9545 mL 1.9091 mL 3.8181 mL 4.7726 mL
50 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.7636 mL 0.9545 mL
100 mM 0.0191 mL 0.0955 mL 0.1909 mL 0.3818 mL 0.4773 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SB 258585 hydrochloride

5-HT6 receptor binding sites in schizophrenia and following antipsychotic drug administration: autoradiographic studies with [125I]SB-258585.[Pubmed:12112397]

Synapse. 2002 Sep 1;45(3):191-9.

The 5-hydroxytryptamine (5-HT; serotonin)-6 receptor (5-HT6R) is a putative target of atypical antipsychotic drugs and its mRNA expression is altered in schizophrenia. [125I]SB-258585 is a selective 5-HT6R antagonist which has been well characterized for use in the rat brain. The present study evaluated its suitability for receptor autoradiography in the human brain and its application to quantitative studies. The affinity (K(d) approximately 1.2 nM) and relative distribution of binding sites (striatum >> cortex approximately hippocampus) were similar to the rat. The distribution of [125I]SB-258585 binding in these regions was also consistent with that of 5-HT6R mRNA, determined in parallel using in situ hybridization. [125I]SB-258585 binding site densities were measured in dorsolateral prefrontal cortex of 20 patients with chronic schizophrenia and compared with 17 normal subjects. No differences were seen between groups. Neither were [125I]SB-258585 binding site densities affected in the frontal cortex or striatum of rats following 2 weeks' administration of the antipsychotic drugs haloperidol, chlorpromazine, olanzapine, risperidone, or clozapine. In summary, [125I]SB-258585 is a suitable radioligand for studies of human brain 5-HT6R binding sites and shows that their distribution is broadly similar to that of the rodent. The lack of effect of schizophrenia or antipsychotic drug administration on [125I]SB-258585 binding suggests that an altered receptor density does not contribute to any involvement which the 5-HT6R may have in the disease or its treatment.

Characterization of [(125)I]-SB-258585 binding to human recombinant and native 5-HT(6) receptors in rat, pig and human brain tissue.[Pubmed:10928963]

Br J Pharmacol. 2000 Aug;130(7):1597-605.

SB-258585 (4-Iodo-N-[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-benzen esulphonamide) is a high affinity ligand at 5-HT(6) receptors. It displays over 100 fold selectivity for the 5-HT(6) receptor over all other 5-HT receptors tested so far. SB-258585 has been radiolabelled, to high specific activity, for its characterization as a 5-HT(6) receptor selective radioligand. [(125)I]-SB-258585 bound, with high affinity, to a single population of receptors in a cell line expressing human recombinant 5-HT(6) receptors. Kinetic and saturation binding experiments gave pK(D) values of 9.01+/-0.09 and 9.09+/-0.02, respectively. In membranes derived from rat or pig striatum and human caudate putamen, [(125)I]-SB-258585 labelled a single site with high levels (>60%) of specific binding. Saturation analysis revealed pK(D) values of 8.56+/-0.07 for rat, 8.60+/-0.10 for pig and 8.90+/-0.02 for human. B(max) values for the tissues ranged from 173+/-23 and 181+/-25 fmol mg(-1) protein in rat and pig striatum, respectively, to 215+/-41 fmol mg(-1) protein in human caudate putamen. The pK(i) rank order of potency for a number of compounds, determined in competition binding assays with [(125)I]-SB-258585, at human caudate putamen membranes was: SB-271046>SB-258585>SB-214111>methiothepin>clozapine>5-Me-OT>5-HT>Ro 04-6790>mianserin>ritanserin=amitriptyline>5-CT>mesulergine. Similar profiles were obtained from pig and rat striatal membranes and recombinant 5-HT(6) receptors; data from the latter correlated well with [(3)H]-LSD binding. Thus, [(125)I]-SB-258585 is a high affinity, selective radioligand which can be used to label both recombinant and native 5-HT(6) receptors and will facilitate further characterization of this receptor subtype in animal and human tissues.

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