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SB 206553 hydrochloride

Potent, selective 5-HT2C/5-HT2B antagonist. Orally active CAS# 1197334-04-5

SB 206553 hydrochloride

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Chemical structure

SB 206553 hydrochloride

3D structure

Chemical Properties of SB 206553 hydrochloride

Cas No. 1197334-04-5 SDF Download SDF
PubChem ID 11957707 Appearance Powder
Formula C17H17ClN4O M.Wt 328.8
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 1-methyl-N-pyridin-3-yl-6,7-dihydropyrrolo[2,3-f]indole-5-carboxamide;hydrochloride
SMILES CN1C=CC2=CC3=C(CCN3C(=O)NC4=CN=CC=C4)C=C21.Cl
Standard InChIKey VGEMBOFBPSNOIO-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H16N4O.ClH/c1-20-7-4-12-10-16-13(9-15(12)20)5-8-21(16)17(22)19-14-3-2-6-18-11-14;/h2-4,6-7,9-11H,5,8H2,1H3,(H,19,22);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.

SB 206553 hydrochloride Dilution Calculator

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SB 206553 hydrochloride Molarity Calculator

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Preparing Stock Solutions of SB 206553 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0414 mL 15.2068 mL 30.4136 mL 60.8273 mL 76.0341 mL
5 mM 0.6083 mL 3.0414 mL 6.0827 mL 12.1655 mL 15.2068 mL
10 mM 0.3041 mL 1.5207 mL 3.0414 mL 6.0827 mL 7.6034 mL
50 mM 0.0608 mL 0.3041 mL 0.6083 mL 1.2165 mL 1.5207 mL
100 mM 0.0304 mL 0.1521 mL 0.3041 mL 0.6083 mL 0.7603 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 206553 hydrochloride

5-HT2A and 5-HT2C/2B receptor subtypes modulate dopamine release induced in vivo by amphetamine and morphine in both the rat nucleus accumbens and striatum.[Pubmed:11850146]

Neuropsychopharmacology. 2002 Mar;26(3):311-24.

In vivo microdialysis and single-cell extracellular recordings were used to assess the involvement of serotonin(2A) (5-HT(2A)) and serotonin(2C/2B) (5-HT(2C/2B)) receptors in the effects induced by amphetamine and morphine on dopaminergic (DA) activity within the mesoaccumbal and nigrostriatal pathways. The increase in DA release induced by amphetamine (2 mg/kg i.p.) in the nucleus accumbens and striatum was significantly reduced by the selective 5-HT(2A) antagonist SR 46349B (0.5 mg/kg s.c.), but not affected by the 5-HT(2C/2B) antagonist SB 206553 (5 mg/kg i.p.). In contrast, the enhancement of accumbal and striatal DA output induced by morphine (2.5 mg/kg s.c.), while insensitive to SR 46349B, was significantly increased by SB 206553. Furthermore, morphine (0.1-10 mg/kg i.v.)-induced increase in DA neuron firing rate in both the ventral tegmental area and the substantia nigra pars compacta was unaffected by SR 46349B (0.1 mg/kg i.v.) but significantly potentiated by SB 206553 (0.1 mg/kg i.v.). These results show that 5-HT(2A) and 5-HT(2C) receptors regulate specifically the activation of midbrain DA neurons induced by amphetamine and morphine, respectively. This differential contribution may be related to the specific mechanism of action of the drug considered and to the neuronal circuitry involved in their effect on DA neurons. Furthermore, these results suggest that 5-HT(2C) receptors selectively modulate the impulse flow-dependent release of DA.

In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.[Pubmed:8821530]

Br J Pharmacol. 1996 Feb;117(3):427-434.

1. SB 206553 (5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2 ,3-f]indole) displays a high affinity (pK1 7.9) for the cloned human 5-HT2C receptor expressed in HEK 293 cells and the 5-HT2B receptor (pA2 8.9) as measured in the rat stomach fundus preparation. SB 206553 has low affinity for cloned human 5-HT2A receptors expressed in HEK 293 cells (pK1 5.8) and (pK1 < 6) for a wide variety of other neurotransmitter receptors. 2. SB 206553 appears to be a surmountable antagonist of 5-HT-stimulated phosphoinositide hydrolysis in HEK 293 cells expressing the human 5-HT2C receptor (pKB 9.0). 3. The compound potently (ID50 5.5 mg kg-1, p.o., 0.27 mg kg-1, i.v.) inhibited the hypolocomotor response to m-chlorophenylpiperazine (mCPP), a putative model of 5-HT2C/5-HT2B receptor function in vivo. 4. At similar doses (2-20 mg kg-1, p.o.) SB 206553 increased total interaction scores in a rat social interaction test and increased punished responding in a rat Geller-Seifter conflict test. These effects are consistent with the possession of anxiolytic properties. 5. SB 206553 also increased suppressed responding in a marmoset conflict model of anxiety at somewhat higher doses (15 and 20 mg kg-1, p.o.) but also reduced unsuppressed responding. 6. These results suggest that SB 206553 is a potent mixed 5-HT2C/5-HT2B receptor antagonist with selectivity over the 5-HT2A and all other sites studied and possesses anxiolytic-like properties.

5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity.[Pubmed:7629791]

J Med Chem. 1995 Jul 7;38(14):2524-30.

The preparation of a series of conformationally restricted analogues of indolylurea 1, namely tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described. The binding affinities of these compounds at 5-HT2A, 5-HT2B, and 5-HT2C receptors were determined. Of these compounds, the 1,2,3,5-tetrahydropyrrolo[2,3-f]indole derivative, compound 11, was found to have high affinity for the 5-HT2C (pKI 8.0) and 5-HT2B receptors (pA2 8.5), with excellent selectivity over the 5-HT2A and various other receptors (pKI < 6). 11 is also considerably more active than 1 in both an in vitro functional model, 5-HT-stimulated phosphoinositol hydrolysis (pKB 8.8), and an in vivo functional model, mCPP-induced hypolocomotion (ID50 5.5 mg/kg po). 11 should therefore be of significant utility as a pharmacological tool to delineate the functional significance of blockade of 5-HT2B and 5-HT2C receptors.

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