2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB-215505

SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.

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SB-215505 Chemical Structure

SB-215505 Chemical Structure

CAS No. : 162100-15-4

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Based on 1 publication(s) in Google Scholar

SB-215505 Related Antibodies

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Description

SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively[1]. SB-215505 increases wakefulness and motor activity in rats[2].

IC50 & Target[1]

5-HT2B Receptor

8.3 (pKi)

5-HT2A Receptor

6.77 (pKi)

5-HT2C Receptor

7.66 (pKi)

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
13 nM
Compound: SB-215505
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
[PMID: 19307114]
CHO-K1 IC50
64 nM
Compound: SB-215505
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
[PMID: 19307114]
In Vitro

SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-215505 Related Antibodies
In Vivo

SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats weighing 230-260 g[2]
Dosage: 0.1, 0.3 and 1.0 mg/kg
Administration: IP; two doses (4 days between two doses)
Result: Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.
Molecular Weight

337.80

Formula

C19H16ClN3O
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=C4C=CC=NC4=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (74.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9603 mL 14.8017 mL 29.6033 mL
5 mM 0.5921 mL 2.9603 mL 5.9207 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9603 mL 14.8017 mL 29.6033 mL 74.0083 mL
5 mM 0.5921 mL 2.9603 mL 5.9207 mL 14.8017 mL
10 mM 0.2960 mL 1.4802 mL 2.9603 mL 7.4008 mL
15 mM 0.1974 mL 0.9868 mL 1.9736 mL 4.9339 mL
20 mM 0.1480 mL 0.7401 mL 1.4802 mL 3.7004 mL
25 mM 0.1184 mL 0.5921 mL 1.1841 mL 2.9603 mL
30 mM 0.0987 mL 0.4934 mL 0.9868 mL 2.4669 mL
40 mM 0.0740 mL 0.3700 mL 0.7401 mL 1.8502 mL
50 mM 0.0592 mL 0.2960 mL 0.5921 mL 1.4802 mL
60 mM 0.0493 mL 0.2467 mL 0.4934 mL 1.2335 mL
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SB-215505 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-215505162100-15-4SB215505SB 2155055-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorwakefulnessmotoractivityintermediatestageofsleepISparadoxicalPSSWS-2Inhibitorinhibitorinhibit

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