2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB 242084

SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

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SB 242084 Chemical Structure

SB 242084 Chemical Structure

CAS No. : 181632-25-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SB 242084:

SB 242084 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SB 242084

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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  • Purity & Documentation

  • References

  • Customer Review

Description

SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3].

IC50 & Target

5-HT2C Receptor

9.0 (pKi)

In Vitro

SB 242084 (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2C receptor in SH-SY5Y cells[1].
SB 242084 (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC[2].

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

SB 242084 Related Antibodies

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 100 nM
Incubation Time: 45 min
Result: Antagonized 5-HT induced concentration-related increase in PI hydrolysis.

RT-PCR[2]

Cell Line: RPTC cells
Concentration: 1-100 nM
Incubation Time: 24 h
Result: Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.
In Vivo

SB 242084 (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests[1].
SB 242084 (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats[1].
SB 242084 (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats[3].
SB 242084 (160-640 µg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo[3].

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

Animal Model: Male Sprague-Dawley (CD) rats[1].
Dosage: 0.1-1 mg/kg
Administration: Intraperitoneal injection; single; 20 min pre-test
Result: Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.
Animal Model: Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model)[1].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; single; 20 min pre-test
Result: Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.
Animal Model: Rats[2].
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection; single
Result: Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
Molecular Weight

394.85

Formula

C21H19ClN4O2
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3
Shipping

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

DMSO : ≥ 44 mg/mL (111.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5326 mL 12.6630 mL 25.3261 mL
5 mM 0.5065 mL 2.5326 mL 5.0652 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.76%

COA (255 KB) LCMS (111 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5326 mL 12.6630 mL 25.3261 mL 63.3152 mL
5 mM 0.5065 mL 2.5326 mL 5.0652 mL 12.6630 mL
10 mM 0.2533 mL 1.2663 mL 2.5326 mL 6.3315 mL
15 mM 0.1688 mL 0.8442 mL 1.6884 mL 4.2210 mL
20 mM 0.1266 mL 0.6332 mL 1.2663 mL 3.1658 mL
25 mM 0.1013 mL 0.5065 mL 1.0130 mL 2.5326 mL
30 mM 0.0844 mL 0.4221 mL 0.8442 mL 2.1105 mL
40 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
50 mM 0.0507 mL 0.2533 mL 0.5065 mL 1.2663 mL
60 mM 0.0422 mL 0.2111 mL 0.4221 mL 1.0553 mL
80 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
100 mM 0.0253 mL 0.1266 mL 0.2533 mL 0.6332 mL
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SB 242084 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 242084181632-25-7SB242084SB-2420845-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptoracute organ damageanxietydepressionschizophreniaSH-SY5YRPTC cellsInhibitorinhibitorinhibit

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