Cat. No.: HY-B1115A

Buspirone

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.

For research use only. We do not sell to patients.

Purity: 99.86%
CAS No.: 36505-84-7
Formula: C₂₁H₃₁N₅O₂
Molecular Weight:385.50

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Buspirone Chemical Structure

CAS No.: 36505-84-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

5-HT_1A Receptor

Dopamine D2 receptor

All 5-HT Receptor Isoforms :

All Dopamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	41 nM Compound: 1	Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR	[PMID: 19147349]
HEK293	IC₅₀	1.7 μM Compound: buspirone	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	12 μM Compound: buspirone	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	46 μM Compound: buspirone	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
Sf21	IC₅₀	104.5 μM Compound: Buspirone	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	369.8 μM Compound: Buspirone	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]

In Vitro

The anxiolytic and anti-depressant effects of Buspirone are produced by activating 5-HT1A autoreceptors and 5-HT1A heteroreceptors, respectively^[1].
Buspirone (0-400 µg/mL; 6 hours) has cytotoxic effect in lymphocytes^[2].
Buspirone (0-180 µg/mL; 0-3 hours; lymphocytes) induces ROS formation, mitochondrial membrane potential collapse(MMP), lipid peroxidation, lysosomal damage and elevation of glutathione disulfide (GSSG)^[2].

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

Cell Viability Assay^[2]

Cell Line:

Lymphocytes
Concentration:

0, 4, 20, 40, 200 and 400 µg/mL
Incubation Time:

6 hours
Result:

Decreased cell viability in a dose-dependent manner.

In Vivo

Buspirone (1-5 mg/kg; i.p. and i.g.; for 5 days; C57BL/6N mice) reduces anxiety/depression behaviors^[1].
Buspirone (1-5 mg/kg; i.p. and i.g.; for 5 days; C57BL/6N mice) restores immobilization stress (IS)-shifted β-diversity in the gut microbiota^[1].

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

Animal Model:

Male C57BL/6N mice^[1]
Dosage:

1 and 5 mg/kg
Administration:

Oral gavage and intraperitoneal injection; for 5 days
Result:

Reduced TNF-α expression and NF-κB⁺/Iba1⁺ cell population in the hippocampus and myeloperoxidase activity and NF-κB⁺/CD11c⁺ cell population in the colon.

Animal Model:

Male C57BL/6N mice^[1]
Dosage:

1 and 5 mg/kg
Administration:

Oral gavage and intraperitoneal injection; for 5 days
Result:

Reduced the IS- or Escherichia coli K1 (EC)-induced gut Proteobacteria population.

Chemical Information

CAS No. 36505-84-7
Appearance Solid
Molecular Weight 385.50
Formula C₂₁H₃₁N₅O₂
Color White to off-white
SMILES

O=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)CC43CCCC4
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

Publications (3)

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Journal Impact Factor

Environ Sci Technol

Data-Driven Discovery of Unknown Precursors of N-Nitrosodimethylamine in Nontargeted Liquid Chromatography-High Resolution Mass Spectrometry Analysis. [Abstract]

2026 Mar 3;60(8):6558-6568. PMID: 41714108
Clin Pharmacol Ther

Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter-Mediated Interactions Using a Human Primary Intestinal 3D Model (EpiIntestinal™). [Abstract]

2025 Jul 14. PMID: 40657937
Mol Pharmacol

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (259.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5940 mL

12.9702 mL

25.9403 mL

5 mM

0.5188 mL

2.5940 mL

5.1881 mL

10 mM

0.2594 mL

1.2970 mL

2.5940 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (6.49 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.49 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.49 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kim JK, et, al. Buspirone alleviates anxiety, depression, and colitis; and modulates gut microbiota in mice. Sci Rep. 2021 Mar 17;11(1):6094. [Content Brief]

[2]. Salimi A, et, al. Analysis of Toxicity Effects of Buspirone, Cetirizine and Olanzapine on Human Blood Lymphocytes: in Vitro Model. Curr Clin Pharmacol. 2018;13(2):120-127. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.5940 mL	12.9702 mL	25.9403 mL	64.8508 mL
	5 mM	0.5188 mL	2.5940 mL	5.1881 mL	12.9702 mL
	10 mM	0.2594 mL	1.2970 mL	2.5940 mL	6.4851 mL
	15 mM	0.1729 mL	0.8647 mL	1.7294 mL	4.3234 mL
	20 mM	0.1297 mL	0.6485 mL	1.2970 mL	3.2425 mL
	25 mM	0.1038 mL	0.5188 mL	1.0376 mL	2.5940 mL
	30 mM	0.0865 mL	0.4323 mL	0.8647 mL	2.1617 mL
	40 mM	0.0649 mL	0.3243 mL	0.6485 mL	1.6213 mL
	50 mM	0.0519 mL	0.2594 mL	0.5188 mL	1.2970 mL
	60 mM	0.0432 mL	0.2162 mL	0.4323 mL	1.0808 mL
	80 mM	0.0324 mL	0.1621 mL	0.3243 mL	0.8106 mL
	100 mM	0.0259 mL	0.1297 mL	0.2594 mL	0.6485 mL

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Buspirone

GPCR/G Protein Compound Library

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Publications Citing Use of MedChemExpress (MCE) Buspirone

All 5-HT Receptor Isoforms

All Dopamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Buspirone Related Classifications

HY-B1115A Related Classifications