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

Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research.

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Gepirone Chemical Structure

Gepirone Chemical Structure

CAS No. : 83928-76-1

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Gepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research[1].

IC50 & Target

5-HT1A Receptor

 

In Vivo

Gepirone (0-3 mg/kg for intraperitoneal injection) interacts with progesterone at 5-HT1A receptors to reduce lordosis behavior in female rats treated with estradiol benzoate and progesterone[1].
Gepirone (10, 15 mg/kg for subcutaneous injection, 2, 7, or 14 days) activates the normosensitive postsynaptic 5-HT1A receptor in Male Sprague-Dawley rats[2].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 0, 0.1, 0.3, 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increases in lordotic activity at lower doses.
Inhibited lordosis by the 0.3 and 1.0 mg/kg doses and further inhibition was produced by the 3.0 mg/kg dose.
Animal Model: Male Sprague-Dawley rats[2]
Dosage: 10, 15 mg/kg
Administration: Subcutaneous injection (s.c.)
Result: Decreased the number of spontaneously active 5-HT neurons and firing rate.
Not modified with long-term treatment with ED50 value of 10.1±0.5 μg/kg in controls and 9.7 ±1.9 μg/kg in treated rats.
Molecular Weight

359.47

Formula

C19H29N5O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(CC(C)(C)C1)N(CCCCN2CCN(C3=NC=CC=N3)CC2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

Ethanol : 33.33 mg/mL (92.72 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (92.72 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 2.7819 mL 13.9094 mL 27.8187 mL
5 mM 0.5564 mL 2.7819 mL 5.5637 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 (protect from light). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.81%

COA (245 KB) HNMR (133 KB) RP-HPLC (271 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, 6 months; -20°C, 1 month (protect from light). 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
Ethanol / DMSO 1 mM 2.7819 mL 13.9094 mL 27.8187 mL 69.5468 mL
5 mM 0.5564 mL 2.7819 mL 5.5637 mL 13.9094 mL
10 mM 0.2782 mL 1.3909 mL 2.7819 mL 6.9547 mL
15 mM 0.1855 mL 0.9273 mL 1.8546 mL 4.6365 mL
20 mM 0.1391 mL 0.6955 mL 1.3909 mL 3.4773 mL
25 mM 0.1113 mL 0.5564 mL 1.1127 mL 2.7819 mL
30 mM 0.0927 mL 0.4636 mL 0.9273 mL 2.3182 mL
40 mM 0.0695 mL 0.3477 mL 0.6955 mL 1.7387 mL
50 mM 0.0556 mL 0.2782 mL 0.5564 mL 1.3909 mL
60 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1591 mL
80 mM 0.0348 mL 0.1739 mL 0.3477 mL 0.8693 mL
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Gepirone 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:

Gepirone83928-76-15-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT1A receptorsgepironeanxiolyticslordosisInhibitorinhibitorinhibit

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