Eptapirone

Catalog No.S0113 Batch:S011301

Technical Data

Formula	C₁₆H₂₃N₇O₂
Molecular Weight	345.40	CAS No.	179756-58-2
Solubility (25°C)*	In vitro	DMSO	69 mg/mL (199.76 mM)
		Ethanol	39 mg/mL (112.91 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.The affinity (pKi) of F11440 for 5-HT1A binding sites is 8.33.

Targets

5-HT1A ^[1]
(in the 5-HT1A binding assay)

8.33(pKi)

In vitro

The affinity of Eptapirone for 5-HT1A binding sites (pKi, 8.33) is higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In HeLa cells expressing human 5-HT1A receptors, Eptapirone decreases the forskolin-induced increase in AMP, and, based on its maximal effect, is found to have an intrinsic activity of 1.0 relative to that of 5-HT, which is significantly higher than that of buspirone (0.49), ipsapirone (0.46) and flesinoxan (0.93).^[1]

In vivo

In vivo, Eptapirone (F11440) is 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). Eptapironeproduced anxiolytic- and antidepressant-like effects in animal models (i.e., increased punished responding in a pigeon conflict procedure and decreased immobility in a rat forced swimming test, respectively) that are more substantial than those of buspirone, ipsapirone and flesinoxan. ^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HeLa cells Concentrations -- Incubation Time 10 min Method Cells are preincubated with DMEM, 10 mM HEPES for 10 min at room temperature. Drugs, at concentrations ranging from 0.1 nM to 100 M, and appropriate vehicle controls, are then added in DMEM, 10 mM HEPES, 100 M forskolin and 100 M IBMX to the cells. Antagonists are added at the same time as the agonists. At the end of the treatment (10 min, room temperature), the reaction is stopped by aspiration of the medium and addition of 0.1 N HCl. Cellular extract is diluted 1:500 or 1:400 in radioimmunoassay buffer, and cAMP content is measured by using a commercially available kit.
Animal Study:^{^[1]}	Animal Models Male Sprague-Dawley rats (160 to 200 g); Male Dunkin-Hartley guinea pigs (310 to 490 ); Male White Carneau pigeons (500 to 650 g) Dosages 0.16 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
HeLa cells
Concentrations
--
Incubation Time
10 min
Method
Cells are preincubated with DMEM, 10 mM HEPES for 10 min at room temperature. Drugs, at concentrations ranging from 0.1 nM to 100 M, and appropriate vehicle controls, are then added in DMEM, 10 mM HEPES, 100 M forskolin and 100 M IBMX to the cells. Antagonists are added at the same time as the agonists. At the end of the treatment (10 min, room temperature), the reaction is stopped by aspiration of the medium and addition of 0.1 N HCl. Cellular extract is diluted 1:500 or 1:400 in radioimmunoassay buffer, and cAMP content is measured by using a commercially available kit.

Animal Study:^{^[1]}

Animal Models
Male Sprague-Dawley rats (160 to 200 g); Male Dunkin-Hartley guinea pigs (310 to 490 ); Male White Carneau pigeons (500 to 650 g)
Dosages
0.16 mg/kg
Administration
i.p.

References

[1] Koek W, et al. J Pharmacol Exp Ther. 1998 Oct;287(1):266-83.

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SHIPPING AND STORAGE
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