Home Neuronal Signaling 5-HT Receptor agonist Eptapirone For research use only.

Eptapirone

Synonyms: F 11440

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.

Eptapirone Chemical Structure

Eptapirone Chemical Structure

CAS No. 179756-58-2

Purity & Quality Control

Batch: S011301 DMSO]69 mg/mL]false]Ethanol]39 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Eptapirone Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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.

Chemical Information & Solubility

Molecular Weight 345.40 Formula

C16H23N7O2
CAS No. 179756-58-2 SDF --
Smiles CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=NC=CC=N3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 69 mg/mL ( (199.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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