Home Neuronal Signaling 5-HT Receptor agonist Eptapirone

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Eptapirone 5-HT Receptor agonist

Cat.No.S0113

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

Chemical Structure

Molecular Weight: 345.40

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 345.40 Formula

C16H23N7O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 179756-58-2 -- Storage of Stock Solutions

Synonyms F 11440 Smiles CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=NC=CC=N3

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble

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In vivo
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Mechanism of Action

Targets/IC50/Ki
5-HT1A
(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, this compound 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).
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). This compound produced 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.

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