1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Eptapirone

Eptapirone (Synonyms: F 11440)

Cat. No.: HY-19946 Purity: 99.91%
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Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.

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

Eptapirone Chemical Structure

Eptapirone Chemical Structure

CAS No. : 179756-58-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 319 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.

In Vitro

The affinity of Eptapirone (F11440) for 5-HT1Abinding sites (pKi, 8.33) was higher than that of buspirone (pKi , 7.50), and somewhat lower than that of flesinoxan (pKi , 8.91).In vivo, Eptapirone (F11440) was 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). Eptapirone (F11440), shown here to be a potent, selective, high efficacy 5-HT1Areceptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans.[1]

Molecular Weight

345.40

Formula

C₁₆H₂₃N₇O₂

CAS No.

179756-58-2

SMILES

O=C(N1C)N(CCCCN2CCN(C3=NC=CC=N3)CC2)N=CC1=O

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
Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (17.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8952 mL 14.4760 mL 28.9519 mL
5 mM 0.5790 mL 2.8952 mL 5.7904 mL
10 mM 0.2895 mL 1.4476 mL 2.8952 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay

Eptapirone (F11440) is dissolved in DMSO. The HeLa cell line permanently transfected with the human 5-HT1A receptor gene and permanently expressing the 5-HT1A receptor protein (HA7). In subsequent experiments, the maximum effect of Eptapirone (F11440) is compared with those of other compounds by repeated testing (n=9) at a concentration of 10-5 M (i.e., a concentration at which the reference compounds used here appeared to attain their maximal effects) in a first series of experiments and at 10-4 M in a second series. Data from each series were analyzed statistically by means of a one-way analysis of variance followed by sequential paired comparisons by means of Newman-Keuls tests[1].

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

Animal Administration
[1]

Rats[1]
For in vivo studies, F 11440 was suspended in distilled water by adding Tween 80 (2 drops/10 ml). When injected i.v., F 11440 was dissolved in a mixture of 60% PEG and 40% physiological saline. Doses are expressed as the weight of the free base. Twenty-four hours before use in the experiments, rats were housed individually in a restricted area (accessible only to the experimenter) and received 15 g standard laboratory food (water continued to be available freely). Experiments, consisting of drug treatments after which animals were decapitated and trunk blood was collected, were conducted between 8:00 a.m. and 10:30 a.m. F 11440 (or vehicle) was administered 60 min before decapitation when given p.o., and 30 min before decapitation when given i.p.[1].

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

References
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Eptapirone
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HY-19946
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