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Eptapirone

Cat. No. M8932
Eptapirone Structure
Synonym:

F11440

Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 500  USD500 In stock
50mg USD 1480  USD1480 In stock
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Quality Control & Documentation
Biological Activity

The affinity of Eptapirone (F11440) for 5-HT1A binding 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).

Chemical Information
Molecular Weight 345.4
Formula C16H23N7O2
CAS Number 179756-58-2
Solubility (25°C) DMSO: 5 mg/mL (Need ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wilson SJ, et al. J Psychopharmacol. The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans.

[2] Koek W, et al. J Pharmacol Exp Ther. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.

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Keywords: Eptapirone, F11440 supplier, 5-HT Receptor, inhibitors, activators


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