F-11440

SKU: orb1225895

Description

A potent, selective 5-HT1A receptor agonist with Ki of 4.8 nM, pKi of 8.33; shows ≥shows 100-fold higher affinity for the other serotonin receptor subtypes, and has no detectable antidopaminergic activity and antihistaminergic activity; decreases the forskolin-induced increase in AMP in HeLa cells expressing human 5-HT1A receptors; produces anxiolytic- and antidepressant-like effects in animal models.Anxiety Phase 1 Discontinued(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.

Key Properties

• CAS Number: 179756-58-2
• MW: 345.3995
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₃N₇O₂
• SMILES: O=C(N1C)N(CCCCN2CCN(C3=NC=CC=N3)CC2)N=CC1=O
• Target: 5-HT Receptor
• Solubility: DMSO: 6 mg/mL (Need ultrasonic)

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Eptapirone

Quick Database Links

Gene Symbol

5-HT Receptor