Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro-
Flesinoxan
CAS: 98206-10-1
Molecular Formula: C22H26FN3O4
Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro- - Names and Identifiers
Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro- - Physico-chemical Properties
| Molecular Formula | C22H26FN3O4 |
| Molar Mass | 415.46 |
| Density | 1.271±0.06 g/cm3(Predicted) |
| Boling Point | 635.8±55.0 °C(Predicted) |
| Specific Rotation(α) | D +26° (c = 1 in methanol) |
| pKa | 14.09±0.10(Predicted) |
| In vivo study | Flesinoxan acts as a partial agonist at postsynaptic and as a full agonist at presynaptic 5-HT1A receptors. The capacity of Flesinoxan to antagonize the effect of 5-HT on CA3 pyramidal neurons was similar to that of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT). The intravenous administration of Flesinoxan suppresses the firing activity of both CA3 pyramidal neurons and dorsal raphe 5-HT neurons. The acute brain penetration of [ 3 H]Flesinoxan and [ 3 H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [ 3 H]8-OH-DPAT reached significantly greater brain concentration than [ 3 H]Flesinoxan. Subcutaneous administration of Flesinoxan and 8-OH-DPAT produce a dose-dependent hypothermia. The Flesinoxan-induced hypothermia is significantly attenuated by prior administration of the non-selective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. Similar degrees of hypothermia are achieved with 3 mg/kg of Flesinoxan and 0.5 mg/kg of 8-OH-DPAT. The maximal effect of Flesinoxan occurs 30 min later than that of 8-OH-DPAT and fades more slowly. |
Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro- - References
| Biological activity | Flesinoxan is a hypotensive agent, an effective, high-affinity selective serotonin 1A (5-HT1A) receptor agonist, with an EC50 value of 24 nM. Flesinoxan also has an effective anti-anxiety/antidepressant effect. |
Last Update：2024-04-10 22:29:15
![Benzamide, N-[2-[4-[(2R)-2,3-dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluoro-](http://res.chembk.com/assets/str/2d/9/98/98206-10-1.png)
Supplier List
View History