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

Flesinoxan 

Cat. No.: HY-121653
Handling Instructions

Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.

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Flesinoxan Chemical Structure

Flesinoxan Chemical Structure

CAS No. : 98206-10-1

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Description

Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects[1][2][3].

IC50 & Target[1]

5-HT1A Receptor

24 nM (EC50)

In Vivo

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)[1].
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 [3H]Flesinoxan and [3H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [3H]8-OH-DPAT reached significantly greater brain concentration than [3H]Flesinoxan[1].
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[1].

Molecular Weight

415.46

Formula

C₂₂H₂₆FN₃O₄

CAS No.

98206-10-1

SMILES

O=C(NCCN1CCN(C2=C3OC[[email protected]@H](CO)OC3=CC=C2)CC1)C4=CC=C(F)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Flesinoxan
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