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

Fananserin (Synonyms: RP 62203)

Cat. No.: HY-103104 Purity: 99.71%
Handling Instructions

Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.

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

Fananserin Chemical Structure

Fananserin Chemical Structure

CAS No. : 127625-29-0

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10 mM * 1  mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 188 In-stock
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Estimated Time of Arrival: December 31
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Description

Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor[1].

IC50 & Target

5-HT2 Receptor

0.37 nM (Ki)

D4 Receptor

2.93 nM (Ki)

In Vitro

Fananserin is relatively selective for 5-HT2 receptor, having lower affinity for the 5-HT1A receptor and very low affinity for the 5-HT3 receptor[1].
Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[1].
RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors[2].

In Vivo

Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex[2].
Fananserin shows moderate affinity for alpha 1-adrenoceptors in the rat thalamus (IC50 = 14 nM) and for histamine H1 receptors in the guinea-pig cerebellum (IC50 = 13 nM)[2].
Fananserin (0.5-4 mg/kg; p.o.) increases the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner[3].

Animal Model: Adult male Sprague Dawley rats (250-300 g)[3]
Dosage: 0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg
Administration: Oral administration
Result: Increased the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg.
Molecular Weight

425.52

Formula

C₂₃H₂₄FN₃O₂S

CAS No.

127625-29-0

SMILES

FC1=CC=C(N2CCN(CCCN(C3=CC=CC4=C3C5=CC=C4)S5(=O)=O)CC2)C=C1

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
References

Purity: 99.71%

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Keywords:

FananserinRP 62203RP62203RP-622035-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2dopamineD4Inhibitorinhibitorinhibit

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