A 5-HT2 antagonist
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Fananserin

Item No. 33216

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-2H-naphth[1,8-cd]isothiazole, 1,1-dioxide
CAS Number
127625-29-0
Synonyms
  • RP-62203
Molecular Formula
C23H24FN3O2S
Formula Weight
425.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=S1(C2=CC=CC3=CC=CC(N1CCCN4CCN(CC4)C5=CC=C(C=C5)F)=C32)=O
InChi Code
InChI=1S/C23H24FN3O2S/c24-19-8-10-20(11-9-19)26-16-14-25(15-17-26)12-3-13-27-21-6-1-4-18-5-2-7-22(23(18)21)30(27,28)29/h1-2,4-11H,3,12-17H2
InChi Key
VGIGHGMPMUCLIQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $53

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    10 mg

    $80

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    25 mg

    $119

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    50 mg

    $185

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    Product Description

    Fananserin is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2 (IC50 = 0.12 nM for the rat receptor).1 It is selective for 5-HT2 over 5-HT1A, 5-HT3, the α1-adrenergic receptor (α1-AR), dopamine D2 receptor (IC50s = 75, 6,600, 4.3, and 390 nM, respectively, for the rat receptors), and histamine H1 receptor (IC50 = 50 nM for the guinea pig receptor). Fananserin is also an antagonist of the dopamine D4 receptor (Ki = 2.93 nM for the human receptor).2 It inhibits the head-twitch response (HTR) induced by mescaline in mice (ED50 = 0.16 mg/kg). Fananserin (2 or 4 mg/kg) increases time in deep non-rapid eye movement (NREM) sleep and decreases time in light NREM sleep in rats.3 It increases the time spent in the open arms of the elevated plus maze in mice when administered at doses of 0.25, 1, or 4 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doble, A., Girdlestone, D., Piot, O., et al. Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist. Br. J. Pharmacol. 105(1), 27-36 (1992).

    2. Heuillet, E., Petitet, F., Mignani, S., et al. The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor. Eur. J. Pharmacol. 314(1-2), 229-233 (1996).

    3. Stutzmann, J.M., Eon, B., Lucas, M., et al. RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats. Sleep 15(2), 119-124 (1992).

    4. Stutzmann, J.M., Eon, B., Darche, F., et al. Are 5-HT2 antagonists endowed with anxiolytic properties in rodents? Neurosci. Lett. 128(1), 4-8 (1991).