Fananserin free base

Fananserin is an orally bioavailable, potent and selective 5-hydroxytryptamine2 receptor antagonist.

For research use only. Not for human or veterinary use.

Target 5-HT Receptor Dopamine Receptor

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

Fananserin structure

CAS No.: 127625-29-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 410.00	BP-02416-250mg	In stock	Get quote
500 mg	USD 660.00	BP-02416-500mg	In stock	Get quote
1 g	USD 1,050.00	BP-02416-1g	In stock	Get quote
2 g	USD 1,680.00	BP-02416-2g	In stock	Get quote
3 g	USD 2,015.00	BP-02416-3g	In stock	Get quote
5 g	USD 2,685.00	BP-02416-5g	In stock	Get quote
10 g	USD 4,300.00	BP-02416-10g	In stock	Get quote

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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 .

Biological activity

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. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM. RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors. In Vivo Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex. 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). 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.

Identifiers

SMILES: FC1=CC=C(N2CCN(CCCN(C3=CC=CC4=C3C5=CC=C4)S5(=O)=O)CC2)C=C1
InChIKey: VGIGHGMPMUCLIQ-UHFFFAOYSA-N

Specifications

MW (average): 425.5190
Formula: C₂₃H₂₄FN₃O₂S
CAS No.: 127625-29-0
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[1].Heuillet E, et al. The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor. Eur J Pharmacol. 1996 Oct 24;314(1-2):229-33.

[2].Malgouris C, et al. Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. In vitro and ex vivo selectivity profile. Eur J Pharmacol. 1993 Mar 16;233(1):29-35.

[3].Stutzmann JM, et al. RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats. Sleep. 1992 Apr;15(2):119-24.

Same target

Search 5-HT Receptor

Same research area

Search Neurological Disease