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Cat.No. 2645 - Fananserin | C23H24FN3O2S | CAS No. 127625-29-0
Description: 5-HT2A antagonist. Also D4 antagonist
Alternative Names: RP 62203
Chemical Name: 2-[3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl]-2H-naphthyl[1,8-cd]isothiazole-1,1-dioxide
Purity: ≥99% (HPLC)

Biological Activity

5-HT2A receptor antagonist that also displays high affinity at D4 receptors (Ki values are 0.26, 2.93, 25, 38, 70 and 726 nM for 5-HT2A, D4, H1, α1, 5-HT1A and D2 receptors respectively). Inhibits inositol phosphate formation evoked by 5-HT in vitro (IC50 = 7.76 nM) and antagonizes mescaline-induced head twitches in vivo.

Technical Data

M. Wt 425.52
Formula C23H24FN3O2S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 127625-29-0
PubChem ID 60785
Smiles FC1=CC=C(C=C1)N1CCN(CCCN2C3=C4C(=CC=CC4=CC=C3)S2(=O)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 42.55 100

Preparing Stock Solutions

The following data is based on the product molecular weight 425.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.35 mL 11.75 mL 23.5 mL
5 mM 0.47 mL 2.35 mL 4.7 mL
10 mM 0.24 mL 1.18 mL 2.35 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

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References are publications that support the products' biological activity.

Malleron et al (1991) Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists. J.Med.Chem. 34 2477 PMID: 1908521

Doble et al (1992) Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist. Br.J.Pharmacol. 105 27 PMID: 1596688

Heuillet et al (1996) The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor. Eur.J.Pharmacol. 314 229 PMID: 8957240

If you know of a relevant reference for Fananserin, please let us know.

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Keywords: Fananserin, supplier, 5-HT2A, antagonists, D4, Serotonin, Receptors, Dopamine, dopaminergic, RP62203, RP, 62203, 5-HT2A, Receptors, D4, Receptors, 5-HT2A, Receptors, Tocris Bioscience

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