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 |
| InChI Key | VGIGHGMPMUCLIQ-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
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
Keywords: Fananserin, supplier, 5-HT2A, antagonists, D4, Serotonin, Receptors, Dopamine, dopaminergic, RP62203, RP, 62203, 5-HT2A, Receptors, D4, Receptors, 5-HT2A, Receptors, Tocris Bioscience
