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Fananserin

Catalog No. T15270   CAS 127625-29-0
Synonyms: RP 62203

Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).

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Fananserin Chemical Structure
Fananserin, CAS 127625-29-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 52.00
5 mg In stock $ 105.00
10 mg In stock $ 148.00
25 mg In stock $ 241.00
50 mg In stock $ 355.00
100 mg In stock $ 528.00
500 mg In stock $ 1,180.00
1 mL * 10 mM (in DMSO) In stock $ 125.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).
Targets&IC50 D4 Receptor:2.93 nM (ki), 5-HT2 receptor:0.37 nM (ki)
In vitro Fananserin displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors[1]. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[3]. Fananserin is relatively selective for 5-HT2 receptor with lower affinity for the 5-HT1A receptor and very low affinity for the 5-HT3 receptor[3].
In vivo Fananserin shows a moderate affinity for alpha 1-adrenoceptors in the rat thalamus with an IC50 of 14 nM and for H1 receptors in the guinea-pig cerebellum with an IC50 of 13 nM[1]. Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in the rat frontal cortex[1]. Fananserin (0.5, 1, 2 and 4 mg/kg; p.o.) dose-dependently increases the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness[2].
Synonyms RP 62203
Molecular Weight 425.52
Formula C23H24FN3O2S
CAS No. 127625-29-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (223.26 mM), sonification is recommended.

TargetMolReferences and Literature

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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library Inhibitor Library Anti-Cancer Compound Library Orally Active Compound Library ReFRAME Related Library Bioactive Compound Library

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Keywords

Fananserin 127625-29-0 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor RP-62203 Inhibitor RP 62203 RP62203 inhibit 5-HT2 dopamine Serotonin Receptor 5-hydroxytryptamine Receptor inhibitor

 

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