Fananserin

Modify Date: 2024-01-02 16:28:31

Fananserin structure	Common Name	Fananserin
	CAS Number	127625-29-0	Molecular Weight	425.51900
	Density	1.331g/cm3	Boiling Point	641.1ºC at 760mmHg
	Molecular Formula	C₂₃H₂₄FN₃O₂S	Melting Point	N/A
	MSDS	N/A	Flash Point	341.5ºC

Use of Fananserin

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[1].

Name	Fananserin
Synonym	More Synonyms

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[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	Ki: 0.37 nM (5-HT2), 2.93 nM (human DA D4 receptor)[1]
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[1]. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[1]. RP 62203 displays low to moderate affinity for α1-adrenoceptors, dopamine D2 receptors and histamine H 1 receptors[2].
In Vivo	Fananserin displaces [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex[2]. 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)[2]. 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[3]. Animal Model: Adult male Sprague Dawley rats (250-300 g)[3] Dosage: 0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg Administration: Oral administration Result: Increased the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg.
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.

Density	1.331g/cm3
Boiling Point	641.1ºC at 760mmHg
Molecular Formula	C₂₃H₂₄FN₃O₂S
Molecular Weight	425.51900
Flash Point	341.5ºC
Exact Mass	425.15700
PSA	52.24000
LogP	4.84860
Vapour Pressure	2.48E-16mmHg at 25°C
Index of Refraction	1.659

Precursor 5
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