CAS 127625-29-0|Fananserin
Introduction：Basic information about CAS 127625-29-0|Fananserin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| 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 | / |
| MSDS | / | Flash Point | 341.5ºC |
Names
| Name | Fananserin |
|---|---|
| Synonym | More Synonyms |
Fananserin BiologicalActivity
| 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 ReceptorSignaling Pathways >>Neuronal Signaling >>Dopamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling 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. |
Chemical & Physical Properties
| 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 |
| InChIKey | VGIGHGMPMUCLIQ-UHFFFAOYSA-N |
| SMILES | O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 |
Synonyms
| C23H24FN3O2S |
| fananserine |
| UNII-38QJ762ET6 |
