| Identification | Back Directory | [Name]
Fananserin | [CAS]
127625-29-0 | [Synonyms]
RP-62203
Fananserin
2-[3-[4-(4-Fluorophenyl)piperazino]propyl]-2H-naphth[1,8-cd]isothiazole 1,1-dioxide
2-[3-[4-(4-Fluorophenyl)-1-piperazinyl]propyl]-2H-naphthyl[1,8-cd]isothiazole-1,1-dioxide
2H-Naphth[1,8-cd]isothiazole, 2-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-, 1,1-dioxide | [Molecular Formula]
C23H24FN3O2S | [MDL Number]
MFCD00866648 | [MOL File]
127625-29-0.mol | [Molecular Weight]
425.52 |
| Chemical Properties | Back Directory | [Melting point ]
95-97 °C(Solv: acetonitrile (75-05-8)) | [Boiling point ]
641.1±65.0 °C(Predicted) | [density ]
1.331±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
7.31±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
Antipsychotic. | [Definition]
ChEBI: LSM-2183 is a sulfonic acid derivative and a member of naphthalenes. | [Biological Activity]
5-HT 2A receptor antagonist that also displays high affinity at D 4 receptors (K i values are 0.26, 2.93, 25, 38, 70 and 726 nM for 5-HT 2A , D 4 , H 1 , α 1 , 5-HT 1A and D 2 receptors respectively). Inhibits inositol phosphate formation evoked by 5-HT in vitro (IC 50 = 7.76 nM) and antagonizes mescaline-induced head twitches in vivo . | [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. |
| [IC 50]
5-HT2 Receptor: 0.37 nM (Ki); D4 Receptor: 2.93 nM (Ki) |
|
| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
| Company Name: |
InvivoChem
|
| Telephone: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|