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| 25mg |
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Fananserin (RP-62203; RP62203) is a novel and potent antipsychotic agent acting as a 5-hydroxytryptamine2 (5-HT2) receptor antagonist (Ki = 0.37 nM for the rat 5-HT2A receptor).
| Targets |
5-HT2 Receptor ( Ki = 0.37 nM ); D4 Receptor ( Ki = 2.93 nM )
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|---|---|
| ln Vitro |
Fananserin has very little affinity for the 5-HT3 receptor and less affinity for the 5-HT1A receptor, making it comparatively selective for the 5-HT2 receptor[1].
Fananserin displaces [3H]spiperone binding to recombinant human dopamine D 4 receptors with a Ki of 2.93 nM[1].
RP 62203 exhibits low to moderate binding affinity towards histamine H1 receptors, dopamine D2 receptors, and α1-adrenoceptors[2].
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| ln Vivo |
Fananserin displaces [125I]AMIK from 5-HT2 receptors at an IC50 of 0.21 nM in rat frontal cortex[2].
Fananserin demonstrates a moderate affinity for the rat thalamus's alpha 1-adrenoceptors (IC50 = 14 nM) and the guinea-pig cerebellum's histamine H1 receptors (IC50 = 13 nM)[2]. Fananserin (0.5-4 mg/kg; p.o.) lengthens the duration of deep nonrapid eye movement (NREM) sleep at the expense of wakefulness in a dose-dependent manner[3]. |
| Enzyme Assay |
The dopamine D4 receptor is a potential target for novel antipsychotic drugs. Most available compounds with affinity for the dopamine D4 receptor also bind to dopamine D2 receptors. This report describe the affinity of the 5-HT2A receptor antagonist RP 62203 (fananserin) for the human dopamine D4 receptor. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D4 receptors with a Ki of 2.93 nM. This compares with an affinity (Ki) of 0.37 nM for the rat 5-HT2A receptor and of 726 mM for the rat dopamine D2 receptor. [3H]Fananserin can be used to label the recombinant dopamine D4 receptor expressed in Chinese hamster ovary cells with a KD of 0.725 nM. Fananserin is, thus, the first compound to be reported that distinguishes between dopamine D4 and D2 receptors[1].
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| Cell Assay |
In this study, quantitative autoradiography was used to determine the selectivity of RP 62203, a novel naphtosultam derivative, for 5-HT2 receptors in vitro and ex vivo, using [125I]7-amino-8-iodo-ketanserin ([125I]AMIK) and [3H]mesulergine as radioligands. The density of [125I]AMIK or [3H]mesulergine binding sites was determined by quantitative image analysis. In in vitro experiments, RP 62203 displaced [125I]AMIK from 5-HT2 receptors with an IC50 of 0.21 nM in rat frontal cortex. Its affinity for 5-HT1C receptors was 100-fold lower (IC50 25 nM versus [3H]mesulergine in rat choroid plexus). RP 62203 showed 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). The tetrabenazine sites were not affected by RP 62203 at a concentration of 30 nM. In ex vivo experiments, RP 62203 was about 4 times more potent than ritanserin in displacing [125I]AMIK from 5-HT2 receptors (ED50 0.58 mg/kg p.o.). A dose of 10 mg/kg of RP 62203 did not displace [3H]mesulergine from 5-HT1C receptors or [125I]AMIK from alpha 1-adrenoceptors and tetrabenazine sites in the rat brain and from histamine H1 receptors in the guinea-pig brain. These results demonstrate that RP 62203 specifically recognizes 5-HT2 receptors in rodent brain[2].
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| Animal Protocol |
Adult male Sprague Dawley rats (250-300 g)
0.5 mg/kg, 1 mg/kg,2 mg/kg, 4 mg/kg Oral administration RP 62203, a naphtosultam derivative, is an antagonist at the 5-hydroxytryptamine2 (HT2) receptor. The sleep pattern of rats treated orally with RP 62203 was studied at doses ranging from 0.5 to 4 mg/kg. Following RP 62203 administration, the duration of deep nonrapid eye movement (NREM) sleep was found to increase at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg. The 5-HT2 receptor agonist DOI and the 5-HT1a receptor agonist 8 OH-DPAT induced a dose-related increase in wakefulness; treatment with RP 62203 reversed the enhancement of wakefulness produced by DOI but not that produced by 8 OH-DPAT. These data provide further evidence for the involvement of 5-HT2 receptors in the regulation of NREM sleep in rats. RP 62203 could therefore be of clinical interest in the management of sleep disorders, particularly those developing within a psychiatric context.[3] |
| References |
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| Additional Infomation |
LSM-2183 is a sulfonic acid derivative and a member of naphthalenes.
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| Molecular Formula |
C23H24FN3O2S
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|---|---|
| Molecular Weight |
425.52
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| Exact Mass |
425.157
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| Elemental Analysis |
C, 64.92; H, 5.69; F, 4.46; N, 9.88; O, 7.52; S, 7.53
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| CAS # |
127625-29-0
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| PubChem CID |
60785
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| Appearance |
Solid powder
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| Density |
1.331g/cm3
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| Boiling Point |
641.1ºC at 760mmHg
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| Flash Point |
341.5ºC
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| Vapour Pressure |
2.48E-16mmHg at 25°C
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| Index of Refraction |
1.659
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| LogP |
4.848
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
683
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1(C2=C([H])C([H])=C([H])C3C([H])=C([H])C([H])=C(C2=3)N1C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])N(C2C([H])=C([H])C(=C([H])C=2[H])F)C([H])([H])C1([H])[H])(=O)=O
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| InChi Key |
VGIGHGMPMUCLIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24FN3O2S/c24-19-8-10-20(11-9-19)26-16-14-25(15-17-26)12-3-13-27-21-6-1-4-18-5-2-7-22(23(18)21)30(27,28)29/h1-2,4-11H,3,12-17H2
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| Chemical Name |
3-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-2lambda6-thia-3-azatricyclo[6.3.1.04,12]dodeca-1(11),4,6,8(12),9-pentaene 2,2-dioxide
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| Synonyms |
RP-62203; RP 62203; 2H-Naphth[1,8-cd]isothiazole, 2-[3-[4-(4-fluorophenyl)-1-piperazinyl]propyl]-, 1,1-dioxide; CHEMBL83894; DTXSID8046743; 38QJ762ET6; Fananserin; RP62203
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~235.0 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.88 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3501 mL | 11.7503 mL | 23.5007 mL | |
| 5 mM | 0.4700 mL | 2.3501 mL | 4.7001 mL | |
| 10 mM | 0.2350 mL | 1.1750 mL | 2.3501 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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