4F 4PP oxalateSelective 5-HT2A antagonist CAS# 144734-36-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 144734-36-1 | SDF | Download SDF |
PubChem ID | 24745966 | Appearance | Powder |
Formula | C24H28FNO5 | M.Wt | 429.49 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO and to 20 mM in ethanol | ||
Chemical Name | (4-fluorophenyl)-[1-(4-phenylbutyl)piperidin-4-yl]methanone;oxalic acid | ||
SMILES | C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCCCC3=CC=CC=C3.C(=O)(C(=O)O)O | ||
Standard InChIKey | VUJYJCRJPFMHEM-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C22H26FNO.C2H2O4/c23-21-11-9-19(10-12-21)22(25)20-13-16-24(17-14-20)15-5-4-8-18-6-2-1-3-7-18;3-1(4)2(5)6/h1-3,6-7,9-12,20H,4-5,8,13-17H2;(H,3,4)(H,5,6) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | A selective 5-HT2A antagonist with almost as high affinity (Ki = 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki = 620 nM). |
4F 4PP oxalate Dilution Calculator
4F 4PP oxalate Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.3283 mL | 11.6417 mL | 23.2834 mL | 46.5669 mL | 58.2086 mL |
5 mM | 0.4657 mL | 2.3283 mL | 4.6567 mL | 9.3134 mL | 11.6417 mL |
10 mM | 0.2328 mL | 1.1642 mL | 2.3283 mL | 4.6567 mL | 5.8209 mL |
50 mM | 0.0466 mL | 0.2328 mL | 0.4657 mL | 0.9313 mL | 1.1642 mL |
100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.4657 mL | 0.5821 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Stimulation of 5-HT2A receptors on astrocytes in primary culture opens voltage-independent Ca2+ channels.[Pubmed:9542727]
Neurochem Int. 1998 Feb;32(2):153-62.
Mechanisms underlying the 5-HT2A receptor induction of intracellular Ca2+ mobilization and Ca2+ influx in type I astroglial cells in primary culture from newborn rat cerebral cortex were evaluated. The 5-HT-evoked Ca(2+)-transients, inhibited by the 5-HT2A antagonists ketanserin or 4-(4-fluorobenzoyl)-1-(4-phenylbutyl) piperidine oxalate, consisted of an initial peak caused by inositol 1,4,5-trisphosphate (IP3)-mediated Ca2+ release from internal stores, and a second sustained part which was due to Ca2+ transport over the plasma membrane. The responses were pertussis toxin-insensitive, suppressed by the phospholipase C inhibitor neomycin and were inhibited by the Ca(2+)-ATPase inhibitor thapsigargin. Furthermore, the responses were inhibited by the IP3 receptor antagonist heparin. When the second sustained part of the 5-HT-evoked response was studied, it was concluded that Ca2+ influx was not a result of opening of voltage operated calcium channels of either L, N or T-type. Instead it appeared that Ca2+ entered the cells through specialized voltage independent Ca2+ channels which were dependent of the IP3 production and subsequent Ca2+ release from internal stores. From this, we conclude that 5-HT opens Ca2+ channels in astrocytes which closely resemble depletion-operated Ca2+ channels (DOCCs).
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.[Pubmed:1479590]
J Med Chem. 1992 Dec 25;35(26):4903-10.
Ketanserin is the prototypic 5-HT2 serotonin antagonist; although it has been an important tool for the study of serotonin pharmacology, it has had relatively little impact on drug design because remarkably little is known about its structure-affinity relationships. Furthermore, ketanserin also binds at 5-HT1C receptors and even less is known about the influence of its structural features on 5-HT1C receptor affinity. The present study reveals that the fluoro and carbonyl groups of the 4-fluorobenzoyl portion of ketanserin make small contributions to 5-HT2 binding and that the intact benzoylpiperidine moiety is an important feature. Ring-opening of the piperidine ring reduces affinity. Although the quinazoline-2,4-dione moiety also contributes to binding, it appears to play a smaller role and can be structurally simplified with retention of 5-HT2 affinity. N-(4-Phenylbutyl)-4-(4-fluorobenzoyl)piperidine (39), for example, binds with nearly the same affinity (Ki = 5.3 nM) as ketanserin (Ki = 3.5 nM). All of the compounds examined bind at 5-HT1C sites with lower affinity than ketanserin, and some of the simplified analogues bind with nearly 10 times the 5-HT2 versus 5-HT1C selectivity of ketanserin; however, none displays > 120-fold selectivity. Several of the compounds, such as the amide 32 and the urea 33 represent examples of new structural classes of 5-HT2 ligands.