| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Tropanserin targets the serotonin 5-HT3 receptor. It acts as a potent and selective antagonist, binding to the 5-HT3 receptor and blocking the action of serotonin. The 5-HT3 receptor is a ligand-gated ion channel that is involved in various physiological processes, including nausea and vomiting (emesis), pain perception, and gastrointestinal motility. By blocking this receptor, tropanserin modulates serotonin-mediated responses. Its selectivity for the 5-HT3 receptor makes it a valuable tool for studying the specific role of this receptor in various conditions.
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| ln Vitro |
In vitro, tropanserin has been shown to be a potent antagonist of the 5-HT3 receptor. In cell-based assays using cells expressing the 5-HT3 receptor, the compound inhibits serotonin-induced ion currents. This has been demonstrated using electrophysiological techniques, such as patch-clamp. The compound's affinity and selectivity for the 5-HT3 receptor have been confirmed in radioligand binding assays.
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| ln Vivo |
In vivo, tropanserin has been studied for its effects on emesis and other serotonin-mediated processes. It has been shown to have antiemetic effects in animal models. The compound's ability to block 5-HT3 receptors in the central and peripheral nervous systems makes it a candidate for studying conditions such as nausea, vomiting, and gastrointestinal disorders. It has anxiolytic activity and is used to treat depression and cognitive disorders in research.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for tropanserin involve studying its binding affinity for the 5-HT3 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the 5-HT3 receptor. The compound is incubated with a radiolabeled ligand, such as [3H]GR65630, and the displacement of the ligand is measured to determine the Ki or IC50. These assays confirm the compound's affinity for the 5-HT3 receptor. Selectivity is assessed by testing the compound against other serotonin receptors and other neurotransmitter receptors.
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| Cell Assay |
In vitro cell-based assays for tropanserin are performed using cells that express the 5-HT3 receptor. Cells are loaded with a calcium-sensitive fluorescent dye or subjected to patch-clamp electrophysiology. The inhibition of serotonin-induced calcium influx or ion currents by tropanserin is measured as a functional readout of receptor antagonism. These assays confirm the compound's potency and selectivity as a 5-HT3 receptor antagonist.
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| Animal Protocol |
In vivo animal experiments for tropanserin are conducted using rodent models of emesis, such as the ferret or the shrew, which are sensitive to emetic stimuli. The compound is administered, and its ability to prevent vomiting induced by various emetic agents, such as cisplatin or copper sulfate, is assessed. The compound's effects on gastrointestinal motility and pain perception are also studied in appropriate models.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tropanserin have been characterized to support its use as a research tool. The compound has a molecular weight of 273.37 and a molecular formula of C17H23NO2. It is a solid with a purity of >99%. The compound is typically administered orally or intraperitoneally in animal studies. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples. The compound's ability to cross the blood-brain barrier is important for its effects on central nervous system functions.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tropanserin are characteristic of a research compound. As a 5-HT3 receptor antagonist, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses. Common side effects may include headache, constipation, and dizziness, which are typical of 5-HT3 receptor antagonists. The compound's long-term safety profile requires further evaluation.
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| Additional Infomation |
Tropine 3,5-dimethylbenzoate is a tropane alkaloid composed of tropine molecules, in which the hydrogen atom on the hydroxyl group is replaced by a 3,5-dimethylbenzoyl group. It is a serotonin antagonist. It is both a tropane alkaloid and a benzoate. Its function is related to tropine. Tropine has been reported to exist in Goniorrhachis marginata, Calycophyllum spruceanum, and several other organisms with relevant data.
Other information: Tropanserin is a research compound used to study the role of the 5-HT3 receptor in emesis, neurotransmission, and other physiological processes. It is a potent and selective 5-HT3 receptor antagonist. The compound is available from chemical suppliers for preclinical research purposes. Its CAS number is 85181-40-4. |
| Molecular Formula |
C17H23NO2
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|---|---|
| Molecular Weight |
273.37
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| Exact Mass |
273.173
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| CAS # |
85181-40-4
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| PubChem CID |
68600
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.023
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
346
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC(=CC(=C1)C(=O)OC2CC3CCC(C2)N3C)C
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| InChi Key |
HDDNYFLPWFSBLN-XYPWUTKMSA-N
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| InChi Code |
InChI=1S/C17H23NO2/c1-11-6-12(2)8-13(7-11)17(19)20-16-9-14-4-5-15(10-16)18(14)3/h6-8,14-16H,4-5,9-10H2,1-3H3/t14-,15+,16?
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| Chemical Name |
[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3,5-dimethylbenzoate
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| Synonyms |
MDL 72422; MDL-72422; Tropanserin
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6580 mL | 18.2902 mL | 36.5805 mL | |
| 5 mM | 0.7316 mL | 3.6580 mL | 7.3161 mL | |
| 10 mM | 0.3658 mL | 1.8290 mL | 3.6580 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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