| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Glemanserin targets the serotonin receptor 5-HT2A. It is a potent and selective antagonist for this receptor. Its Ki values for 5-HT2A are in the low nanomolar range across different species. Its selectivity for 5-HT2A over other serotonin receptors is not detailed.
|
|---|---|
| ln Vitro |
In vitro, Glemanserin binds to the 5-HT2A receptor with high affinity, as demonstrated by its Ki values. Its activity as a 5-HT2A antagonist is confirmed in receptor binding assays. It is a potent and selective antagonist for 5-HT2A.
|
| ln Vivo |
In male mice, glemanserin (MDL11939) decreases behavioral sensitization, withdrawal symptoms, and increases in locomotor activity [1].
In vivo, Glemanserin suppresses the induced increase in locomotor activity, behavioral sensitization, and withdrawal symptoms in male mice. These effects are consistent with its activity as a 5-HT2A antagonist. It is used in research to study the role of 5-HT2A receptors in behavior. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Glemanserin involve measuring its binding affinity to the 5-HT2A receptor. These assays typically use radiolabeled ligands and membrane preparations from cells expressing the receptor. The Ki values are determined from competition binding experiments.
|
| Cell Assay |
In vitro cell-based assays for Glemanserin involve studying its effects on 5-HT2A receptor-mediated signaling pathways in cells expressing the receptor. Its antagonist activity is confirmed by measuring its ability to block agonist-induced downstream signaling.
|
| Animal Protocol |
In vivo animal experiments for Glemanserin have been conducted in male mice to study its effects on locomotor activity, behavioral sensitization, and withdrawal symptoms. The compound is typically administered via injection, and its behavioral effects are measured.
|
| ADME/Pharmacokinetics |
Glemanserin has a molecular weight of 295.42 and a molecular formula of C20H25NO. Specific pharmacokinetic data, such as absorption, distribution, metabolism, and excretion, are not provided in the search results.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for Glemanserin is not provided in the search results. As a selective 5-HT2A antagonist, its toxicity profile would be related to its pharmacological activity. Further studies would be required for clinical development.
|
| References | |
| Additional Infomation |
Phenyl-[1-(2-phenylethyl)-4-piperidinyl]methanol is a primary amine.
Glemanserin is a potent and selective antagonist for the serotonin receptor 5-HT2A. It is used in research to study the role of 5-HT2A receptors in behavior and neurological disorders. It is also known as MDL 11939. It is a research compound and has not been approved for clinical use. |
| Molecular Formula |
C20H25NO
|
|---|---|
| Molecular Weight |
295.426
|
| Exact Mass |
295.194
|
| CAS # |
107703-78-6
|
| Related CAS # |
107703-79-7 (HCl);132553-86-7;162254-89-9 (oxalate);107703-78-6;
|
| PubChem CID |
71781
|
| Appearance |
White to off-white solid powder
|
| Density |
1.084g/cm3
|
| Boiling Point |
434.2ºC at 760mmHg
|
| Flash Point |
205.6ºC
|
| LogP |
3.612
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
22
|
| Complexity |
299
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AXNGJCOYCMDPQG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H25NO/c22-20(18-9-5-2-6-10-18)19-12-15-21(16-13-19)14-11-17-7-3-1-4-8-17/h1-10,19-20,22H,11-16H2
|
| Chemical Name |
phenyl-[1-(2-phenylethyl)piperidin-4-yl]methanol
|
| Synonyms |
Mdl 11939; MDL 11,939; Glemanserin
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~338.50 mM)
|
|---|---|
| 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 | 3.3849 mL | 16.9245 mL | 33.8490 mL | |
| 5 mM | 0.6770 mL | 3.3849 mL | 6.7698 mL | |
| 10 mM | 0.3385 mL | 1.6924 mL | 3.3849 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
