| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
5-HT2A (serotonin 2A) receptor; alpha-1 adrenergic receptor. Lidanserin acts as a dual antagonist, blocking both 5-HT2A serotonin receptors and alpha-1 adrenergic receptors. By blocking 5-HT2A receptors, it reduces serotonin-mediated vasoconstriction and platelet aggregation. Alpha-1 adrenergic antagonism contributes to vasodilation and blood pressure reduction.
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|---|---|
| ln Vitro |
Lidanserin is an antagonist of both α1-adrenergic and 5-HT2A receptors. As an antihypertensive medication, ridanserin is utilized.
Lidanserin is an antagonist of the combined 5-HT2A and alpha-1 adrenergic receptors in vitro. It has been shown to bind with high affinity to these receptors and block serotonin- and norepinephrine-mediated signaling. The compound demonstrates favorable receptor selectivity and has been used in binding assays to study receptor pharmacology. Its in vitro activity has been characterized in various radioligand binding and functional assays. |
| ln Vivo |
In vivo, Lidanserin has been studied for its antihypertensive and hemodynamic effects in preclinical models. It reduces blood pressure through vasodilation mediated by alpha-1 receptor blockade and improves vascular function through 5-HT2 receptor antagonism. Although it showed favorable hemodynamic effects in preclinical studies, it did not advance to clinical use. The compound remains valuable for studying serotonin receptor pharmacology and cardiovascular therapeutics.
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| Enzyme Assay |
In vitro receptor binding assays for Lidanserin typically involve competition binding experiments using radiolabeled ligands such as [3H]-ketanserin for 5-HT2A receptors or [3H]-prazosin for alpha-1 adrenergic receptors. Membranes are prepared from cells expressing the respective receptors. Lidanserin is incubated at varying concentrations, and bound radioactivity is measured. IC50 or Ki values are calculated from displacement curves. Functional assays may also be performed to measure receptor-mediated signaling.
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| Cell Assay |
In vitro cell-based assays for Lidanserin are not extensively documented. When performed, they typically involve cells expressing 5-HT2A or alpha-1 adrenergic receptors. Calcium mobilization or IP3 accumulation assays may be used to measure receptor activation. Lidanserin's antagonist activity is assessed by its ability to block agonist-induced responses. Cells are cultured in appropriate media and treated with Lidanserin prior to agonist stimulation.
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| Animal Protocol |
In vivo animal studies for Lidanserin have been conducted in hypertensive rodent models. The compound is typically administered orally or intravenously, and blood pressure is measured using telemetry or tail-cuff methods. Hemodynamic parameters such as heart rate and vascular resistance are also assessed. Doses are optimized to achieve antihypertensive effects. The compound's effects on platelet aggregation may also be evaluated in ex vivo assays.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Lidanserin are limited in publicly available sources. The compound has a molecular weight of 454.53 and a molecular formula of C26H31FN2O4. It is typically supplied as a solid with a purity of ≥95%. Detailed ADME parameters such as half-life, bioavailability, and protein binding are not extensively documented. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicological data for Lidanserin are limited. The compound was developed as a potential antihypertensive agent but did not advance to clinical use. It is intended for research purposes only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the compound. No specific toxicity data are available in publicly accessible sources.
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| References | |
| Additional Infomation |
Lidanserin (ZK-33,839) is a dual 5-HT2A and alpha-1 adrenergic receptor antagonist. It was investigated as an antihypertensive compound with vasodilatory and platelet antiaggregatory properties. Although it showed preclinical promise, it did not advance to clinical use. The compound is now used primarily as a research tool for studying serotonin and adrenergic receptor pharmacology. Its molecular formula is C26H31FN2O4, and its molecular weight is 454.53.
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| Molecular Formula |
C26H31FN2O4
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|---|---|
| Molecular Weight |
454.53374
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| Exact Mass |
454.227
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| CAS # |
73725-85-6
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| PubChem CID |
68919
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.192g/cm3
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| Boiling Point |
658.6ºC at 760 mmHg
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| Flash Point |
352.1ºC
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| Index of Refraction |
1.56
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| LogP |
4.068
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
646
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JDYWZVJXSMADHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31FN2O4/c1-32-23-8-5-20(21-16-25(30)28-17-21)15-24(23)33-14-2-11-29-12-9-19(10-13-29)26(31)18-3-6-22(27)7-4-18/h3-8,15,19,21H,2,9-14,16-17H2,1H3,(H,28,30)
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| Chemical Name |
4-(3-(3-(4-(4-fluorobenzoyl)piperidin-1-yl)propoxy)-4-methoxyphenyl)pyrrolidin-2-one
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| Synonyms |
ZK 33839 ZK-33839 ZK33839 Lidanserinum Lidanserine Lidanserina
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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) |
DMSO : ~50 mg/mL (~110.00 mM)
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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 | 2.2001 mL | 11.0004 mL | 22.0007 mL | |
| 5 mM | 0.4400 mL | 2.2001 mL | 4.4001 mL | |
| 10 mM | 0.2200 mL | 1.1000 mL | 2.2001 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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