| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
5-HT2A Receptor 72 nM (IC50) 5-HT2C Receptor 103 nM (IC50) 5-HT2B Receptor 570 nM (IC50)
(-)-5-HT2C agonist-3 selectively targets the serotonin 2C receptor (5-HT2C). It functions as an agonist, meaning it binds to and activates the receptor, leading to the initiation of downstream signaling cascades. It shows a preference for the Gq signaling pathway, which is the primary transducer for 5-HT2C receptors. By activating 5-HT2C, this compound can modulate neurotransmitter release, affecting mood, appetite, and psychotic symptoms. |
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| ln Vitro |
(-)-5-HT2C agonist-3 demonstrates potent and selective in vitro activity at the 5-HT2C receptor. It has an EC50 value of 103 nM for the 5-HT2C receptor, indicating high potency【3L12-L13, L16-L17】. It has lower activity at other related receptors, with EC50 values of 570 nM for 5-HT2B and 72 nM for 5-HT2A. This selectivity profile is crucial for minimizing off-target effects and provides a distinct functional fingerprint for research into specific receptor-mediated behaviors.
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| ln Vivo |
Specific in vivo activity data for (-)-5-HT2C agonist-3 is not detailed. However, as a selective 5-HT2C agonist, it is designed for in vivo research into the treatment of psychiatric disorders, as indicated by its use in antipsychotic research. 5-HT2C agonists are known to have effects on psychosis, anxiety, and impulse control in animal models. The compound is being investigated as a potential antipsychotic medication.
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| Enzyme Assay |
The binding affinity and selectivity can be determined using standard radioligand binding assays with membranes from cells overexpressing human serotonin receptors. Procedure: Membranes from CHO-K1 cells stably expressing human 5-HT2C receptors are incubated with a fixed concentration of a high-affinity radioligand (e.g., [3H]Mesulergine or [125I]DOI) for 60 minutes at 27degC in binding buffer (50 mM Tris-HCl, pH 7.4, 10 mM MgCl2, 0.1% BSA, 0.1% ascorbic acid). Varying concentrations of (-)-5-HT2C agonist-3 (0.01 nM to 10 microM) are added to compete for binding. Non-specific binding is defined with 10 microM mianserin. Bound radioligand is separated by filtration through GF/B filters and counted by liquid scintillation. The inhibitory constant (Ki) is calculated from the IC50 using the Cheng-Prusoff equation.
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| Cell Assay |
Functional selectivity and potency are measured by calcium mobilization assays, as 5-HT2C receptor is Gq-coupled. Procedure: CHO-K1 cells stably expressing the human 5-HT2C receptor are seeded in 384-well plates (20,000 cells/well) and incubated overnight. On the assay day, cells are loaded with a calcium-sensitive dye (e.g., Fluo-4-AM) for 60 minutes at 37degC. The plates are then placed in a fluorometric imaging plate reader (FLIPR). Following the addition of varying concentrations of (-)-5-HT2C agonist-3 (e.g., 0.01 nM to 100 microM), the change in fluorescence (excitation 485 nm, emission 525 nm) is measured. The EC50 value (103 nM) is calculated from the peak fluorescence signal as a function of the compound's concentration. A parallel set of experiments is run on cells expressing 5-HT2A and 5-HT2B receptors to determine selectivity.
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| Animal Protocol |
The in vivo effects of (-)-5-HT2C agonist-3 can be assessed in a mouse model for antipsychotic-like activity, such as the prepulse inhibition (PPI) of the startle reflex. Procedure: Male C57BL/6J mice (8-10 weeks) are administered (-)-5-HT2C agonist-3 (dissolved in a suitable vehicle like 10% DMSO/90% saline) intraperitoneally at doses of 0.1, 0.3, and 1 mg/kg, 30 minutes prior to testing. The PPI test involves placing a mouse in a startle chamber. After a 5-minute acclimation period, the mouse is exposed to a series of startle pulse-alone trials (e.g., 120 dB) and prepulse + startle trials (e.g., a 74, 78, or 82 dB prepulse followed by a 120 dB startle). The percentage of prepulse inhibition is calculated. A reversal of a PPI deficit induced by a psychotomimetic drug (e.g., dizocilpine or amphetamine) is interpreted as an antipsychotic-like effect.
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| ADME/Pharmacokinetics |
Specific PK data for (-)-5-HT2C agonist-3 is not provided in the search results. As a small molecule (MW 351.84) with a halogen (fluorine and chlorine) substituents, it is expected to be designed for metabolic stability and good blood-brain barrier (BBB) penetration. The presence of a fluorine atom is a common strategy in medicinal chemistry to improve metabolic stability and bioavailability. Further ADME studies would be required to characterize its PK profile in preclinical species.
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| Toxicity/Toxicokinetics |
Specific toxicology data for (-)-5-HT2C agonist-3 is not available. As an agonist of the 5-HT2C receptor, potential on-target effects include nausea and decreased appetite, which are also common side effects of serotonergic drugs. The selectivity over the 5-HT2B receptor (EC50 570 nM) is important as 5-HT2B agonism is associated with cardiac valvulopathy. The compound is for research use only and not intended for human use. Standard safety precautions should be followed.
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| References | |
| Additional Infomation |
The 5-HT2C receptor is a G protein-coupled receptor (GPCR) that is widely expressed in the central nervous system, particularly in the choroid plexus, hippocampus, and hypothalamus. It plays a crucial role in the regulation of mood, anxiety, feeding behavior, and the control of psychotic symptoms. This has made it a major drug target for schizophrenia, depression, and obesity. (-)-5-HT2C agonist-3, with its Gq signaling preference and selectivity profile, is a valuable tool for dissecting the specific contributions of the 5-HT2C receptor to behavior and for developing novel antipsychotic medications with fewer side effects than current treatments. This product is for research use only.
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| Molecular Formula |
C19H23CLFNO2
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|---|---|
| Molecular Weight |
351.84
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| Exact Mass |
351.14
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| CAS # |
2104810-16-2
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| PubChem CID |
137640062
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| Appearance |
Solid Powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
24
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| Complexity |
367
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=C(C=C(C=C1)F)[C@H]2C[C@@H]2CNCC3=CC=CC=C3OC.Cl
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| InChi Key |
KNTRIIJGIFKPED-XMZRARIVSA-N
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| InChi Code |
InChI=1S/C19H22FNO2.ClH/c1-22-18-6-4-3-5-13(18)11-21-12-14-9-16(14)17-10-15(20)7-8-19(17)23-2;/h3-8,10,14,16,21H,9,11-12H2,1-2H3;1H/t14-,16+;/m1./s1
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| Chemical Name |
1-[(1S,2S)-2-(5-fluoro-2-methoxyphenyl)cyclopropyl]-N-[(2-methoxyphenyl)methyl]methanamine;hydrochloride
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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 Note: (1). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~284.22 mM; with ultrasonication)
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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 | 2.8422 mL | 14.2110 mL | 28.4220 mL | |
| 5 mM | 0.5684 mL | 2.8422 mL | 5.6844 mL | |
| 10 mM | 0.2842 mL | 1.4211 mL | 2.8422 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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