| 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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| 250mg | |||
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| Targets |
Dopamine D2 receptor; dopamine D3 receptor; serotonin 5-HT1A receptor. Adoprazine acts as a high potency dopamine D2 receptor antagonist and an efficacious serotonin 5-HT1A receptor agonist. It is a complete antagonist of D2 and D3 receptors with pA2 values of 9.3 at hD2 and 8.9 at hD3 receptors. It also has affinity for D4 receptors (pKi 8.0).
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| ln Vitro |
Adoprazine (SLV313) SLV313) exhibits a strong affinity for human recombinant D2, D3, D4, 5-HT2B, and 5-HT1A receptors, with pKs of 8.4, 8.4, 8.0, 7.9 and 9.1 respectively [1]. Adoprazine (SLV313) has a pKB value of 8.5 and an Emax value (% impact of 10 μM 5-HT) of 73, making it a highly potent serotonin 5-HT1A receptor agonist as well as a highly potent antagonist of the dopamine D2 receptor [2].
Adoprazine demonstrates high potency dopamine D2 receptor antagonist activity and efficacious serotonin 5-HT1A receptor agonist activity in vitro. It has an Emax value of 73 for 5-HT1A receptor agonism and a pKB value of 8.5. The compound exhibits pA2 values of 9.3 at hD2 receptors and 8.9 at hD3 receptors. Its binding affinity for D4 receptors is pKi 8.0. |
| ln Vivo |
Adorazine (SLV313) (0.1-10 mg/kg; oral; single dosage) is adequate to lower extracellular 5-HT and enhance dopamine levels in the nucleus accumbens in a dose- and time-dependent manner [1].
In vivo, Adoprazine is a potential atypical antipsychotic with combined dopamine D2 antagonist and serotonin 5-HT1A agonist properties. It has been studied for its antipsychotic effects in animal models and its potential for treating schizophrenia and related disorders. Detailed in vivo efficacy data are limited in publicly available sources. |
| Enzyme Assay |
In vitro receptor binding assays for Adoprazine involve competition binding experiments using radiolabeled ligands for dopamine D2, D3, and serotonin 5-HT1A receptors. Membranes are prepared from cells expressing the respective receptors. Adoprazine is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure D2 receptor antagonism and 5-HT1A receptor agonism.
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| Cell Assay |
Cellular assays for Adoprazine involve culturing cells expressing dopamine D2, D3, or serotonin 5-HT1A receptors. Cells are treated with Adoprazine at varying concentrations. D2 receptor antagonism is assessed by measuring inhibition of dopamine-induced cAMP reduction. 5-HT1A receptor agonism is assessed by measuring activation of G protein-coupled receptor signaling, such as calcium mobilization or GTPγS binding.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (275-350 g) [1]
Doses: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg Route of Administration: Oral; single outcome Experimental Results: Causes a dose- and time-dependent increase in extracellular DA, DOPAC and HVA levels. On the contrary, it resulted in a decrease in 5-HT levels without a change in 5-HIAA levels. In vivo animal studies for Adoprazine are conducted in rodent models of schizophrenia or psychosis. The compound is typically administered orally or intraperitoneally. Behavioral assays such as amphetamine-induced hyperlocomotion, prepulse inhibition, and conditioned avoidance response are used to assess antipsychotic activity. Dosing regimens vary depending on the study objectives. |
| ADME/Pharmacokinetics |
Adoprazine has a molecular weight of 405.46 g/mol and a molecular formula of C24H24FN3O2. It is soluble in DMSO at 50 mg/mL (123.32 mM) and insoluble in water (<0.1 mg/mL). The compound should be stored at -20°C protected from light. It is available with a purity of >98%. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Adoprazine is generally considered safe for research use at appropriate concentrations. Comprehensive toxicological data are limited as the compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the compound.
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| References |
[1]. Andrew C McCreary, et al. SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsych
[2]. Liesbeth A Bruins Slot, et al. Differential profile of antipsychotics at serotonin 5-HT1A and dopamine D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70. |
| Additional Infomation |
Adoprazine (SLV313) is a potential atypical antipsychotic with potent D2/D3 receptor antagonist and 5-HT1A receptor agonist properties. It has pA2 values of 9.3 at hD2 and 8.9 at hD3 receptors. The compound is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C24H24N3O2F
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| Molecular Weight |
405.46466
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| Exact Mass |
405.185
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| CAS # |
222551-17-9
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| PubChem CID |
9887537
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.984
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
537
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=C(C2=CN=CC(CN3CCN(C4=C5OCCOC5=CC=C4)CC3)=C2)C=C1
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| InChi Key |
IUVSEUFHPNITEQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24FN3O2/c25-21-6-4-19(5-7-21)20-14-18(15-26-16-20)17-27-8-10-28(11-9-27)22-2-1-3-23-24(22)30-13-12-29-23/h1-7,14-16H,8-13,17H2
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| Chemical Name |
1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)pyridin-3-yl]methyl]piperazine
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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 (~123.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 30 mg/mL (73.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 300.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 3 mg/mL (7.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4663 mL | 12.3317 mL | 24.6633 mL | |
| 5 mM | 0.4933 mL | 2.4663 mL | 4.9327 mL | |
| 10 mM | 0.2466 mL | 1.2332 mL | 2.4663 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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