| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Stepholidine targets dopamine D1 and D2 receptors. It acts as a mixed D1 receptor agonist and D2 receptor antagonist. Stepholidine also binds to the dopamine D1 receptor as an inhibitor and is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A.
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| ln Vitro |
Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. It binds to dopamine D1 and D2 receptors. Stepholidine is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. The compound has neuroprotective effects and inhibits heroin-induced reinstatement.
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| ln Vivo |
Stepholidine attenuates heroin self-administration and cue-induced reinstatement in vivo. It also elicits anti-dyskinesia effects. The compound has neuroprotective effects. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources.
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| Enzyme Assay |
The binding affinity of stepholidine to dopamine D1 and D2 receptors can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant dopamine receptors. Competition binding experiments are performed with increasing concentrations of stepholidine against a fixed concentration of a radiolabeled receptor-specific ligand. Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of stepholidine at dopamine D1 and D2 receptors is evaluated in vitro using cells expressing recombinant dopamine receptors. Cells are treated with increasing concentrations of stepholidine, and receptor-mediated signaling pathways (e.g., cAMP modulation) are measured. Agonist activity at D1 receptors and antagonist activity at D2 receptors are characterized.
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| Animal Protocol |
Stepholidine is administered to animal models of drug addiction or dyskinesia. In rodent models of heroin self-administration, stepholidine is given at various doses via intraperitoneal or oral routes. Drug-seeking behavior, reinstatement, and dyskinesia are assessed to evaluate efficacy.
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| ADME/Pharmacokinetics |
Stepholidine has a molecular formula of C19H21NO4 and a molecular weight of 327.38. It is a natural product. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of stepholidine is not extensively documented. As a dopamine receptor modulator, potential adverse effects may include those related to dopaminergic signaling, such as motor effects and psychiatric symptoms. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
l-Stepholidine has reportedly been found in Fibraurea recisa, Stephania yunnanensis, and other organisms with available data.
Stepholidine (CAS# 16562-13-3) is also known as L-Stepholidine or (-)-Stepholidine. It exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. Stepholidine attenuates heroin self-administration and cue-induced reinstatement, and elicits anti-dyskinesia effects. It also has neuroprotective effects. |
| Molecular Formula |
C19H21NO4
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|---|---|
| Molecular Weight |
327.38
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| Exact Mass |
327.147
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| CAS # |
16562-13-3
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| PubChem CID |
6917970
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
524.0±50.0 °C at 760 mmHg
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| Melting Point |
120-122ºC
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| Flash Point |
270.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.680
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| LogP |
2.16
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
447
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC1=C(C=C2[C@@H]3CC4=C(CN3CCC2=C1)C(=C(C=C4)O)OC)O
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| InChi Key |
JKPISQIIWUONPB-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C19H21NO4/c1-23-18-8-12-5-6-20-10-14-11(3-4-16(21)19(14)24-2)7-15(20)13(12)9-17(18)22/h3-4,8-9,15,21-22H,5-7,10H2,1-2H3/t15-/m0/s1
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| Chemical Name |
(13aS)-3,9-dimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline-2,10-diol
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| Synonyms |
(-)-Stepholidine L-Stepholidine Stepholidine
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~305.46 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 | 3.0546 mL | 15.2728 mL | 30.5455 mL | |
| 5 mM | 0.6109 mL | 3.0546 mL | 6.1091 mL | |
| 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 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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