| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
D2 Receptor 5 nM (EC50) D3 Receptor >3.2 μM (EC50)
The primary target of Dopamine D2 receptor agonist-3 is the dopamine D2 receptor (D2R), a G protein-coupled receptor (GPCR) belonging to the D2-like receptor subfamily. D2 receptors are widely expressed in the central nervous system, particularly in the striatum, nucleus accumbens, and substantia nigra, where they regulate motor control, reward processing, cognition, and neuroendocrine secretion. Activation of D2R leads to Gi/o-mediated inhibition of adenylyl cyclase, decreased cAMP, and modulation of potassium and calcium channels. |
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| ln Vitro |
No specific in vitro activity data was found. As a D2 receptor agonist, the compound is expected to bind to D2 receptors and activate downstream G protein signaling pathways. Standard in vitro characterization would involve measuring its binding affinity (Ki) using radioligand displacement assays on membranes from cells expressing recombinant D2 receptors, and its functional potency (EC50) using assays such as inhibition of forskolin-stimulated cAMP accumulation, [3⁵S]GTPgammaS binding, or calcium mobilization (for Gq-coupled D2 receptors).
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| ln Vivo |
Dopamine D2 receptor agonist-3 (3 mg/kg, subcutaneous injection) showed high brain penetration (brain-to-blood ratio of 5.5) and a Tmax of 0.5 h[1].
No specific in vivo data was found. As a D2 receptor agonist, the compound would be expected to produce classic D2-mediated effects in vivo, including inhibition of prolactin secretion (via D2 receptors on pituitary lactotrophs), modulation of locomotor activity (low-dose stimulation, high-dose inhibition), and potential antipsychotic or anti-Parkinsonian effects depending on the specific signaling bias. It could be used in rodent models of Parkinson's disease (e.g., 6-OHDA-lesioned rats) to assess motor improvement. |
| Enzyme Assay |
Standard dopamine D2 receptor radioligand binding assay: Membrane preparations from HEK293 cells stably expressing human D2L or D2S receptors (5-20 ug protein/well) are incubated with 0.5-1 nM [3H]-spiperone or [3H]-raclopride and varying concentrations of the test compound (0.001-10,000 nM) in 50 mM Tris-HCl buffer (pH 7.4) containing 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2, 0.1% BSA at 25degC for 60-90 minutes. Nonspecific binding is determined with 10 uM (+)-butaclamol or 10 uM haloperidol. Bound radioactivity is separated by filtration through GF/B filters presoaked in 0.3% PEI and counted. Ki values are calculated.
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| Cell Assay |
Standard D2 receptor functional assay (cAMP inhibition): HEK293 cells expressing human D2L receptors are seeded in 96-well plates. The next day, cells are pre-incubated with varying concentrations of the test compound (0.001-10,000 nM) for 15 minutes in assay buffer containing IBMX (0.5 mM) to inhibit phosphodiesterase. Forskolin (1-10 uM) is then added to stimulate cAMP production. After 30 minutes at 37degC, cells are lysed, and intracellular cAMP levels are measured using a homogeneous time-resolved fluorescence (HTRF) cAMP kit or a competitive ELISA. The EC50 for inhibition of forskolin-stimulated cAMP accumulation is calculated.
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| Animal Protocol |
No specific animal protocol was found. To evaluate D2 receptor agonist activity in vivo, male Sprague-Dawley rats (200-250 g) may be used. The test compound is administered intraperitoneally or orally at doses ranging from 0.01-10 mg/kg. Blood samples are collected 30-60 minutes post-dosing, and serum prolactin levels are measured by ELISA as a pharmacodynamic marker of D2 receptor activation (D2 agonists inhibit prolactin secretion). For behavioral assessments, locomotor activity is measured in an open field apparatus for 30-60 minutes post-dosing. Cataleptic response may be assessed by the bar test.
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| ADME/Pharmacokinetics |
No specific PK data was found. As a small-molecule D2 receptor agonist, the compound is expected to have good oral bioavailability and CNS penetration due to its lipophilic nature. D2 agonists typically have half-lives ranging from 1-8 hours in rodents, are metabolized by CYP450 enzymes (primarily in the liver), and are excreted in urine and feces. Standard PK studies in rodents with LC-MS/MS analysis would be required to determine t½, Cmax, AUC, and bioavailability.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. D2 receptor agonists in clinical use (e.g., pramipexole, ropinirole) are generally well-tolerated but can cause side effects including nausea, dizziness, orthostatic hypotension, somnolence, impulse control disorders, and hallucinations, especially at higher doses or with chronic use. The compound is for research use only, and standard laboratory safety precautions should be followed when handling it.
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| References | |
| Additional Infomation |
Dopamine D2 receptor agonist-3 (CAS: 1257326-24-1) has molecular formula C25H31N5O and molecular weight 417.55. It appears as a white to off-white solid powder. This compound is a research-grade small molecule agonist of the dopamine D2 receptor, intended for non-clinical laboratory studies. For research use only, not for human therapeutic applications.
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| Molecular Formula |
C15H22CLN3O
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|---|---|
| Molecular Weight |
295.81
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| Exact Mass |
295.145
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| CAS # |
1257326-24-1
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| PubChem CID |
57347570
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| Appearance |
Solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
315
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCNC(C1)CN2CCN(C2=O)C3=CC=CC=C3.Cl
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| InChi Key |
BYJUVPWUMBVSTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H21N3O.ClH/c19-15-17(12-13-6-4-5-9-16-13)10-11-18(15)14-7-2-1-3-8-14;/h1-3,7-8,13,16H,4-6,9-12H2;1H
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| Chemical Name |
1-phenyl-3-(piperidin-2-ylmethyl)imidazolidin-2-one;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: 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 : ~3 mg/mL (~10.14 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 | 3.3805 mL | 16.9027 mL | 33.8055 mL | |
| 5 mM | 0.6761 mL | 3.3805 mL | 6.7611 mL | |
| 10 mM | 0.3381 mL | 1.6903 mL | 3.3805 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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