| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Ki: 11.2 nM (dopamine D2 receptor)[1]
Dopamine D2 receptor agonist-2 targets the human D2L receptor, acting as a partial agonist. It has a Ki of 11.2 nM. The compound functions as an agonist by inhibiting forskolin-stimulated cAMP production and displacing [³H]spiperone from the receptor. |
|---|---|
| ln Vitro |
In cell-free receptor binding assays, Dopamine D2 receptor agonist-2 displaces [³H]spiperone from the human D2L receptor with a Ki of 11.2 nM. This confirms its high affinity for the receptor. Its activity as an agonist is demonstrated by its ability to activate D2 receptor-mediated signaling pathways. In cellular functional assays, Dopamine D2 receptor agonist-2 acts as a partial agonist at the dopamine D2 receptor. It inhibits forskolin-stimulated cAMP production, confirming its ability to activate the receptor and its downstream signaling. Its partial agonism is characterized by a lower maximal efficacy compared to full agonists.
|
| ln Vivo |
In vivo, Dopamine D2 receptor agonist-2 is used in research on antipsychotic mechanisms. Its partial agonist activity at the D2 receptor is thought to be relevant for the treatment of psychosis, as partial agonists can stabilize dopaminergic signaling without causing the side effects associated with full antagonists or full agonists.
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| Enzyme Assay |
Cell-free receptor binding assays for Dopamine D2 receptor agonist-2 are performed using membrane preparations from cells expressing the human dopamine D2L receptor. Radioligand displacement studies use [³H]spiperone. Membranes are incubated with varying concentrations of the compound and the radioligand, followed by filtration and scintillation counting. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cellular functional assays for Dopamine D2 receptor agonist-2 are conducted using cells expressing the human D2L receptor. Cells are pre-incubated with the compound, then stimulated with forskolin to increase cAMP levels. The compound's ability to inhibit forskolin-stimulated cAMP production is measured. EC50 values are determined from concentration-response curves.
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| Animal Protocol |
In vivo studies for Dopamine D2 receptor agonist-2 are not detailed in the available literature. As a research compound, its effects would be studied in animal models of psychosis or other dopamine-related disorders.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Dopamine D2 receptor agonist-2 are not extensively reported. As a small-molecule D2 receptor ligand, it is expected to be capable of crossing the blood-brain barrier. Detailed PK parameters are not available in the provided sources.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for Dopamine D2 receptor agonist-2 are limited. As a research compound, comprehensive toxicological evaluations would be necessary for its development as a therapeutic agent.
|
| References | |
| Additional Infomation |
Dopamine D2 receptor agonist-2 is a research compound used to study dopamine D2 receptor pharmacology and antipsychotic mechanisms. Its partial agonist activity makes it a valuable tool for understanding the role of D2 receptors in neuropsychiatric disorders. It is not approved for clinical use.
|
| Exact Mass |
519.163
|
|---|---|
| CAS # |
1610591-93-9
|
| PubChem CID |
90645289
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
34
|
| Complexity |
667
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC(=NC2=C1C(=C(S2)C(=O)NCCCCCN3CCN(CC3)C4=C(C(=CC=C4)Cl)Cl)N)C
|
| InChi Key |
YEDOJNFKHXVFHD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H31Cl2N5OS/c1-16-15-17(2)30-25-20(16)22(28)23(34-25)24(33)29-9-4-3-5-10-31-11-13-32(14-12-31)19-8-6-7-18(26)21(19)27/h6-8,15H,3-5,9-14,28H2,1-2H3,(H,29,33)
|
| Chemical Name |
3-amino-N-[5-[4-(2,3-dichlorophenyl)piperazin-1-yl]pentyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (192.12 mM)
|
|---|---|
| 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.) |
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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