Dopamine Receptors

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  1. partial dopamine D2 and D3 receptor agonist

    Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.
  2. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  3. D1/D5 receptor full agonist

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  4. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  5. dopamine reuptake inhibitor

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM).
  6. D1-like dopamine receptor (D1/D5) agonist

    Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity.
  7. dopamine reuptake inhibitor

    GBR 12935 is a potent, and selective dopamine reuptake inhibitor.
  8. dopamine D2 receptor antagonist

    Haloperidol D4 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
  9. dopamine D2 receptor antagonist

    Haloperidol-d4-1 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.

  10. dopamine D4 receptor partial agonist

    Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
  11. 5-HT / dopamine receptor antagonist

    Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  12. dopamine D2/D3 receptor antagonist

    Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
  13. D2R antagonist

    Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist.
  14. analgesic agent

    Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  15. analgesic agent

    Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  16. dopamine D1-like receptor antagonist

    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively.
  17. Dopamine Precursor

    L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
  18. 5-HT5A Receptor Antagonist

    SB-699551 free base is a selective antagonist of the 5-HT5A receptor, characterized by a pKi of 8.2 nM, which allows for effective brain penetration. It exhibits significant selectivity over various serotonin receptor subtypes, dopamine receptors, and the α1B adrenoceptor. This compound disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, influencing the phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. SB-699551 free base is valuable for research into anxiety, breast cancer, and Alzheimer's disease.
  19. 5-HT5A Antagonist

    SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease.
  20. Dopamine β-hydroxylase Inhibitor

    Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers.
  21. Dopamine D2/D3 Agonist

    Piribedil is a potent and orally active agonist of dopamine D2 and D3 receptors, also exhibiting antagonistic activity at α2-adrenoceptors. Additionally, Piribedil inhibits MLL1 methyltransferase with an EC50 value of 0.18 μM. This compound is primarily utilized in research focused on Parkinson’s disease, circulatory disorders, and certain cancers, making it a valuable tool for exploring dopaminergic pathways and related therapeutic strategies.
  22. MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
  23. Dopamine D2/D3 Agonist

    Piribedil maleate is a potent agonist of dopamine D2 and D3 receptors, with additional activity as an α2-adrenoceptor antagonist. It has been shown to inhibit MLL1 methyltransferase activity with an EC50 of 0.18 μM. Piribedil maleate is of interest for research applications related to Parkinson’s disease, circulatory disorders, and various cancers.
  24. Dopamine D2/D3 Agonist

    Piribedil hydrochloride is a potent agonist of dopamine D2 and D3 receptors, serving as a valuable tool for investigating dopaminergic signaling pathways. In addition to its agonistic activity, it acts as an antagonist at α2-adrenoceptors and inhibits MLL1 methyltransferase with an EC50 of 0.18 μM. This compound is primarily utilized in research related to Parkinson's disease, circulatory disorders, and certain types of cancer, making it an important reagent for studies focused on neurodegeneration and tumor biology.
  25. Dopamine D2/D3 Agonist

    Piribedil dihydrochloride is a potent dopamine D2 and D3 agonist, also functioning as an antagonist at α2-adrenoceptors. This compound exhibits inhibitory activity on MLL1 methyltransferase with an EC50 of 0.18 μM. It is primarily utilized in research focused on Parkinson's disease, circulatory disorders, and various types of cancers.
  26. Stable Isotope

    Dopamine-d5 hydrochloride is a deuterium-labeled analogue of dopamine, a catecholamine neurotransmitter primarily synthesized in the substantia nigra, ventral tegmental area, and hypothalamus. This compound retains the essential biological functions of dopamine, including its interaction with D2 dopamine receptors, which mediates the endocytosis of VEGFR2, a key process in angiogenesis. Dopamine-d5 hydrochloride is valuable for research applications involving neurotransmitter dynamics, neuropharmacology, and angiogenic pathways.
  27. Antipsychotic Agent

    Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml.
  28. Dopamine Receptor Antagonist

    Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes.
  29. Stable Isotope

    Quetiapine Sulfoxide-d8 is a deuterated analog of Quetiapine sulfoxide, a primary metabolite of the second-generation antipsychotic Quetiapine. This compound acts as a 5-HT receptor agonist and dopamine receptor antagonist, playing a critical role in the pharmacokinetic studies of Quetiapine metabolism. Quetiapine Sulfoxide-d8 is commonly utilized in research applications involving drug metabolism, pharmacology, and analytical chemistry, particularly in the development and validation of quantitation methods in biological samples.
  30. Pergolide Metabolite

    Pergolide sulfone is a metabolite of Pergolide, primarily acting as a dopamine receptor agonist. This compound exhibits significant dopaminergic activity, making it relevant for research into Parkinson's disease and other neurological disorders. Pergolide sulfone can be utilized in studies investigating the pharmacological profiles of dopamine receptor interactions and their implications in neurodegenerative conditions.
  31. Drug Metabolite

    Reduced Haloperidol, a primary metabolite of Haloperidol, functions as a dopamine receptor antagonist. It exhibits significant antipsychotic activity, primarily utilized in research related to schizophrenia and other psychotic disorders. This compound is instrumental in studies investigating the modulation of neurotransmitter systems, aiding in the reduction of hallucinations and delusions associated with these conditions.
  32. A2AR-D2R Heteromer Ligand

    Heterobivalent ligand-1 is a potent heterobivalent ligand targeting the Adenosine A2A-dopamine D2 receptor heteromer, exhibiting binding affinities of 2.1 nM for A2AR and 0.13 nM for D2R. This compound is valuable for studying receptor heteromerization and signal transduction in neurological research. Its unique design enables exploration of the functional interplay between these receptors in various biological contexts.
  33. D3R PAM-Antagonist

    MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.
  34. Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
  35. Dopamine D2 inhibitor

    Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions.
  36. D2 receptor antagonist

    Adoprazine is part of the Antidepressant Agent group
  37. D2 receptor agonist

    B-HT 920 is a dopamine agonist that has been proposed as an antiparkinsonian agent. It also has α1-adrenergic and α2-adrenergic agonist activity.
  38. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  39. Dopamine agonist

    Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  40. dopamine D3 receptor antagonist

    SB-277011 is a drug which acts as a potent and selective dopamine D3 receptor antagonist which is around 80-100x selective for D3 over D2 and lacks any partial agonist activity.
  41. Dopamine receptor ligand

    ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
  42. Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.
  43. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  44. Ropinirole a selective dopamine D2 receptors inhibitor with IC5N/A of 29 nM.
  45. Ropinirole Hydrochloride is a dopamine receptor agonist.
  46. Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
  47. 5-HT/dopamine D2 antagonist

    Ocaperidone is an effective antipsychotic agent.
  48. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
  49. dopamine β-hydroxylase (DBH) inhibitor

    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
  50. dopamine D3 Receptor (DRD3) antagonist

    GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.

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