Dopamine Receptors

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  1. Dopamine Receptors Blocker

    Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis.
  2. Stable Isotope

    Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis.
  3. Autophagy Inducer

    Cabergoline diphosphate is an ergot alkaloid that acts as an agonist of dopamine D2-like receptors, demonstrating high affinity for D2, D3, and 5-HT2B receptors with Ki values of 0.7, 1.5, and 1.2, respectively. It serves as an autophagy inducer, making it a valuable tool for research focused on cellular processes related to autophagy and neurobiology. This compound is instrumental in studies investigating neurodegenerative diseases and metabolic regulation, providing insights into the role of dopamine receptors in cellular homeostasis.
  4. Stable Isotope

    Cabergoline-d6 is a stable isotope-labeled form of Cabergoline, an ergot-derived dopamine D2-like receptor agonist. This compound exhibits high affinity for dopamine receptors D2 and D3, as well as 5-HT2B receptors, with Ki values of 0.7, 1.5, and 1.2 nM respectively. Cabergoline-d6 is utilized in pharmacokinetic studies and metabolic research to investigate the behavior of Cabergoline in biological systems.
  5. Dopamine Receptor Antagonist

    Pimozide-d4 is a deuterated derivative of Pimozide, functioning primarily as a dopamine receptor antagonist. It demonstrates potent inhibitory activity with Ki values of 1.4 nM, 2.5 nM, and 588 nM against the dopamine D2, D3, and D1 receptors, respectively. Additionally, Pimozide-d4 exhibits affinity for the α1-adrenoceptor (Ki = 39 nM) and inhibits signaling pathways associated with STAT3 and STAT5. This compound is valuable for research focusing on neuropharmacology and the modulation of dopaminergic signaling pathways.
  6. Stable Isotope

    Pimozide-d5 is a stable isotope-labeled form of Pimozide, a potent antagonist of dopamine receptors primarily targeting D2, D3, and D1 receptors with Ki values of 1.4 nM, 2.5 nM, and 588 nM, respectively. This compound also exhibits affinity for the α1-adrenoceptor with a Ki of 39 nM and has been shown to inhibit signaling pathways through STAT3 and STAT5. Pimozide-d5 is valuable in pharmacological studies and research involving dopamine signaling and receptor interaction.
  7. Stable Isotope

    Pimozide-d5 N-Oxide is a deuterium-labeled derivative of Pimozide, which primarily functions as a dopamine receptor antagonist, exhibiting Ki values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. Additionally, this compound has notable affinity for the α1-adrenoceptor with a Ki of 39 nM. Pimozide also inhibits the signaling pathways of STAT3 and STAT5, making it relevant for research applications in neurobiology and cancer biology studies.
  8. Dopamine Receptor Agonist

    Apomorphine is a potent dopamine receptor agonist with additional inhibitory effects on monoamine oxidases A and B. It demonstrates neuroprotective properties, evidenced by its ability to reduce reactive oxygen species production, inhibit DNA fragmentation, and downregulate JNK and ERK1/2 phosphorylation. Apomorphine also facilitates the degradation of intracellular Aβ40 and Aβ42, lowers tau protein levels, and suppresses MMP-9 expression. Its radical scavenging and iron chelating capabilities make it valuable for research in neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease, as well as studies related to breast carcinoma and erectile dysfunction.
  9. D2/H1 Antagonist

    Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research.
  10. Anticholinergic Agent

    Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies.
  11. Antipsychotic Agent

    Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders.
  12. Dopamine Receptor Antagonist

    Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes.
  13. 5-HT2/D1/D2 Antagonist

    Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems.
  14. Dopamine D4 Receptor Antagonist

    L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro.
  15. Dopamine Receptor Antagonist

    Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology.
  16. D4R Antagonist

    Dopamine D4 receptor ligand 3 is a selective antagonist of the dopamine D4 receptor (D4R), exhibiting a pKi of 8.86. It demonstrates significant activity with pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 signaling pathways in HEK-293T cells, respectively. Additionally, this compound has been shown to inhibit cell viability in three human glioma cell lines—U87 MG, T98G, and U251 MG—while also inducing reactive oxygen species (ROS) production and mitochondrial dysfunction in these glioma cells. This makes it a valuable tool for studying the role of D4R antagonism in cancer biology and neuropharmacology.
  17. Dopamine Receptors Blocker

    Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis.
  18. Monosaccharide

    Rhamnose (L-Rhamnose) is a naturally occurring deoxysugar that primarily targets inflammatory pathways. It has been shown to inhibit pro-inflammatory interleukins and matrix metalloproteinases (MMPs) in models of skin aging, highlighting its potential in anti-aging research. Additionally, Rhamnose enhances the phosphorylation of protein kinase A (PKA) substrates and hormone-sensitive lipase (HSL) in adipocytes, promoting PKA signaling and fat metabolism. Its ability to stimulate dopamine receptors and induce thermogenesis makes Rhamnose a valuable compound in obesity studies, while Rhamnose monohydrate is also utilized in research involving Ehrlich’s solid tumors and sarcomas.
  19. hD4 Receptor Antagonist

    L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro.
  20. Histamine Receptor Antagonist

    Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies.
  21. Dopamine Receptor Agonist

    Proterguride is a potent agonist of dopamine receptors, demonstrating significant potential in modulating dopaminergic signaling. Additionally, it exhibits antagonistic activity at the histamine H(1) receptor and alpha(1)-adrenoceptor, while also partially activating serotonergic 5-HT2A/B receptors. This compound is valuable for research focused on neurological diseases, including Parkinson's disease, providing insights into dopaminergic mechanisms and receptor interactions.
  22. D2/H1 Antagonist

    Norzine dimalate, a potent antagonist of dopamine D2 and histamine H1 receptors, exhibits significant anti-emetic and antipsychotic properties. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β load in murine models. Its diverse biological activities make Norzine dimalate a valuable reagent for research in neuropharmacology and Alzheimer's disease studies.
  23. Stable Isotope

    Benztropine-d3 mesylate is a deuterium-labeled form of the centrally acting anticholinergic agent, Benztropine mesylate. This compound is primarily utilized in Parkinson's disease research and exhibits anti-histaminic properties alongside its function as a dopamine reuptake inhibitor. Additionally, Benztropine mesylate acts as an allosteric antagonist at the human D2 dopamine receptor and demonstrates effects against cancer stem cells (CSCs), making it valuable for studies in both neuropharmacology and oncology.
  24. Dopamine Receptor Antagonist

    Thiothixene is a potent dopamine D2 receptor antagonist, exhibiting selectivity over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). This compound demonstrates significant biological activity by reducing spontaneous and amphetamine-induced locomotor activity in rodent models, thereby influencing behavioral paradigms. Additionally, thiothixene enhances latent inhibition and competitive behavior, suggesting potential applications in understanding psychotropic effects and selective attention. Its diverse receptor binding profile also includes interactions with serotonin, histamine, adrenergic, muscarinic acetylcholine, and sigma receptors, broadening its relevance in psychopharmacological research.
  25. 5-HT Receptor Antagonist

    Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions.
  26. Histamine Receptor Inhibitor

    Perphenazine-d8 dihydrochloride is a deuterium-labeled derivative of Perphenazine, primarily functioning as a histamine receptor inhibitor. This compound exhibits potent antipsychotic properties by interacting with serotonin and dopamine receptors. It is valuable for research focused on neuropharmacology, chemical biology, and the study of receptor-ligand interactions in psychiatric disorders.
  27. Dopamine Receptor Inhibitor

    BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications.
  28. Amfebutamone (Bupropion) is an atypical antidepressant and smoking cessation aid.
  29. Dopamine Receptor antagonist

    Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
  30. Chlorprothixene exerts strong antagonism at the following receptors: 5-HT2; D1, D2, D3; H1;mACh; α1-adrenergic.
  31. Dopamine (abbreviated as DA), a simple organic chemical in the catecholamine family, is a monoamine neurotransmitter - a chemical released by nerve cells to send signals to other nerve cells.
  32. CYP2D6 inhibitor

    Haloperidol (Haldol) is an antipsychotic and butyrophenone.
  33. dopamine beta-hydroxylase inhibitor

    Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
  34. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  35. Dopamine Receptor Agonist

    Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS).
  36. Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder.
  37. D2 dopamine agonist

    U-95666E is a D2 selective dopamine agonist with an ED50 of about 46 nM, was investigated for its effect on rat striatal acetylcholine (ACh) concentration
  38. 5-HT (serotonin) and dopamine receptor antagonist

    Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  39. Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
  40. 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.
  41. 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.
  42. D1/D5 receptor full agonist

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

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

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM).
  45. 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.
  46. dopamine reuptake inhibitor

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

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

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

  49. dopamine D4 receptor partial agonist

    Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
  50. 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.

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