GPCR/G Protein

Items 3101-3150 of 5455

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  1. Dopamine D2/D5 Receptor Antagonist

    Molindone is a potent antagonist of dopamine D2 and D5 receptors, classified as an indole derivative. This compound exhibits significant biological activity in modulating dopaminergic neurotransmission and is primarily used in the research of schizophrenia and severe mental illnesses. Its mechanism of action makes it a valuable tool for studying dopaminergic pathways and their implications in psychiatric disorders.
  2. D2 Receptor Blocker

    Trimethobenzamide is a D2 receptor blocker that serves as an effective antiemetic. It is primarily used to prevent nausea and vomiting, making it valuable in various clinical settings. This compound can be utilized in research applications focused on gastrointestinal motility and central nervous system interactions.
  3. Dopamine D2-receptor Agonist

    5-OH-DPAT (5-Hydroxy-DPAT) is a potent and selective agonist of the dopamine D2 receptor, with minimal activity at 5-HT receptors. This compound is known to enhance male rat sexual behavior, providing insights into the role of dopamine in sexual function. As a valuable tool in neuropharmacology research, 5-OH-DPAT can be utilized to study dopamine receptor signaling and its implications in various behavioral models.
  4. D1-Dopamine Receptor Antagonist.

    Trepipam is a D1-dopamine receptor antagonist, primarily utilized for its neuroprotective properties. It has demonstrated efficacy in reducing self-injurious behavior in 6-OHDA-lesioned rats, making it a valuable tool in behavioral neuroscience studies. Trepipam has potential applications in researching conditions such as epilepsy and anxiety disorders, facilitating insights into dopaminergic signaling pathways.
  5. D1R/D2R Ligand

    (-)-MDO-NPA is a dual-target ligand for dopamine receptors D1R and D2R, functioning as an N-propylnorapomorphine analog. It demonstrates β-arrestin EC50 values of 1949 nM for D1R and 520 nM for D2R, and cAMP EC50 values of 717.5 nM for D1R and 7.7 nM for D2R. This compound is particularly valuable for studying dopamine-related disorders, including Parkinson's disease, and contributes to understanding receptor signaling pathways in pharmacological research.
  6. D2 Receptor Antagonist

    Tiapride is a selective antagonist of the D2 and D3 dopamine receptors, exhibiting IC50 values of 110-320 nM and 180 nM, respectively. This compound demonstrates anti-dyskinetic and anxiolytic properties, making it valuable in neurological research. Tiapride is classified as a neuroleptic agent and is utilized in studies related to movement disorders and anxiety-related conditions.
  7. SKF-77434 Enantiomer

    (S)-SKF-77434 is a selective enantiomer targeting the dopamine D1 receptor, exhibiting an IC50 value of 2800 nM. This compound is utilized in research focused on neuropsychiatric disorders, providing insights into dopamine receptor modulation. Its affinity for the D1 receptor makes it a valuable tool for exploring the mechanisms underlying cognitive and behavioral functions.
  8. D3R/MOR Antagonist

    D3R/MOR antagonist 2 targets the dopamine D3 receptor (D3R) and the mu-opioid receptor (MOR) as a dual antagonist. With affinities of Ki 361 nM for D3R and 85.2 nM for MOR, this compound exhibits potential analgesic effects through MOR partial agonism while simultaneously mitigating opioid misuse liability via D3R antagonism. It serves as a valuable tool for research in pain management and addiction pharmacology.
  9. D2R Antagonist

    SV 156 is a highly selective antagonist of the D2 dopamine receptor, exhibiting a Ki value of 2.5 nM for human D2 receptors. With approximately 40-fold selectivity for the D2 receptor over the D3 subtype, SV 156 is primarily utilized in research related to L-DOPA-associated abnormal involuntary movements (AIMs). This compound serves as a valuable tool for investigating the mechanisms underlying dopaminergic signaling and movement disorders.
  10. Dopamine D3 Receptor Antagonist

    (±)-BAK2-66 is a potent dopamine D3 receptor antagonist, exhibiting Ki values of 1 nM for the D3 receptor and 960 nM for the D2 receptor. This compound is valuable for research applications focused on modulating dopaminergic signaling and exploring mechanisms underlying addiction in animal models. Its selectivity makes it an important tool for studying the role of the D3 receptor in various neurological conditions.
  11. D2 Receptor Antagonist

    (S)-Remoxipride is a selective antagonist of the dopamine D2 receptor, exhibiting an IC50 value of 1.57 μM. This compound is primarily utilized in research pertaining to psychotic disorders, offering insights into dopaminergic signaling and its implications in various neuropsychiatric conditions. Its specificity for the D2 receptor makes it a valuable tool for studying the effects of dopamine modulation in both in vitro and in vivo settings.
  12. D3 Partial Agonist

    FAUC 346 is a highly selective partial agonist of the dopamine D3 receptor, exhibiting an EC50 of 1.5 nM. This compound demonstrates significant biological activity in modulating dopaminergic signaling, making it a valuable tool for research focused on neuropharmacology and psychiatric disorders. FAUC 346 can be utilized to explore the therapeutic potential of D3 receptor modulation in various neurological conditions.
  13. Dopamine Receptor Inhibitor

    Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia.
  14. D3 Antagonist

    AVE-5997 is a selective D3 dopamine receptor antagonist. It effectively reduces hyperactivity induced by MK-801, making it a valuable tool for studying dopaminergic dysregulation. This compound is particularly relevant in the research of schizophrenia and related neuropsychiatric disorders.
  15. D2 Receptor Antagonist

    N-Methylspiroperidol is a potent D2 receptor antagonist that plays a critical role in neuropharmacological research. It can be utilized in PET (Positron Emission Tomography) imaging studies, allowing for the investigation of binding dynamics to the 5-HT2C receptor. This compound is particularly valuable for assessing neurotransmitter interactions, including the competitive effects of dopamine, thereby enhancing our understanding of neuropsychiatric disorders.
  16. Dopamine D1/D2 Receptor Inhibitor

    (Z)-Flupenthixol decanoate is a potent antagonist of dopamine D1 and D2 receptors, functioning primarily to inhibit dopaminergic signaling. This compound exhibits significant antipsychotic activity, making it valuable in the study of psychiatric disorders and neuropharmacology. Research applications include investigations into the modulation of dopaminergic pathways and the evaluation of therapeutic strategies for schizophrenia and related conditions.
  17. Dopamine Receptor Agonist

    Preclamol is a potent dopamine receptor agonist that stimulates both autoreceptors and postsynaptic receptors. It has been shown to inhibit locomotor activity in rodent models at low doses, making it a valuable tool for studying dopaminergic signaling and related behavioral effects. This compound is useful in research related to neuropharmacology and the exploration of dopamine-related disorders.
  18. D1 Dopamine Receptor Antagonist

    (R)-SKF 38393 hydrochloride is a potent and selective antagonist of the D1 dopamine receptor. This compound effectively inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels, making it a valuable tool for exploring dopamine signaling pathways. It is commonly used in research applications focused on neuropharmacology and the modulation of dopaminergic systems.
  19. D2 Receptor Agonist

    Carmoxirole is a selective peripheral dopamine D2 receptor agonist, demonstrating antihypertensive properties in vivo. This compound is valuable for research into the modulation of cardiovascular functions and the mechanisms underlying hypertension. Its targeted action on the D2 receptor makes it a useful tool for investigating dopaminergic signaling pathways.
  20. Dopamine Receptor Agonist

    (R)-SKF-81297 hydrobromide is the R-enantiomer of SKF-81297, acting primarily as a selective agonist for the dopamine D1 receptor. It demonstrates key biological activities related to the modulation of dopaminergic signaling pathways. This reagent is valuable in research applications focusing on neuropharmacology, including studies on dopamine-related disorders and the exploration of its effects on cognition and behavior.
  21. Neuroleptics

    Prosulpride is a neuroleptic compound that selectively antagonizes dopamine receptors, primarily targeting D2 and D3 subtypes. It exhibits significant antipsychotic properties, making it relevant for the treatment of various psychiatric disorders. Prosulpride is utilized in research to explore dopaminergic signaling pathways and to investigate its therapeutic potential in conditions such as schizophrenia and mood disorders.
  22. Dopamine Receptor Antagonist

    JHW007 hydrochloride is a selective antagonist of dopamine receptors, primarily targeting the D2 subtype. It demonstrates notable activity in modulating neurotransmitter release and has been investigated for its potential effects in cocaine-related research. This compound is valuable for studies exploring addiction mechanisms and neuropharmacology.
  23. Dopamine Receptor Antagonist

    (-)-GSK598809 is a selective antagonist of the dopamine D3 receptor (DRD3). This compound exhibits potent inhibition of DRD3 activity, making it a valuable tool for research into neuropsychiatric disorders and addiction. Its specificity for DRD3 allows for detailed investigations into dopamine-related signaling pathways and their implications for various therapeutic areas.
  24. Dopamine Receptor Agonist

    Bromocriptine is a potent agonist of the dopamine D2 and D3 receptors, exhibiting a high binding affinity with a pKi of 8.05 ± 0.2. This compound is primarily utilized in research to investigate dopaminergic signaling pathways and their implications in various neurological and psychiatric disorders. It is also employed in studies related to endocrine functions, particularly in conditions such as hyperprolactinemia and Parkinson's disease.
  25. Dopamine Receptor Inhibitor

    Seproxetine hydrochloride is a dopamine receptor inhibitor known for its selective serotonin reuptake inhibitory activity. By specifically blocking the serotonin uptake transporter, it increases serotonin levels in the brain, while also exhibiting significant interactions with dopamine receptors. This compound is actively researched for its potential therapeutic applications in mood disorders and associated neurological conditions, showcasing enhanced biological activity and efficacy through its ability to form stable charge transfer complexes.
  26. Dopamine Receptor Antagonist

    Nor-SCH-12679 maleate is a dopamine receptor antagonist that plays a crucial role in research focused on dopaminergic signaling pathways. By inhibiting dopamine receptor activity, it can counteract the stimulatory effects of other compounds, such as peppermint oil, on locomotor activity in experimental models. This compound is valuable for studies investigating the modulation of behavior and neuropharmacological effects related to dopamine signaling.
  27. Dopamine Receptor Antagonist

    JNJ-37822681 is a fast-dissociating antagonist of the D2 dopamine receptor, primarily employed in the research of schizophrenia. This compound demonstrates high specificity for D2 receptors and effectively increases levels of extracellular serotonin, dopamine, and norepinephrine within the rat cerebral cortex. Additionally, JNJ-37822681 exhibits antidepressant-like effects in the mouse tail suspension test while achieving favorable brain distribution and minimizing prolactin release, making it a valuable tool for neuroscience research.
  28. PF-06256142 Enantiomer

    (R)-PF-06256142 is the R enantiomer of PF-06256142, selectively acting as an orthosteric agonist for the D1 dopamine receptor. This compound demonstrates significant potential in modulating receptor desensitization compared to dopamine and other catechol-containing agonists. Its properties make it a valuable tool for research into dopamine-related signaling pathways and receptor pharmacology.
  29. Dopamine D2/D3 Receptor Antagonist

    Raclopride tartrate is a selective antagonist of the dopamine D2 and D3 receptors, exhibiting high binding affinity with Ki values of 1.8 nM and 3.5 nM, respectively. This compound demonstrates potential antipsychotic effects and is primarily utilized in research focused on the modulation of dopaminergic signaling. Its application extends to studying neuropsychiatric disorders and exploring therapeutic strategies for schizophrenia and related conditions.
  30. Dopamine D3?Receptor Ligand

    Dopamine D3 receptor ligand-4 is a highly potent and selective ligand for the dopamine D3 receptor, exhibiting a Ki value of 0.5 nM. It demonstrates impressive selectivity for the D3 receptor over the D2 receptor, with a Ki of 7.43 nM. This compound is valuable for research applications focused on understanding dopamine-related pathways and potential therapeutic targets in neuropsychiatric disorders.
  31. PD3 Receptor Antagonist

    S 33138 is a potent D3 receptor antagonist. This compound has demonstrated the ability to inhibit addictive behaviors in various animal models, as well as ameliorate cognitive deficits in rodent and primate models of schizophrenia and Parkinson's disease. S 33138 serves as a valuable tool for research applications focused on neurological disorders, advancing the understanding of pathophysiological mechanisms and potential therapeutic strategies.
  32. Dopamine Autoreceptor Agonist

    PD 119819 is a selective dopamine autoreceptor agonist belonging to the benzopyran-4-one class. It modulates dopaminergic activity by inhibiting spontaneous locomotor activity and reducing brain dopamine synthesis. This compound is valuable for research into dopamine-related neurophysiology and the study of disorders influenced by dopamine receptor activity.
  33. Dopamine Receptor Agonist

    (-)-UH 232 is a central dopamine receptor agonist with a primary action of modulating dopaminergic signaling. It has been shown to reduce the formation of 3,4-dihydroxyphenylalanine (DOPA) in striatal and limbic regions of the rat brain. This compound serves as a valuable tool for investigating neurological disorders, including Parkinson's disease and schizophrenia.
  34. Dopamine Receptor Agonist

    RS-12254 is a dopamine receptor agonist that exerts hypotensive and diuretic effects through its regulation of blood pressure and electrolyte balance. This compound effectively lowers blood pressure and minimizes plasma norepinephrine levels, contributing to its diuretic and natriuretic properties. RS-12254 is valuable in research applications focused on cardiovascular regulation and sympathetic nerve activity modulation.
  35. D3R Antagonist

    ST 198 is a selective D3 receptor (D3R) antagonist that demonstrates oral bioactivity. It effectively inhibits nicotine-induced conditioned place preference (CPP) at specific doses targeting D3R. This compound is valuable for research investigating neurological diseases and the mechanisms underlying dopaminergic signaling.
  36. D3R PAM-Antagonist

    Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist targeting the D3 dopamine receptor (D3R) that effectively penetrates the blood-brain barrier. It demonstrates robust antagonist activity in D3R-mediated β-arrestin recruitment assays, exhibiting an IC50 of 2.5 μM and a Kd of 0.49 μM, and in D3R-mediated Go-BRET assays, with an IC50 of 0.34 μM. This reagent is suitable for investigating neuropsychiatric disorders, including substance use disorder, providing valuable insights into D3R's role in these conditions.
  37. Dopamine Receptor Agonist

    Razpipadon ((-)-PW0464) is a dopamine receptor partial agonist with a specific affinity for the D1 receptor. This compound is crucial for research into dopamine-mediated psychiatric disorders, as it allows for the investigation of receptor activity and its impact on neurochemical signaling. Razpipadon serves as a valuable tool for elucidating the role of dopamine in various neurological and psychiatric conditions.
  38. Dopamine D2 Receptor Antagonist

    Bromopride hydrochloride is a selective, irreversible dopamine D2 receptor antagonist with oral bioactivity. It effectively crosses the blood-brain barrier to inhibit the vomiting center while promoting gastrointestinal motility by enhancing smooth muscle contraction. This compound is valuable for research into digestive system disorders, including gastric hypomotility, nausea, and vomiting, and demonstrates no harmful effects on abdominal wall healing in the context of postoperative abdominal infections.
  39. D2 Receptor Antagonist

    SLV310 is an orally active antagonist of the dopamine D2 receptor, exhibiting a Ki value of 5 nM, and also acts as a serotonin reuptake inhibitor. It effectively antagonizes Apomorphine-induced climbing behavior and 5-HTP-induced serotonin syndrome in murine models, with an ED50 of 5.6 and 5.9 mg/kg, respectively. This compound serves as a valuable tool for antipsychotic research, particularly in studies related to schizophrenia.
  40. D2/D3 Receptor Agonist

    N-Despropyl Ropinirole (SKF-104557) is a potent agonist targeting dopamine D2 and D3 receptors. As an active metabolite of Ropinirole, it exhibits full agonistic activity at human D2 and D3 receptors while acting as a partial agonist at the hD4 receptor. This compound is valuable for research applications investigating dopaminergic signaling and potential therapeutic strategies for diseases such as Parkinson's and schizophrenia.
  41. Dopamine D4 Receptor Antagonist,

    CP-293019 is a selective antagonist of the dopamine D4 receptor, characterized by a Ki value of 3.4 nM. This compound effectively inhibits apomorphine-induced hyperactivity in rat models, making it a valuable tool for research into neuropharmacology and the role of dopamine receptors in behavioral studies. Its application extends to studies exploring the mechanisms underlying dopamine-related disorders.
  42. Dopamine Receptor Antagonist

    Bromperidol decanoate is a dopamine receptor antagonist primarily utilized in the treatment of schizophrenia. Its notable biological activity includes the inhibition of dopaminergic pathways, which contributes to its antipsychotic effects. This compound is relevant in research focused on psychotropic drug development and the exploration of dopamine-related disorders.
  43. Dopamine Receptor Antagonist

    Ordopidine is a selective dopamine D2 receptor antagonist that effectively inhibits hyperactivity induced by psychostimulants. This compound is valuable for neurological research, providing insights into the modulation of dopaminergic pathways and the study of related disorders. Its application may facilitate the exploration of therapeutic strategies for conditions such as schizophrenia and other dopamine-related disorders.
  44. D3R Antagonist

    VK4-116 is a selective antagonist of the Dopamine D3 receptor (D3R) with a Ki value of 6.84 nM. This compound effectively inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models, demonstrating its potential as a therapeutic agent for addiction-related behaviors. Furthermore, VK4-116 has been shown to prevent the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models, highlighting its applications in addiction research.
  45. D2-receptor Agonist

    (±)-N-Propylnorapomorphine functions as a dopamine D2-receptor agonist, selectively activating the D2 receptor pathway. This compound demonstrates significant biological activity related to dopaminergic signaling, making it valuable for research in neuropharmacology and the study of dopamine-related disorders. Its application extends to investigating the physiological and behavioral effects of dopamine modulation.
  46. Lisuride Analogue

    Bromerguride is an analogue of the ergot-derived dopamine agonist Lisuride, functioning primarily as a central antidopaminergic agent. This compound is utilized in pharmacological research to investigate the modulation of dopaminergic pathways and their implications in neurological conditions. Its unique properties make it a valuable tool for studying dopamine receptor interactions and their effects on various biological systems.
  47. PPHT Derivatives

    4-Amino-PPHT is a derivative of PPHT that selectively targets dopamine D-2 receptors, exhibiting a binding affinity characterized by a Ki value of 6.8 nM. This compound is essential for investigating the role of dopamine signaling in neuropharmacology and related research applications. It provides a valuable tool for studies focused on neuropsychiatric disorders and the development of therapeutic agents targeting dopamine receptors.
  48. Dopamine Receptor

    CJB-090 dihydrochloride is a partial agonist targeting dopamine D3 receptors. This compound demonstrates unique partial agonist properties in vitro and has been shown to provoke yawning responses in monkeys with a history of cocaine use. CJB-090 is also effective in reducing the reinstatement of cocaine-induced behaviors, making it a valuable tool for studies on addiction and dopamine receptor functions.
  49. Dopamine Receptor Agonist

    Dopamine D2 receptor agonist-2 is a selective agonist targeting the dopamine D2 receptor, exhibiting a binding affinity with a Ki value of 11.2 nM. This compound demonstrates biased agonism, making it a valuable tool for investigating mechanisms underlying antipsychotic effects. It is suitable for research applications focused on the modulation of dopamine signaling and the study of psychiatric disorders.
  50. Dopamine Receptor Antagonist

    Dopamine D3 receptor antagonist-1 is a selective antagonist of the dopamine D3 receptor, exhibiting a binding affinity with a Ki value of 1.58 nM. This compound is of particular interest in the study of central nervous system disorders, as it may play a role in modulating dopaminergic signaling pathways. Its unique bitopic ligand properties suggest applications in researching both psychiatric and neurodegenerative conditions, providing valuable insights into therapeutic interventions.

Items 3101-3150 of 5455

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