GPCR/G Protein

Items 4801-4850 of 6977

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  1. Analgesics

    Tramadol N-oxide is a derivative of tramadol that primarily targets analgesic pathways. It produces dose-dependent, long-lasting antinociception through its affinity for the μ-opioid receptor (Ki = 38.5 μM) while exhibiting weaker interactions with δ and κ receptors (Ki > 100 μM). This compound is valuable for research into analgesic effects and the mechanisms underlying pain relief.
  2. Opioid Compound

    3,4-Difluoro-N-desmethyl U-47700 hydrochloride is an opioid compound that acts on the μ-opioid receptor, demonstrating potent analgesic properties. This reagent is primarily utilized in research focused on pain management and addiction studies, contributing to a deeper understanding of opioid receptor activities and their therapeutic implications. Its unique fluorinated structure enhances its pharmacological profile, making it a valuable tool for scientific investigations into opioid-related pathways.
  3. Opioid Analog

    Chlorphine is a halogenated opioid analog that primarily targets opioid receptors in the central nervous system. This compound exhibits significant neuroactive properties, making it valuable for studying pain modulation and addiction mechanisms. Its unique structure allows for exploration of receptor interactions and the development of potential therapeutic agents in pain management and opioid research.
  4. Opioid Receptor

    3,4-Difluoro U-49900 hydrochloride is a selective opioid receptor agonist, primarily targeting the mu-opioid receptor. This compound exhibits strong analgesic properties and is utilized in research to investigate opioid signaling pathways and pain management mechanisms. Its potential applications include studies on addiction, analgesia, and opioid receptor pharmacology.
  5. Opioid Compound

    Desmethylmoramide is an opioid compound that exerts its effects primarily through interaction with opioid receptors, facilitating pain relief. This compound demonstrates notable analgesic activity in rodent models, making it a valuable tool for research into pain management and opioid pharmacology. Its structural similarity to established opioids may provide insights into opioid receptor function and the development of new analgesic therapies.
  6. mu-Opiate Receptor Ligand

    CHIR 4531 is a trimer peptide that functions as a mu-opiate receptor ligand, exhibiting a binding affinity characterized by a Ki value of 6 nM. This compound is primarily utilized in research focused on pain management, addiction, and opioid signaling pathways. Its ability to selectively engage the mu-opiate receptor makes it a valuable tool for studying the biological effects of opiates in various experimental contexts.
  7. Opioid Receptor

    DuP 747 hydrochloride is a selective agonist of the kappa-opioid receptor, primarily involved in analgesic activity. Studies indicate its administration can yield variable responses, with a lesser agonistic profile when given subcutaneously compared to intraperitoneal or oral routes. Notably, the 5-hydroxy-desmethoxy metabolite of DuP 747 predominantly influences behaviors associated with the saline-appropriate lever. These findings highlight the potential role of its metabolites in mediating responses similar to other kappa-opioid receptor ligands, enabling further exploration in the field of pain management and receptor pharmacology.
  8. Opioid Compound

    Ortho-methyl 4-anilino-1-boc-piperidine is an opioid compound that serves as a crucial precursor in synthetic pathways for the development of opioid receptor ligands. This reagent is valuable in chemical research aimed at designing and optimizing new analgesics with potential therapeutic applications in pain management and addiction treatment. Its structural features allow for modifications that can lead to enhanced receptor selectivity and activity.
  9. Opioid Receptor

    CP-866,087 is a potent and selective μ-opioid receptor antagonist. It effectively inhibits opioid effects and has demonstrated promising preclinical efficacy in models related to alcohol consumption. Additionally, CP-866,087 has been utilized in research investigating female sexual dysfunction.
  10. Opioid Compound

    Orphine is an opioid compound that primarily targets the opioid receptors in the central nervous system. It has been shown to enhance antinociceptive effects in murine models, with these effects being reversed by Naloxone, indicating its potential utility in pain management research. This compound is valuable for studying opioid mechanisms and developing analgesic therapies.
  11. Opioid Compound

    AH 8529 is an orally active opioid compound that primarily targets opioid receptors. It exhibits potent analgesic activity, making it valuable for pain management research. Its unique pharmacological profile enables investigations into opioid receptor signaling and the development of novel pain therapeutics.
  12. NOP Agonist

    NOP Agonist-2 is a selective nociceptin/orphanin FQ peptide (NOP) receptor agonist. It exhibits key biological activities associated with modulating pain perception, anxiety, and various affective disorders. This compound is valuable for research applications focusing on the nociceptin system's role in neurobiology and the potential development of therapeutic agents targeting NOP receptors.
  13. Opioid Compound

    N-(1-Benzyl-4-piperidyl)-N-benzylpropanamide hydrochloride is an opioid compound that interacts with opioid receptors, primarily influencing the mu-opioid receptor pathway. This compound exhibits significant analgesic properties, making it a valuable tool for research focused on pain management and opioid receptor characterization. Its unique structure provides a basis for exploring potential leads in the development of novel analgesics.
  14. Opioid Compound

    2,4-Difluoro U-48800 hydrochloride is a selective u-opioid receptor agonist. It exhibits significant analgesic properties, making it valuable in pain management research. This compound is useful for studying opioid receptor interactions and the development of novel analgesics in medicinal chemistry.
  15. Opioid Compound

    Methylketobemidone is an opioid receptor agonist that interacts primarily with the mu-opioid receptor. This compound exhibits significant analgesic activity, making it a valuable tool for investigating pain pathways and developing pain management therapies. Its structural similarity to existing opioids allows for comparative studies in opioid receptor pharmacology and the evaluation of potential side effects and efficacy in preclinical research.
  16. Opioid Compound

    3,4-Difluoro U-50488 hydrochloride is a selective kappa-opioid receptor agonist. This compound exhibits potent analgesic activity and has been utilized in research to explore the neuropharmacological effects of kappa-opioid receptor modulation. Its unique structural modifications enhance specificity, making it a valuable tool for investigating pain pathways and opioid signaling mechanisms in various biological contexts.
  17. Opioid Compound

    2-Naphthyl U-47700 is a selective μ-opioid receptor agonist. It demonstrates potent analgesic activity, making it an important compound for research into pain management and opioid receptor functionality. This reagent is useful for exploring the pharmacological effects of opioids and investigating potential therapeutic applications in pain relief.
  18. Opioid Compounds

    AH 8507 is an analog of AH 7563, belonging to the class of opioid compounds. Despite its structural similarity, AH 8507 displays minimal analgesic effects in animal models, with ED50 values exceeding 100 mg/kg in both the phenylquinone and hot plate tests. This compound is primarily utilized in research to further understand the mechanisms of opioid activity and to explore the structure-activity relationship within opioid analogs.
  19. Opioid Compound

    3,4-Difluoro propyl U-47700 is an opioid compound that acts as a selective agonist at the mu-opioid receptor. This compound exhibits potent analgesic properties and is primarily utilized in pharmacological research related to pain management and opioid receptor studies. Its structural modifications enhance its biological activity, making it a valuable tool for understanding opioid mechanisms and potential therapeutic applications.
  20. DOP Agonist

    DPI-287 is a selective delta-opioid receptor (DOP) agonist, exhibiting a Ki value of 0.39 nM. This compound is crucial for research focusing on pain modulation and the development of analgesic therapies. Its high affinity for DOP allows for in-depth studies of the receptor's role in pain pathways and potential therapeutic targets.
  21. Opioid Receptor Modulator

    Samidorphan hydrochloride is an opioid receptor modulator with significant binding affinity for μ-opioid, κ-opioid, and δ-opioid receptors. It functions primarily as an antagonist at μ-opioid receptors while acting as a partial agonist at κ- and δ-opioid receptors. This unique profile enables Samidorphan hydrochloride to modulate opioid activity, making it a valuable tool in research focused on depression and other mood disorders. Its ability to improve behavioral outcomes in depressed animal models highlights its potential applications in neuropharmacology.
  22. Opioid Compound

    3,4-Difluoro isopropyl U-47700 is a synthetic opioid compound that acts primarily on the mu-opioid receptor. It exhibits potent analgesic effects, making it relevant for research into pain management and opioid receptor pharmacology. Its unique structure allows for the exploration of opioid effects as well as potential applications in the study of drug interactions and addiction mechanisms.
  23. KOR Agonist

    Difelikefalin acetate is a selective kappa opioid receptor (KOR) agonist that primarily exerts its effects peripherally. This compound demonstrates significant anti-inflammatory properties and shows potential in alleviating pruritus associated with conditions such as chronic kidney disease. Its targeted mechanism of action makes it a valuable tool for investigating KOR-related pathways and their impact on inflammatory and pruritic processes.
  24. Opioid Compound

    U-49900 is a u-opioid receptor agonist that demonstrates significant analgesic properties. Its primary mechanism involves modulating pain responses by activating the u-opioid receptor, which is integral in the management of pain signaling pathways. This compound is commonly used in pharmacological studies focusing on pain relief, opioid receptor interactions, and the development of novel analgesics.
  25. NOP Partial Agonist

    NOP Agonist-1 is a partial agonist for the nociceptin opioid receptor (NOP). This compound has demonstrated the ability to attenuate parkinsonian disabilities in 6-OHDA hemilesioned rat models. Its applications in research may provide insights into the therapeutic potential of NOP modulation in movement disorders and pain management.
  26. Opioid Receptor Agonist

    Salvinorin A carbamate is a potent κ-opioid receptor agonist, exhibiting an EC50 value of 6.2 nM and a Ki of 3.2 nM. This compound demonstrates significant biological activity in modulating pain and has potential applications in the study of addiction and mood disorders. Its unique pharmacological profile makes it a valuable tool for research in opioid receptor signaling and therapeutic development.
  27. Analgesics

    Corynantheidine is a mu-opioid receptor (MOR) partial agonist, demonstrating analgesic effects through MOR activation in preclinical models. This compound is primarily utilized in research focused on pain management and the exploration of opioid receptor activity. Its ability to modulate pain responses makes it a valuable tool for studying the mechanisms underlying analgesia and opioid signaling.
  28. Opioid Compound

    Bipiperidinyl 4-ANPP is an opioid compound that interacts primarily with the mu-opioid receptor. This compound demonstrates significant analgesic properties and is utilized in research focused on pain management and opioid receptor pharmacology. Its structural similarity to known opioids positions it as a valuable tool for investigating the mechanisms underlying opioid action and potential therapeutic applications in chronic pain and addiction studies.
  29. μ-Opioid Receptor Agonist

    Endomorphin 2 is a high-affinity agonist of the μ-opioid receptor, exhibiting selectivity and potency in targeting this pathway. It also shows moderate affinity for kappa3 binding sites, with a Ki value ranging from 20 to 30 nM. This compound is valuable for research in pain management, neurobiology, and the pharmacological characterization of opioid receptors. Its unique properties make it suitable for studies focused on opioid signaling and potential therapeutic applications in pain relief.
  30. Orexin Receptor Agonist

    Danavorexton is an orexin receptor agonist with notable brain permeability. This compound selectively activates the OX2R receptor, demonstrating efficacy in enhancing wakefulness and alleviating symptoms of sleepiness in preclinical models. Danavorexton serves as a valuable tool for research into sleep disorders and the pharmacological modulation of the orexin system.
  31. Alixorexton Enantiomer

    Alixorexton enantiomer is a selective, orally active agonist targeting the orexin-2 receptor. This compound is primarily investigated for its potential applications in the study of hypersomnias and related sleep disorders. Its ability to penetrate the blood-brain barrier makes it a valuable tool for exploring orexin system functioning and its implications in sleep regulation.
  32. OX Receptor Antagonist

    EMPA is a selective and reversible antagonist of the orexin OX2 receptor. It demonstrates high-affinity binding, with KD values of 1.1 nM for human and 1.4 nM for rat OX2-HEK293 membranes. This compound is valuable for research into the role of orexin signaling in various physiological processes and related disorders.
  33. Orexin Type 2 Receptor Agonist

    Oveporexton is a selective agonist of the orexin type 2 receptor (OX2R) with an EC50 of 2.5 nM and demonstrates a remarkable 3000-fold selectivity over the orexin type 1 receptor (OX1R). This compound is particularly relevant for research into hypersomnia disorders, including narcolepsy, providing insights into sleep regulation and potential therapeutic approaches. Its oral bioactivity enables convenient experimental application in various preclinical studies.
  34. OX1R/OX2R Antagonist

    Vornorexant is a potent antagonist of both the OX1R and OX2R receptors, exhibiting IC50 values of 1.05 nM and 1.27 nM, respectively. This compound is primarily utilized in studies focused on sleep physiology and insomnia, demonstrating significant sleep-promoting effects in vivo. It serves as a valuable tool for researchers investigating the pathophysiology of sleep disorders and the therapeutic potential of orexin receptor modulation.
  35. OX2R Activator

    Alixorexton is a selective OX2R activator that effectively crosses the blood-brain barrier, functioning as a wake-promoting agent. This compound is primarily utilized in research related to sleep disorders, including narcolepsy and idiopathic hypersomnia, making it a valuable tool for investigating the mechanisms of sleep regulation and potential therapeutic interventions.
  36. Orexin Receptor 2 Agonist

    YNT-185 is a selective agonist of the orexin type-2 receptor (OX2R), exhibiting an EC50 of 0.028 μM for OX2R and 2.75 μM for OX1R. This nonpeptide compound has been shown to alleviate symptoms of narcolepsy-cataplexy in murine models, making it a valuable tool for researching sleep disorders and neurodegenerative conditions related to orexin signaling.
  37. Orexin-2 Receptor Antagonist

    Seltorexant hydrochloride is a selective antagonist of the orexin-2 receptor (OX2R), exhibiting high affinity characterized by pKi values of 8.0 and 8.1 in human and rat OX2R, respectively. This compound is capable of permeating the blood-brain barrier and effectively occupies OX2R binding sites in the rat brain. Seltorexant hydrochloride is valuable for research applications focused on sleep disorders and the modulation of wakefulness, making it a pertinent tool in neuroscience studies.
  38. Orexin Receptor 2 Agonist

    YNT-185 dihydrochloride is a selective agonist of the orexin type-2 receptor (OX2R), demonstrating an EC50 of 0.028 μM for OX2R and 2.75 μM for OX1R. This compound has shown efficacy in ameliorating symptoms associated with narcolepsy-cataplexy in murine models, making it a valuable tool for research in sleep disorders and related pathophysiologies. Its selectivity for OX2R positions YNT-185 dihydrochloride as a significant reagent for exploring orexin receptor mechanisms and therapeutic interventions.
  39. Orexin Receptor Agonist

    Orexin B is an endogenous agonist for the orexin receptors, exhibiting a Ki of 420 nM for the OX1 receptor and 36 nM for the OX2 receptor. This peptide plays a crucial role in regulating various physiological processes, including energy homeostasis, sleep-wake cycles, and appetite. Orexin B is primarily utilized in research applications focused on neurobiology and metabolic diseases, providing insights into the mechanisms of sleep regulation and potential therapeutic targets for disorders like narcolepsy and obesity.
  40. Orexin Receptor Antagonist

    ACT-462206 is a potent dual antagonist of the Orexin 1 and Orexin 2 receptors, demonstrating IC50 values of 60 nM and 11 nM, respectively. This orally active compound exhibits favorable brain penetration, making it suitable for research into insomnia, anxiety disorders, and addiction. Its targeted mechanism allows for exploration of orexin signaling pathways and their role in regulating sleep and stress responses.
  41. Orexin 1 Receptor Inhibitor

  42. Orexin 1 Receptor Agonist

    (R)-YNT-3708 is a selective agonist of the orexin 1 receptor (OX1R), exhibiting an EC50 of 7.48 nM. This compound demonstrates significant antinociceptive effects, making it a valuable tool for research in pain modulation and potential therapeutic applications in disorders related to orexin signaling.
  43. Orexin-1 Receptor Antagonist

    CVN766 is an orally active orexin-1 receptor antagonist, exhibiting an IC50 of 8 nM for OX1R and greater than 10 μM for OX2R, indicating selectivity. This compound demonstrates effective blood-brain barrier permeability, making it suitable for neurological studies. CVN766 is primarily utilized in research related to schizophrenia, providing insights into the role of orexin receptors in neuropsychiatric disorders.
  44. OX1R Antagonist

    JNJ-54717793 is a selective and high-affinity antagonist of the orexin-1 receptor (OX1R), demonstrating significant brain penetration and oral bioactivity with a plasma EC50 of 85 ng/mL. Its Ki values for the human OX1R and OX2R are 16 nM and 700 nM, respectively. This compound is primarily utilized in research on anxiety disorders, providing insights into the modulation of orexin signaling pathways.
  45. OX40 Agonist Antibody

    Ordastobart is a hexavalent OX40 agonist antibody that enhances OX40 receptor clustering and signaling. This mechanism leads to increased proliferation and activation of CD4+ and CD8+ T cells both in vitro and in vivo. Ordastobart demonstrates anti-tumor activity and has been shown to improve survival in mouse models of cancers, such as fibrosarcoma and colorectal cancer. It is suitable for research applications focusing on cancer immunotherapy.
  46. Orexin Receptor Antagonist

    Fazamorexant is a dual orexin receptor antagonist targeting both OX1R and OX2R, with IC50 values of 32 nM and 41 nM, respectively. This compound is known to enhance total sleep time and improve sleep efficiency, making it a valuable tool for the study of insomnia and sleep disorders. Fazamorexant is suitable for use in various research applications focused on therapeutic strategies for sleep-related conditions.
  47. Orexin Type 2 Receptor Agonist

    Suntinorexton is an Orexin Type 2 Receptor (OX2R) agonist that modulates neuropeptide signaling. This compound enhances respiratory function during sleep, making it valuable for research on sleep disorders and respiratory physiology. Suntinorexton can be utilized to investigate the role of the orexin system in regulating wakefulness, arousal, and metabolic processes.
  48. OX2 Agonist

    [Ala11,D-Leu15]-Orexin B (human) is a selective agonist of the orexin-2 receptor (OX2), exhibiting a significant 400-fold selectivity for OX2 with an EC50 of 0.13 nM compared to OX1 (52 nM). This compound plays a critical role in the regulation of arousal, sleep, and appetite. It is widely used in research applications aimed at understanding the neurobiology of sleep disorders and metabolic conditions.
  49. OX1R Inhibitor

    Tebideutorexant is a selective inhibitor of the orexin receptor 1 (OX1R), demonstrating significant oral bioavailability and the ability to cross the blood-brain barrier. With a human OX1R pKi of 8.17 and a rat OX1R pKi of 8.13, this compound specifically targets OX1R while exerting minimal effects on OX2R. Tebideutorexant is a valuable tool for investigating panic and anxiety disorders in preclinical research settings.
  50. Isomer

    (2R,3R)-Firazorexton is a selective agonist of the orexin type 2 receptor (OX2R), known for its potential to enhance wakefulness and alleviate symptoms associated with narcolepsy. As an isomer of Firazorexton, this compound exhibits the same brain-penetrating properties, making it suitable for research in sleep disorders and circadian rhythm regulation. Its biological activity supports investigations into therapeutic avenues for energy balance and long-term wakefulness.

Items 4801-4850 of 6977

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