GPCR/G Protein

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  1. CB1 Ligand

    CB-25 is a partial agonist of the CB1 cannabinoid receptor. It has been shown to enhance Forskolin-induced cAMP formation specifically in cancer cells, while not affecting hCB1-CHO cells. This compound serves as a valuable tool for investigating the role of cannabinoid signaling pathways in cancer biology and related research applications.
  2. CB1R Allosteric Modulator

    CB1R Allosteric Modulator 5 is a selective allosteric modulator targeting the Cannabinoid receptor type 1 (CB1R) with a pIC50 of 6.89. This compound effectively reduces cocaine-seeking behavior associated with cue-induced reinstatement and mitigates cocaine-induced behavioral sensitization, while leaving locomotor activity unaffected. It is suitable for research applications concerning addiction, neuropharmacology, and the modulation of cannabinoid signaling pathways.
  3. Cannabinoids Precursor

    (1H-Indol-3-yl)(2,2,3,3-tetramethylcyclopropyl)methanone serves as a key precursor in the synthesis of synthetic cannabinoids. This compound is integral for the development of potent cannabinoid receptor modulators, facilitating research into cannabinoid pathways and their physiological effects. It is valuable for studies focused on cannabinoid-related pharmacology and drug development.
  4. CB2R Antagonist

    PGN36 is a selective antagonist of the cannabinoid CB2 receptor (CB2R), with a Ki of 0.09 µM for CB2R and >40 µM for CB1R. This compound effectively inhibits the upregulation of collagen type I gene expression induced by promoters of bone metabolism. Notably, PGN36 is capable of crossing the blood-brain barrier, making it a valuable tool for studying frontotemporal dementia (FTD) and other neurological conditions.
  5. Stable Isotope

    Linoleoyl ethanolamide-d4 is a deuterated analog of Linoleoyl ethanolamide, targeting cannabinoid receptors type-1 (CB1) and type-2 (CB2). This compound exhibits weak binding affinity, with inhibition constants (Kis) of 10 μM and 25 μM for CB1 and CB2, respectively. It is utilized in biochemical research to investigate cannabinoid receptor dynamics and efficacy in functional assays. Additionally, Linoleoyl ethanolamide-d4 serves as a useful tool in studies exploring fatty acid ethanolamides and their biological effects.
  6. CB2 receptor Agonist

    A-836339 is a selective agonist of the CB2 receptor, demonstrating Ki values of 0.4 nM and 0.8 nM for human and rat CB2 receptors, respectively. It exhibits significant analgesic, anti-inflammatory, gastric protective, and antioxidant activities. Activation of CB2 receptors in the dorsal root ganglia and spinal cord mediates its antinociceptive properties. Additionally, A-836339 reduces pro-inflammatory cytokines like TNF-α and IL-1β while enhancing the activity of antioxidant enzymes such as catalase and superoxide dismutase. This compound is valuable for research into inflammatory pain, neuropathic pain, gastric ulcers, and cerebral ischemia.
  7. CB1 Inhibitor

    ANEB-001 is an orally active inhibitor of the cannabinoid receptor type 1 (CB1). This compound is primarily utilized in research focused on acute cannabinoid intoxication, providing insights into the physiological effects and potential therapeutic approaches related to CB1 modulation. Its selective inhibition of CB1 makes it a valuable tool for studies investigating cannabinoid-related pathways and their implications in various biological contexts.
  8. CB2 Receptor Agonist

    LEI-101 is a selective, orally bioavailable agonist of the cannabinoid CB2 receptor, exhibiting a pEC50 of 8 for human CB2. With a pKi of less than 4 for hERG, it demonstrates minimal off-target activity. This compound is approximately 100-fold more potent in binding to CB2 receptors compared to CB1 receptors, making it a valuable tool for research in pain modulation, inflammation, and neuroprotection studies.
  9. CB2 Selective Agonist

    CB65 is a selective agonist for the CB2 receptor, demonstrating potent activity with a Ki value of 3.3 nM. Its affinity for the CB1 receptor is significantly lower, with a Ki value exceeding 1000 nM. This compound is primarily utilized in research focused on cannabinoid receptor signaling pathways and has potential applications in studying inflammation and pain modulation.
  10. Endocannabinoid Analog

    Docosahexaenoyl glycerol is an analog of the endocannabinoid system that primarily targets cannabinoid receptors. This compound enhances glucose uptake and demonstrates anti-inflammatory properties, making it a valuable tool for research in metabolic and inflammatory disorders. Its utility extends to studies exploring the interplay between endocannabinoids and energy metabolism, providing insights into potential therapeutic applications.
  11. GPR55 Antagonist

    PSB-SB-487 is a potent antagonist of GPR55, exhibiting an IC50 value of 0.113 µM, and acts as an agonist for the CB2 receptor with a Ki value of 0.292 µM. This compound is valuable for investigating various biological processes and disease states, including diabetes, Parkinson’s disease, neuropathic pain, and cancer. Its dual activity makes it a significant tool for understanding the role of cannabinoid receptors in disease mechanisms and potential therapeutic interventions.
  12. CB2 Receptor Agonists

    CB2 receptor agonist 10 specifically targets the cannabinoid receptor type 2 (CB2) with a Ki of 3.7 nM for human CB2 and a Ki of 110 nM for human CB1. It exhibits a potent EC50 of 0.52 nM for hCB2, indicating its high efficacy in activating this receptor. This compound is primarily utilized in research applications focused on cannabinoid signaling pathways, inflammation, and neuroprotection.
  13. CB2 Agonist

    GP1a is a potent agonist of the cannabinoid receptor 2 (CB2), demonstrating significant anti-inflammatory properties. This compound is effective in promoting skin wound healing by inhibiting inflammation and fibrogenesis, while facilitating the process of re-epithelialization. GP1a is valuable for research applications related to tissue repair and inflammation regulation.
  14. CB1 antagonist

    MJ15 is a potent and selective antagonist of the cannabinoid receptor type 1 (CB1), with a Ki of 27.2 pM and an IC50 of 118.9 pM specifically for rat CB1 receptors. This compound has demonstrated significant biological activity in models of obesity and hyperlipidemia, effectively inhibiting food intake and preventing increases in body weight in diet-induced obese rats and mice. MJ15 is valuable for research applications focused on metabolic disorders and the endocannabinoid system.
  15. Cannabinoid Analogue

    Cannabinodiol is a cannabinoid analogue that interacts with the endocannabinoid system. It exhibits biological activity by modulating cannabinoid receptors, providing insights into the therapeutic potential of cannabinoids. This compound is primarily utilized in research focused on cannabis pharmacology, receptor signaling, and potential therapeutic applications in various medical conditions.
  16. CB1R PAM

    GAT211 is a positive allosteric modulator of the cannabinoid 1 receptor (CB1R). It enhances cAMP and β-arrestin2 signaling with EC50 values of 260 nM and 650 nM, respectively. GAT211 is suitable for research focused on neuropathic and inflammatory pain pathways, making it a valuable tool for studying cannabinoid receptor modulation and its therapeutic implications.
  17. VR1/CB1 Agonist

    OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system.
  18. CB1 Agonist

    Noladin ether is a potent and selective agonist of the cannabinoid CB1 receptor, exhibiting a binding affinity with a Ki value of 21.2 nM. This compound is known to induce hypothermic effects, intestinal immobility, and mild antinociception, making it relevant for studies on cannabinoid signaling pathways and their physiological effects. Research applications include investigating the role of CB1 receptors in pain modulation and appetite regulation.
  19. CB2 Modulator

    CB2 Modulator 1 is a potent modulator of the cannabinoid receptor type 2 (CB2). This compound exhibits significant biological activity in regulating immune responses and inflammation. It shows promise for research applications related to immune disorders, osteoporosis, and renal ischemia, making it a valuable tool for studies investigating these conditions.
  20. CB2R/FAAH Modulator

    CB2R/FAAH modulator-3 is a dual-targeting compound that functions as an agonist of the cannabinoid receptor type 2 (CB2R) and an inhibitor of fatty acid amide hydrolase (FAAH). It exhibits Ki values of 20.1 nM for CB2R and 67.6 nM for CB1R, with an IC50 of 3.4 μM for FAAH. This modulator is valuable for research into cancer biology, inflammatory processes associated with neurodegenerative diseases, and potential therapeutic approaches for COVID-19.
  21. CB1 Receptor Ligand

    S-1 Methanandamide is an analog of Anandamide that acts as a ligand for the CB1 receptor, exhibiting a Ki value of 173 nM. It demonstrates significant biological activity by inhibiting electrically-evoked twitch responses in the mouse vas deferens, with an IC50 value of 230 nM. This compound is valuable for research focused on endocannabinoid signaling pathways and the physiological effects associated with CB1 receptor modulation.
  22. CB2 Receptor Agonist

    CB2 receptor agonist 3 is a highly selective agonist for the CB2 cannabinoid receptor, exhibiting an affinity of 7.6 nM for CB2 and a significantly lower affinity of 900 nM for CB1. This compound effectively activates downstream signaling pathways, as evidenced by its ability to significantly enhance P-ERK 1/2 expression in HL-60 cells. CB2 receptor agonist 3 is valuable for research investigating the role of CB2 receptors in various biological processes and potential therapeutic applications in inflammation and pain management.
  23. CB1 Receptor Modulator

    (R)-Monlunabant is a selective modulator of the CB1 receptor, engaging in critical interactions that influence endocannabinoid signaling. This compound exhibits potential anti-obesity effects and is valuable for investigating metabolic diseases. Its application in research may provide insights into therapeutic strategies for metabolic disorders associated with dysregulated appetite and energy homeostasis.
  24. CB1 Receptor Activator

    Nonabine (BRL-4664) is a cannabinoid that selectively activates the CB1 receptor, primarily targeting the brainstem and enteric nervous system. This compound exhibits significant antiemetic properties, making it valuable for research focused on nausea and vomiting mechanisms. Its ability to modulate cannabinoid receptors provides insight into potential therapeutic applications for gastrointestinal disorders and central nervous system regulation.
  25. DAGLα Inhibitor

    O-7460 is a selective inhibitor of diacylglycerol lipase alpha (DAGLα), exhibiting an IC50 value of 0.69 μM. This compound demonstrates selectivity against monoacylglycerol lipase (MAGL) and both human CB1 and CB2 cannabinoid receptors. O-7460 has been shown to effectively reduce elevated 2-arachidonoylglycerol (2-AG) levels associated with high-fat diet conditions, making it a valuable tool for studying endocannabinoid signaling and its implications in metabolic disorders.
  26. CB1 Receptor Antagonist

    LH21 is a potent CB1 receptor antagonist that functions as an in vivo neutral cannabinoid. It effectively reduces food intake and body weight gain in obese Zucker rats, making it a valuable tool for research into appetite regulation and obesity management. Its efficacy as a feeding inhibitor highlights its potential applications in metabolic studies and pharmacological research targeting feeding behaviors.
  27. CB2 Agonist

    L759633 is a selective agonist of the cannabinoid receptor type 2 (CB2), demonstrating a Ki value of 6.4 nM for CB2 and 1043 nM for CB1, highlighting its potency and selectivity. This compound inhibits Forskolin-stimulated cAMP production, making it a valuable tool for investigating CB2 receptor signaling pathways. L759633 holds significant potential for research applications in areas such as immunology and neurobiology, where modulation of the endocannabinoid system may provide therapeutic insights.
  28. CB2 Agonist

    S-777469 is a selective cannabinoid type 2 receptor (CB2) agonist with a Ki value of 36 nM. This compound exhibits significant antipruritic activity by effectively suppressing compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 operates by inhibiting itch signal transmission through its action on the CB2 receptor, making it a valuable tool for research in itch modulation and related sensory pathways.
  29. CB1R Antagonist

    Surinabant is a selective antagonist of the cannabinoid receptor type 1 (CB1R). It has been investigated for its potential biological activity in regulating appetite and influencing alcohol consumption. Surinabant is relevant for research applications focusing on obesity and alcoholic behavior, making it a valuable tool for studying metabolic disorders and addiction mechanisms.
  30. CB1 Receptor Antagonist

    Rosonabant is a selective antagonist of the cannabinoid receptor type 1 (CB1), demonstrating anti-obesity effects by promoting weight loss and mitigating obesity-related cardiovascular metabolic diseases. Its ability to inhibit CB1 activity makes it a valuable tool for research into metabolic regulation and potential therapeutic interventions for obesity. However, the compound has been associated with adverse effects, including nausea and psychiatric symptoms, warranting careful consideration in experimental applications.
  31. Cannabinoid Receptor Antagonist

    PSNCBAM-1 is a selective allosteric antagonist of the cannabinoid receptor type 1 (CB1), with an EC50 of 0.1 μM. This compound serves as a valuable tool in the investigation of obesity and related metabolic disorders, providing insights into the modulation of cannabinoid signaling pathways. Its specificity for the CB1 receptor makes it suitable for exploring therapeutic approaches targeting endocannabinoid system regulation.
  32. Stable Isotope

    Eicosapentaenoyl ethanolamide-d4 is a deuterium-labeled analogue of Eicosapentaenoyl ethanolamide, targeting cannabinoid receptors CB1 and CB2. This compound exhibits significant biological activity as a metabolic signal and is involved in modulating lifespan extension related to dietary restriction. Research applications include studies on the effects of Eicosapentaenoyl ethanolamide on lifespan dynamics in wild-type models and TOR pathway mutants, contributing to the understanding of metabolic and signaling pathways in physiology.
  33. Phytocannabinoid Derivative

    10(R)-Hydroxy-9(S)-hexahydrocannabinol is a phytocannabinoid derivative that exhibits structural similarity to established cannabinoids. This compound has shown potential biological activity relevant to cannabinoid receptors, making it a valuable tool for research into endocannabinoid signaling pathways. Its applications include studies on pain modulation, anti-inflammatory effects, and neuroprotection, contributing to a deeper understanding of cannabinoid pharmacology and therapeutic potential.
  34. Cannabinoid Receptor

    b-AEA is a biotinylated analog of anandamide (AEA) that selectively targets cannabinoid receptors. It has been designed to accumulate intracellularly, mimicking the behavior of its parent compound. Notably, b-AEA does not engage with other components of the endocannabinoid system, ensuring no interference with their physiological roles. This reagent is suited for studying the localization and distribution of endocannabinoids in cellular contexts.
  35. CB2 Receptor Agonist

    SER-601 is a potent and selective agonist of the peripheral cannabinoid (CB2) receptor, exhibiting a Ki of 6.3 nM. It demonstrates significant analgesic and antidiabetic effects, making it a valuable tool for research in pain management and metabolic disorders. This compound is pertinent for studies focused on the modulation of the endocannabinoid system and its therapeutic potential.
  36. Endogenous Cannabinoid

    Heptadecanoyl ethanolamide is an endogenous cannabinoid that targets cannabinoid receptors in the body. As a synthetic analog of palmitoylethanolamide (PEA), it features a unique 17-carbon fatty acid chain, which may enhance its biological activity. This compound is primarily utilized in research exploring pain modulation, inflammation, and neuroprotection. Its potential applications also include studies on the endocannabinoid system and its role in various physiological processes.
  37. Stable Isotope

    Anandamide-d11 is a deuterium-labeled analog of Anandamide, a known immune modulator in the central nervous system. It primarily targets cannabinoid receptors CB1 and CB2, while also engaging other pathways such as GPR18 and GPR55. This stable isotope is valuable for research applications in pharmacology and biochemistry, particularly in studies investigating endocannabinoid signaling and its role in various physiological processes.
  38. Cannabinoid Receptor

    CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways.
  39. CB/FAAH Inhibitor

    Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is a potent inhibitor of the central cannabinoid receptor (CB1) and fatty acid amide hydrolase (FAAH), exhibiting similar inhibitory activities with IC50 values around 2 nM. It serves as a valuable tool for investigating cannabinoid signaling pathways and lipid metabolism in various biological contexts. Researchers utilize IDEFP to explore the therapeutic potential of modulating endocannabinoid systems in pain, inflammation, and neuroprotection studies.
  40. CB1 Antagonist

    (R)-SLV 319 is a potent and selective antagonist of the cannabinoid receptor 1 (CB1) with a Ki value of 894 nM. This compound serves as the dextrorotatory isomer of SLV 319 and is valuable for research applications investigating the role of CB1 in various physiological processes and potential therapeutic targets in obesity, addiction, and neuroprotection.
  41. CB1 Receptor Allosteric Modulator

    RTICBM-189 is a potent allosteric modulator of the cannabinoid type-1 (CB1) receptor, demonstrating a pIC50 of 7.54 in Ca2+ mobilization assays. This compound exhibits selective activity with pIC50 values of 5.29 for human CB1 and 6.25 for mouse CB1. RTICBM-189 significantly reduces reinstatement of drug-seeking behavior in rodent models, making it valuable for research on addiction and related neurological disorders.
  42. CB2 Receptor Agonist

    CB2 Receptor Agonist 9 is an orally active compound targeting the cannabinoid receptor 2 (CB2) with an EC50 of 16.2 nM. This agonist effectively inhibits the expression of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6. It demonstrates significant anti-inflammatory activity in a dextran sulfate sodium-induced mouse model of acute colitis, making it a valuable tool for research into inflammatory diseases.
  43. Cannabinoid Receptor Agonist

    Virodhamine hydrochloride is a cannabinoid receptor agonist, acting as a partial agonist at the CB1 receptor and a full agonist at the CB2 receptor. This compound plays a significant role in modulating endocannabinoid signaling, making it valuable for studies related to the endocannabinoid system. Research applications include investigations of pain management, inflammation, and neuroprotection within the context of cannabinoid therapy.
  44. CB1R Agonist

    O-1269 is a partial agonist of cannabinoid receptor 1 (CB1R), displaying a binding affinity characterized by a Ki value of 32 nM. This compound exhibits significant analgesic effects, making it a valuable tool for investigations into pain modulation and cannabinoid receptor signaling pathways. Its application in research may provide insights into therapeutic strategies targeting CB1R-related conditions.
  45. CB1 Antagonist

    O-2050 is a potent cannabinoid CB1 receptor antagonist with an affinity of Ki = 2.5 nM. In addition, it exhibits significant inhibitory activity at the CB2 receptor with a Ki of 0.2 nM. This compound has been observed to induce locomotor stimulation in murine models, making it relevant for studies exploring the pharmacological effects of cannabinoid signaling in various research applications.
  46. CB2 Receptor Antagonist

    CB-52 is a selective antagonist of the CB2 cannabinoid receptor, functioning as a neutral ligand. It plays a significant role in modulating the endocannabinoid system and is utilized in research focused on pain management, inflammation, and immune response. The compound is valuable for studies investigating the therapeutic potential of cannabinoid modulation in various physiological and pathological conditions.
  47. CB1 Agonist

    BPR-890 is a highly selective agonist of the cannabinoid receptor 1 (CB1). This compound demonstrates significant efficacy in promoting CB1 activation, making it a valuable tool for investigating the endocannabinoid system. Its potent activity and selectivity also allow for research applications in obesity models, particularly in understanding the metabolic effects in diet-induced obese mice.
  48. CB2 Receptor Inverse Agonists

    MDA77 is an inverse agonist of the CB2 receptor, exhibiting a potent EC50 of 5.82 nM. This compound demonstrates selectivity for the human CB2 receptor while showing no activity on the CB1 receptor. MDA77 is suitable for research applications investigating cannabinoid-related signaling pathways and their therapeutic potential in various conditions.
  49. CB1R Allosteric Modulator

    CB1R Allosteric Modulator 4 is a positive allosteric modulator that targets the cannabinoid type-1 receptor (CB1R). It effectively inhibits cAMP production and demonstrates significant activity in β-arrestin-2 recruitment. This compound is valuable for research in cannabinoid signaling pathways and the modulation of endocannabinoid systems.
  50. BChE Inhibitor/CB2R Agonist

    hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation.

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