Cannabinoid Receptors

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. CB1/CB2 Agonist

    BAY 38-7271 is a highly potent and selective agonist of the cannabinoid CB1 and CB2 receptors, exhibiting binding affinities with Kis of 1.85 nM for the human CB1 receptor and 5.96 nM for the CB2 receptor. This compound demonstrates significant neuroprotective properties, making it a valuable tool for research in neuropharmacology and the therapeutic potential of cannabinoid systems. Its activation of CB1 and CB2 receptors can aid in understanding various neurological disorders and the roles of endocannabinoids in pain management and inflammation.
  38. Cannabinoid Receptor Agonist

    APP-FUBINACA is a potent cannabinoid receptor agonist derived from phenylalaninamide-based indazole-3-carboxamide. This compound displays neurostimulatory properties, making it a valuable tool for research involving cannabinoid signaling pathways and their impact on neurological functions. Its applications include studies on pain modulation, mood disorders, and the neurobiological effects of cannabinoids.
  39. Cannabinoid Receptor Agonist

    CB2R agonist 3 is a selective agonist of cannabinoid receptor 2 (CB2R), exhibiting an EC50 of 0.37 μM. This compound modulates immune responses, making it valuable for research focused on inflammation, pain management, and neurological disorders. Its ability to selectively target CB2R allows for the investigation of cannabinoid pathways in various biological systems.
  40. CB2 Receptor Agonist

    HU 433 is a synthetic cannabinoid that functions as a selective agonist of the CB2 receptor. It demonstrates significant anti-inflammatory and neuroprotective properties through its interaction with CB2 receptors. This compound is valuable for research applications focused on neuroinflammation and retinal disorders, facilitating a deeper understanding of these conditions and their potential treatments.
  41. Cannabinoid Receptor Agonist

    JTE 7-31 is a selective agonist of peripheral cannabinoid receptors, designed to minimize central nervous system side effects. It demonstrates potent immunomodulatory, anti-inflammatory, and anti-allergic properties, making it a valuable tool for research applications focused on inflammation and immune responses. Additionally, JTE 7-31 exhibits inhibitory effects on nephritis, further supporting its utility in studies related to kidney health.
  42. CB2 Ligand

    CB2 receptor antagonist 5 is a selective antagonist of the cannabinoid 2 (CB2) receptor, which plays a crucial role in the endocannabinoid system. This compound effectively inhibits CB2 receptor signaling, making it valuable for studying pain modulation, inflammation, and immune responses. It serves as a useful tool in research aimed at understanding the therapeutic potential of CB2 receptor modulation in various diseases.
  43. CB2 Receptor Agonist

    CB2 receptor agonist 7 is a selective agonist for the cannabinoid 2 (CB2) receptor, exhibiting permeability across the blood-brain barrier. This compound demonstrates significant biological activity in modulating cannabinoid receptor signaling, making it a valuable tool for studying the role of CB2 receptors in neuroinflammation and pain management research. Its unique properties enable exploration of therapeutic applications for various neurological disorders.
  44. CB1/CB2 Ligand

    PSB-SB-1203 is a dual ligand for CB1 and CB2 receptors, functioning as a CB1 antagonist and a CB2 agonist (CB1 Ki 0.244 μM; CB2 Ki 0.210 μM; EC50 0.054 μM). This compound demonstrates significant potential for research in the fields of obesity and cancer, providing valuable insights into the role of cannabinoid receptors in these conditions. Its unique mechanism of action may help to elucidate therapeutic pathways and contribute to the development of targeted treatments.
  45. CB2 Inverse Agonist

    SMM-189 is a potent and selective inverse agonist of the cannabinoid receptor 2 (CB2). This compound demonstrates significant biological activity relevant to the modulation of inflammatory and neuroprotective pathways, making it a valuable tool in the investigation of neurodegenerative disorders and traumatic brain injury. Its selective targeting of the CB2 receptor provides insights into therapeutic approaches for conditions associated with these pathologies.
  46. CB2 Receptor Agonist

    MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2) with an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. It demonstrates strong affinity for both human and rat CB2 receptors, indicated by Ki values of 422 nM and 238 nM, respectively. MDA7 exhibits notable analgesic effects in rat models, making it a valuable tool for researching cannabinoid signaling and pain modulation.
  47. Cannabinoid

    Cannabicitran is a cannabinoid that primarily targets the endocannabinoid system. It has been shown to decrease intraocular pressure in rabbit models, indicating potential therapeutic applications in the treatment of glaucoma and other ocular conditions. This compound may also be useful in studying cannabinoid receptor pathways and their biological effects.
  48. Cannabinoid Receptor Antagonist

    CE-178253 benzenesulfonate is a cannabinoid receptor 1 (CB1) antagonist that effectively interferes with cannabinoid signaling in the central nervous system. Its inhibition of CB1 receptors makes it a valuable tool for studying the roles of endocannabinoids in various physiological processes and potential therapeutic applications for addiction and neurological disorders. This compound serves as an important reagent for researchers investigating cannabinoid receptor modulation and its implications in pharmacology.
  49. CB2 Receptor Agonist

    L-759656 is a selective agonist of the cannabinoid CB2 receptor, demonstrating a Ki of 11.8 nM for the human receptor. This compound effectively inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 value of 3.1 nM. L-759656 serves as a valuable tool for investigating immune-related and inflammatory diseases.
  50. Stable Isotope

    Olivetol-d9 is a deuterium-labeled derivative of Olivetol, a naturally occurring phenol primarily found in lichens and produced by specific insects. It functions as a competitive inhibitor of cannabinoid receptors CB1 and CB2, thus influencing endocannabinoid signaling pathways. Additionally, Olivetol-d9 has inhibitory effects on the cytochrome P450 enzymes CYP2C19 and CYP2D6, making it a valuable tool in pharmacological research and studies related to cannabinoid biology.

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