GPCR/G Protein

Tetrahydromagnolol, a potent and selective agonist of the cannabinoid CB2 receptor, exhibits an EC50 value of 170 nM. It has a binding affinity (Ki) for the CB2 receptor of 416 nM, which is significantly higher compared to the CB1 receptor. This compound demonstrates notable biological activities, including antifungal, anti-inflammatory, and analgesic effects, making it valuable for research in pain management and inflammatory disorders. Additionally, its role as a GPR55 antagonist further enhances its potential utility in cannabinoid-related studies.

2-Linoleoyl glycerol is a monoacylglycerol that serves as an antagonist and partial agonist at the cannabinoid receptor type 1 (CB1). It effectively modulates the activity of cannabinoids such as anandamide (AEA) and 2-arachidonoylglycerol (2-AG) by attenuating their effects without enhancing them. This compound has significant implications in cannabinoid research, particularly in studies focused on the endocannabinoid system and potential therapeutic targets for various conditions. Additionally, its potency can be influenced by the inhibition of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).

CB1 agonist 1 is a potent agonist of the cannabinoid receptor type 1 (CB1). With a pIC50 value of 5.7, it exhibits significant binding affinity to the CB1 receptor. This compound is primarily utilized in research focusing on brain disorders, aiding in the exploration of cannabinoid signaling and its implications in neurological conditions.

PSB-KK1445 is a potent and selective GPR18 agonist, exhibiting EC50 values of 45.4 nM for human GPR18 and 124 nM for mouse GPR18. It demonstrates over 200-fold selectivity against both cannabinoid receptor subtypes, GPR55, and GPR183. This compound is valuable for research applications exploring the physiological roles of GPR18 in various biological processes and potential therapeutic uses related to the endocannabinoid system.

O1918 is a selective antagonist of the cannabinoid receptor GPR18. It effectively inhibits GPR18 signaling, making it a valuable tool for studying the role of this receptor in various physiological processes. O1918 is primarily used in research focusing on cannabinoid modulation and its effects on the endocannabinoid system.

AM281 is a selective antagonist of the cannabinoid receptor type 1 (CB1) with an IC50 value of 9.91 nM. This compound exhibits significant potency in inhibiting the CB1 receptor, while demonstrating a much lower affinity for the CB2 receptor with an IC50 of 13,000 nM. AM281 is primarily utilized in research applications related to endocannabinoid signaling, neurobiology, and the potential modulation of disorders involving CB1 receptor activity.

AM6545 is a highly selective CB1 receptor antagonist that functions peripherally without crossing the blood-brain barrier (Ki=1.7 nM). By competitively inhibiting the CB1 receptors, AM6545 disrupts endocannabinoid signaling, thereby mitigating appetite stimulation and inflammatory responses without altering cAMP levels. This compound has been shown to significantly decrease food intake and body weight in murine models while improving metabolic syndrome-related renal impairment, including proteinuria, fibrosis, and insulin resistance. AM6545 is instrumental in research focused on obesity and its associated complications.

CB1/2 Agonist 3 is a potent non-selective cannabinoid receptor agonist targeting both CB1 and CB2 receptors. With Ki values of 5.9 nM for hCB1 and 3.5 nM for hCB2, this compound exhibits significant binding affinity. It is instrumental in studying cannabinoid signaling pathways and their implications in various biological processes and therapeutic areas.

Arvanil is a selective ligand for the vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1). It exhibits potent neuroprotective properties and has been shown to inhibit spasticity. This compound is of interest in research applications focused on pain management, neuroprotection, and the modulation of endocannabinoid signaling pathways.

Arachidonylcyclopropylamide (ACPA) is a highly selective agonist of the CB1 receptors. It effectively inhibits forskolin-stimulated cAMP production in Chinese hamster ovary (CHO) cells expressing human cannabinoid CB1 receptors, exhibiting an IC50 of 2 nM. ACPA is widely utilized in research to investigate the role of endocannabinoids in physiological processes and the therapeutic potential of cannabinoid modulation.

2-Arachidonoylglycerol-d8 is a deuterated analog of 2-Arachidonoylglycerol, a natural endocannabinoid that acts as a ligand for cannabinoid receptors in the central nervous system. This stable isotope is utilized in biochemical and pharmacological research to study cannabinoid signaling and interactions. Its application includes mass spectrometry-based analysis, enabling precise quantification of endocannabinoid levels in biological samples for further investigation of their physiological roles.

CB1/2 Agonist 1 is a selective cannabinoid receptor agonist, targeting both CB1 and CB2 receptors with EC50 values of 56.15 nM and 11.63 nM, respectively. This compound effectively reduces glutamate release and LPS-induced microglial cell activation, demonstrating significant anti-inflammatory and antinociceptive properties. Due to its unique pharmacological profile, CB1/2 Agonist 1 has potential applications in research related to multiple sclerosis and other neuroinflammatory conditions.

AM-6538 is a high-affinity, pseudo-irreversible cannabinoid (CB) antagonist that serves as a valuable tool for research on cannabinoid receptor modulation. As a structural analog of rimonabant, it effectively evaluates the efficacy of both full and partial agonists at cannabinoid receptors. Additionally, AM-6538's unique alkyne group allows it to function as a click chemistry reagent, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This makes it suitable for applications that require temporary modulation of cannabinoid receptor availability.

(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays.

CB2R PAM is a positive allosteric modulator of cannabinoid type-2 receptors (CB2Rs) with oral bioavailability. This compound exhibits significant antinociceptive activity, demonstrated in vivo in mouse models of neuropathic pain. CB2R PAM offers valuable insights for research applications related to pain management and cannabinoid pharmacology.

GW 833972A is a selective agonist of the CB2 receptor, exhibiting a pEC50 value of 7.3 for human CB2. With approximately 1000-fold higher selectivity for the CB2 receptor over CB1, GW 833972A effectively inhibits induced neuronal depolarization and alleviates cough reflex in guinea pig models. This compound is valuable for research into chronic cough mechanisms and potential therapeutic interventions.

CB1 antagonist 4 is a selective inverse agonist for the cannabinoid receptor 1 (CB1), demonstrating an IC50 of 8.5 nM in human CB1 assays. This compound exhibits a notable selectivity for CB1 over CB2 receptors, with an IC50 of 604.9 nM. CB1 antagonist 4 effectively inhibits GTP binding in CB1-overexpressing cell membranes, with an EC50 of 18.5 nM, making it a valuable tool for studying CB1 receptor biology and signaling pathways.

Ibipinabant is a potent and selective antagonist of the cannabinoid CB1 receptor, exhibiting a Ki value of 7.8 nM. This compound demonstrates over 1000-fold selectivity for CB1 compared to CB2, with a Ki of 7943 nM. Ibipinabant is primarily utilized in research related to obesity and diabetes, facilitating studies on the modulation of appetite and metabolic regulation.

Eicosapentaenoyl ethanolamide is a cannabinoid receptor agonist targeting the CB1 and CB2 receptors. This omega-3 fatty acid, classified as a N-acylethanolamine, serves as a crucial metabolic signal. Research demonstrates that eicosapentaenoyl ethanolamide inhibits lifespan extension induced by dietary restriction in wild-type organisms and additionally suppresses lifespan extension in TOR pathway mutants. Its applications include studies in metabolism, aging, and cannabinoid receptor signaling.

Dihomo-γ-Linolenoyl Ethanolamide is a potent cannabinoid receptor agonist, selectively targeting human recombinant CB1 and CB2 receptors with inhibition constants (Kis) of 857 nM and 598 nM, respectively. This endocannabinoid plays a crucial role in modulating various physiological processes, making it relevant for studies in pain management, inflammation, and neuroprotection. Its unique mechanism of action positions it as a valuable tool for cannabinoid research and therapeutic exploration.

Drinabant is a potent antagonist of the CB1 receptor, specifically designed for oral activity. It effectively inhibits agonist-stimulated calcium signaling, demonstrating IC50 values of 25 nM for human CB1 receptors and 10 nM for rat CB1 receptors, while showing no efficacy against human CB2 receptors. This compound is valuable for research applications involving the endocannabinoid system and its role in various physiological processes.

SCH 336 is a potent and selective inverse agonist of the CB2 receptor. It has been shown to inhibit the migration of BaF3 cells expressing CB2, as well as significantly reduce leukocyte migration in vivo. Additionally, SCH 336 effectively blocks ovalbumin-induced eosinophilia in mouse models, making it a valuable tool for research into inflammation and immune response modulation.

CB1 inverse agonist 2 is a potent orally active inverse agonist targeting the Cannabinoid Receptor CB1. This compound effectively inhibits CP55940-induced hypothermia and anorexia in mouse models, making it a valuable tool for studying cannabinoid receptor-mediated pathways. Its ability to modulate CB1 receptor activity positions it as a significant reagent for research in neuropharmacology and metabolic disorders.

2-Palmitoylglycerol is a cannabinoid receptor CB1 agonist that shows modest binding affinity. This compound is closely related to 2-arachidonoylglycerol and may also act as an endogenous ligand for the GPR119 receptor. Its research applications include studying cannabinoid signaling pathways and exploring potential therapeutic implications in neurobiology and metabolic disorders.

AZD1940 is a high-affinity agonist for the cannabinoid receptors CB1 and CB2, exhibiting pKi values of 7.93 and 9.06, respectively. This compound demonstrates significant analgesic activity, making it a valuable tool for studying pain pathways and cannabinoid signaling. Its oral bioactivity encourages research applications in neuropharmacology and potential therapeutic development for pain management.