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CB1/2 Receptor Agonist
CB1/2 Receptor-1 is a potent agonist of the CB1 and CB2 receptors, playing a significant role in modulating cannabinoid signaling pathways. This compound exhibits key biological activities relevant to angiogenesis research, offering valuable insights into vascular growth and development mechanisms. It serves as an essential tool for investigators exploring the therapeutic potential of cannabinoid receptors in various biological contexts. -
CB2 Receptor Agonist
CB2 receptor agonist 4 is a highly selective agonist for the cannabinoid receptor type 2 (CB2) with an EC50 of 13.99 nM. This compound demonstrates minimal activity against cannabinoid receptor type 1, ensuring specificity in its biological effects. CB2 receptor agonist 4 is intended for use in research related to pain modulation and immune-related diseases, making it valuable for studies investigating therapeutic strategies in these areas. -
CB1 Receptor Probe
IDFP (iso-Prdodecylfluorophosphonate) is a chemical affinity probe specifically targeting the cannabinoid CB1 receptor. This compound is utilized in research to investigate the role of the CB1 receptor in various physiological processes and neurological conditions. Its selective binding properties make IDFP a valuable tool for studying cannabinoid signaling pathways and their implications in pharmacology and therapeutics. -
CB2R Ligand
CB2R ligand-1 (Compound L14) is a highly selective ligand for the Cannabinoid type 2 receptor (CB2R), demonstrating a Ki of 0.16 nM, indicating significant potency over CB1R. This compound is valuable for research applications involving positron emission tomography (PET) imaging, particularly in the study of neurodegenerative diseases, inflammation, and cancer. Its specificity provides a useful tool for elucidating the role of CB2R in various pathological conditions. -
Cannabinoid Mimetics
1'-Naphthoyl-2-methylindole is a cannabinoid mimetic that interacts with cannabinoid receptors, demonstrating inhibitory effects on [3H]Win 55212-2 binding. At a concentration of 3 μM, it inhibits 34% of binding, providing utility in studies focused on cannabinoid receptor regulation and signaling pathways. This compound is valuable for research applications investigating the pharmacological effects of cannabinoids and their potential therapeutic uses. -
Cannabinoid Receptors Agonist
MDMB-FUBICA is a potent agonist of the cannabinoid receptors, exhibiting psychoactive properties that support its use in various research applications. This compound is particularly relevant for the study of electronic cigarette formulations and their interactions with cannabinoid pathways. Its unique pharmacological profile makes it a valuable tool for investigating the effects of cannabinoids on neural activity and behavior. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB2R Probe
CB2R Probe 1 is a fluorescent probe targeting the cannabinoid 2 receptor (CB2R), with an affinity (Ki) of 130 nM. This probe exhibits low cytotoxicity in cancer cell lines, making it suitable for cellular imaging and receptor studies. It is ideal for research applications focused on CB2R-related signaling pathways and their implications in cancer biology. -
Anandamide Analogue
(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide is an analogue of the endogenous cannabinoid receptor ligand anandamide, targeting both CB1 and CB2 receptors. This compound exhibits weak binding affinity to these receptors, with inhibition constants (Kis) measured at 21 μM. Its potential applications in research include studies on cannabinoid signaling pathways and exploring the therapeutic effects of cannabinoid receptor modulation. -
Cannabinoid Receptor Antagonist
Hemopressin (human, mouse) TFA targets the cannabinoid CB1 receptor as a selective inverse agonist. This nonapeptide, derived from the α1-chain of hemoglobin and originally isolated from rat brain homogenates, demonstrates oral bioavailability. Hemopressin TFA has been shown to exert antinociceptive effects in models of inflammatory pain, making it valuable for research in pain management and cannabinoid signaling pathways. -
CB1R/iNOS Antagonist
(Rac)-Zevaquenabant is a potent cannabinoid receptor type 1 (CB1R) and iNOS antagonist, exhibiting a Ki value of 5.7 nM for CB1R. This compound is primarily utilized in studies related to liver fibrosis, providing valuable insights into its pathophysiology and potential therapeutic interventions. Its selective inhibition of CB1R and iNOS pathways makes it a significant tool for investigating cannabinoid signaling and its implications in fibrotic diseases. -
Stable Isotope
2-Arachidonoylglycerol-d11 is a deuterated form of 2-arachidonoylglycerol, a naturally occurring cannabinoid that acts as an endogenous ligand for cannabinoid receptors in the central nervous system. This stable isotope is useful for tracing and quantifying the metabolism of endocannabinoids in various biological studies. Its applications include pharmacokinetic research and studies of cannabinoid signaling pathways. -
CB2R/FAAH Modulator
CB2R/FAAH modulator-2 is a dual-targeting modulator that functions as an agonist of the cannabinoid receptor 2 (CB2R) and an inhibitor of fatty acid amide hydrolase (FAAH). It exhibits Ki values of 10.8 nM for CB2R and 152.9 nM for CB1R, with an IC50 of 6.2 μM for FAAH. This compound is suitable for investigating therapeutic applications in cancer, neurodegenerative diseases characterized by inflammatory processes, and potential impacts on COVID-19 infection pathways. -
CB1 Agonist
Docosatetraenylethanolamide (DEA) is a potent cannabinoid receptor 1 (CB1) agonist. It exhibits significant inhibition of the specific binding of cannabinoid probes to rat synaptosomal membranes, demonstrating a Ki value of 34.4 nM. DEA is valuable in the study of neurological processes and the role of cannabinoids in the nervous system. -
CB2R Agonist
CB2R Agonist 1 is a selective agonist for the cannabinoid receptor subtype 2 (CB2R) with an EC50 of 0.56 µM, demonstrating high affinity and specificity for human CB2R. This compound modulates the production of both pro-inflammatory and anti-inflammatory cytokines, highlighting its potential for immunomodulatory effects. It is a valuable tool for research in inflammation and immune response pathways. -
Cannabinoid Analog
R-2 Methanandamide is a cannabinoid analog that selectively interacts with cannabinoid receptors, exhibiting a Ki value of 119 nM as determined in rat brain membranes. This compound is primarily utilized in research to investigate the effects of cannabinoid signaling on various physiological processes. Its structural similarity to Anandamide enables the exploration of its potential applications in neuropharmacology and the understanding of endocannabinoid system modulation. -
CB1 Receptor Agonist
LBP1 is an orally active CB1 receptor agonist with low brain penetrance. It demonstrates notable anti-allodynic and anti-hyperalgesic properties in rodent models of neuropathic pain. This compound is valuable for research aimed at understanding pain mechanisms and evaluating potential therapeutic strategies targeting cannabinoid receptors. -
CB1 Receptor Agonist
S-2 Methanandamide is a potent agonist of the CB1 receptor, exhibiting an IC50 value of 173 nM in the presence of PMSF. It demonstrates significantly lower activity at the CB2 receptor, with an IC50 value of 8216 nM. This compound is primarily utilized in research applications investigating cannabinoid receptor signaling and the physiological effects of endocannabinoids. -
S1R Antagonist
CM304 free base is a potent antagonist of the sigma-1 receptor (S1R). It enhances the antinociceptive effects of cannabinoid receptor agonists and exhibits anticonvulsant properties, effectively inhibiting convulsions in rat models. This compound is valuable for research applications focusing on pain modulation and seizure management. -
CB1R Inverse Agonist
TC-C 14G is a potent inverse agonist of the Cannabinoid-1 Receptor (CB1R), exhibiting a Ki value of 4 nM and an EC50 of 11 nM for HCB1R. This compound is valuable for research exploring the role of CB1R in various physiological processes and the pathophysiology of diseases related to cannabinoid signaling. Its efficacy in modulating CB1R activity makes it a significant tool for studies focused on neurobiology, appetite regulation, and potential therapeutic interventions. -
CB1 Receptor Antagonist
Amauromine is a selective antagonist of the cannabinoid receptor type 1 (CB1), displaying Ki and Kb values of 178 nM and 66.6 nM, respectively. Its pharmacological profile makes it a valuable tool for exploring the role of CB1 receptors in various physiological processes. Amauromine is applicable in research related to cannabinoid pharmacology, metabolic disorders, and potential therapeutic interventions targeting the endocannabinoid system. -
Dopamine Activator/CB1 Receptor Ligand
BB-22 is a potent CB1 receptor ligand that acts as a dopamine activator. It exhibits a high affinity for CB1 receptors with a Ki value of 0.11 nM and demonstrates effective activation with an EC50 value of 2.9 nM. This compound may be valuable in studying the roles of endocannabinoid and dopaminergic systems in various neurological and psychiatric disorders. -
CB1R Inverse Agonist
CB1R Antagonist 1 is a selective inverse agonist of the cannabinoid-1 receptor (CB1R) with an IC50 value of 4.2 μM. This compound effectively modulates CB1R activity, making it a valuable tool for investigating metabolic processes and obesity-related pathways. Its specificity and potency facilitate research into the therapeutic potential of targeting CB1R in metabolic disorders. -
CB1R Antagonist
BNS808 is a selective antagonist of the cannabinoid-1 receptor (CB1R), demonstrating an IC50 value of 0.8 nM while exhibiting notable selectivity for the CB2 receptor and limited central nervous system penetration. This compound is primarily utilized in research focused on obesity and its related metabolic disorders, including metabolic dysfunction-associated steatotic liver disease (MASLD). BNS808's reduced availability for CNS entry enhances its safety profile and minimizes the potential for drug-drug interactions due to high plasma protein binding. -
CB1 Agonist
CB1/2 agonist 4 serves as a full agonist for the CB1 receptor and a partial agonist for the CB2 receptor, exhibiting EC50 values of 15.09 nM and 1.16 nM, respectively. It demonstrates high affinity for human CB1 and CB2 receptors, with Ki values of 1.1 nM and 4.2 nM. This compound displays notable antinociceptive activity and effectively activates both cannabinoid and TRPV1 receptors, featuring IC50 and EC50 values of 0.8 μM and 0.12 μM, respectively. CB1/2 agonist 4 is valuable for studies exploring cannabinoid receptor functions and their implications in pain modulation. -
CB1/CB2 Receptor Agonists
O-2545 hydrochloride acts as a highly potent agonist for both CB1 and CB2 receptors, exhibiting Ki values of 1.5 nM and 0.32 nM, respectively. This water-soluble compound is valuable for research applications in epilepsy, pain management, and multiple sclerosis. Its selective interaction with cannabinoid receptors makes it a useful tool for exploring therapeutic pathways related to these conditions. -
CB1R Inverse Agonist
MK-5596 is a selective and orally active inverse agonist of the cannabinoid receptor 1 (CB1R), exhibiting an IC50 of 1.0 nM and an EC50 of 5.8 nM. This compound demonstrates significant biological activity in promoting weight loss and appetite suppression. Additionally, MK-5596 exhibits mild inhibitory effects on several cytochrome P450 enzymes, including CYP3A4, CYP2C8, CYP2C9, and CYP2D6, with IC50 values ranging from 3.3 to 18 μM. This reagent is primarily utilized in research focused on obesity and its associated metabolic disorders. -
CB1/2 Inhibitor
AM12814 is a potent and selective inhibitor of cannabinoid receptors CB1 and CB2, demonstrating Ki values of 0.7 nM and 3.4 nM, respectively. This compound effectively inhibits cAMP accumulation and promotes β-arrestin 2 recruitment, mimicking cannabimimetic effects. AM12814 is suitable for research applications related to neurological diseases, including studies on catalepsy. -
CB1 Ligand
O-1812 is a selective cannabinoid receptor type 1 (CB1) ligand, primarily targeting the CB1 receptor involved in the endocannabinoid system. It exhibits weak inhibition of the enzyme amine oxidase (AMT), making it a useful tool in investigations of neuropharmacology. This compound can be applied in research focused on chronic pain, migraines, and inflammation, contributing to the understanding of these conditions at the molecular level. -
CB1 Receptor Antagonist
rel-O-2050 is a neutral antagonist of the cannabinoid CB1 receptor. It effectively inhibits the activity of this receptor, which is implicated in the regulation of appetite and energy balance. Research indicates that rel-O-2050 can decrease food intake in murine models, making it a useful tool for studying cannabinoid signaling and its effects on metabolism and appetite control. -
CB2R Agonist/FAAH Inhibitor
CB2R/FAAH modulator-1 is a potent full agonist of the cannabinoid type 2 receptor (CB2R), exhibiting a binding affinity with a Ki of 14.8 nM for CB2R and 241.3 nM for CB1R. This compound also serves as an inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 of 4 μM. CB2R/FAAH modulator-1 is effective in modulating cytokine production by decreasing pro-inflammatory cytokines while enhancing anti-inflammatory cytokine levels, making it valuable for research in inflammation and pain modulation. -
CB1 Antagonist
AZD-2207 is a potent antagonist of the cannabinoid receptor CB1, exhibiting high lipophilicity and favorable intestinal permeability in the Caco-2 model. This compound is particularly relevant in research focused on metabolic disorders such as type 2 diabetes and obesity, facilitating investigations into potential therapeutic strategies for these conditions. -
CB1/2 Agonist
CB1/2 Agonist 2 is a potent non-selective cannabinoid ligand that targets the cannabinoid receptors CB1 and CB2. With Ki values of 3.5 nM and 1.2 nM, respectively, it functions as a full agonist at CB1 while acting as a competitive inverse agonist at CB2. This compound demonstrates significant antinociceptive activity, making it a valuable tool for research in pain management and cannabinoid signaling pathways. -
CB1R Allosteric Modulator
CB1R Allosteric Modulator 2 is a potent allosteric inhibitor of the cannabinoid receptor type 1 (CB1R). This compound negatively modulates the functional activity of orthosteric ligands at CB1Rs, acting as a negative allosteric modulator (NAM). Its unique mechanism makes it a valuable tool for studying the effects of cannabinoid signaling and its downstream biological pathways, providing insights into potential therapeutic applications in neurological disorders and metabolic regulation. -
CB1R Modulator
GAT564 is a potent allosteric modulator of the cannabinoid 1 receptor (CB1R), exhibiting EC50 values of 87 nM for cAMP and 320 nM for β-arrestin2. This compound enhances orthosteric ligand binding to hCB1R, indicating its role in modulating receptor activity. In research applications, GAT564 demonstrates significant efficacy as a topical agent, effectively reducing intraocular pressure (IOP) in ocular normotensive murine models of glaucoma. -
E Configuration Of RNB-61
(E)-RNB-61 is an orally active cannabinoid receptor agonist, specifically targeting the CB2 receptor with a Ki range of 0.13 nM to 1.81 nM. This compound exhibits notable renal protective and anti-fibrotic properties, making it a valuable tool for research in renal disease and fibrosis models. Its selective action on the CB2 receptor positions (E)-RNB-61 as a promising candidate for studies investigating the therapeutic potential of cannabinoids in inflammatory and fibrotic conditions. -
CB1R Allosteric Modulator
CB1R Allosteric Modulator 1 is a potent allosteric modulator targeting the cannabinoid receptor type 1 (CB1R). It functions as a negative allosteric modulator, inhibiting the activity of orthosteric ligands at CB1Rs. This compound is valuable for exploring the role of CB1R in various physiological processes and has potential applications in research related to neuropharmacology and therapeutic development for disorders influenced by the endocannabinoid system. -
CB1 Activator
AM841 is an electrophilic ligand that acts as a high-affinity activator of the CB1 cannabinoid receptor. By covalently binding to a cysteine residue in helix six, AM841 effectively reduces Forskolin-stimulated cAMP accumulation and has been shown to slow gastrointestinal motility. This compound is useful for research applications investigating cannabinoid receptor signaling and its physiological effects. -
CB1 Inverse agonist
TM38837 is a selective inverse agonist targeting cannabinoid receptor 1 (CB1), exhibiting an IC50 of 24 nM. With a significantly higher selectivity for CB1 over cannabinoid receptor 2 (CB2) (IC50: 4500 nM), TM38837 demonstrates potential in modulating metabolic processes. Its biological activity includes reducing body weight and improving plasma inflammatory markers and glucose homeostasis, making it a valuable tool for research on metabolic disorders and obesity. -
CB1R agonist
Δ9-THCB (Δ9-Tetrahydrocannabutol) is a potent agonist of the CB1 receptor, exhibiting a Ki value of 15 nM for human CB1 and 51 nM for CB2 receptors. This compound demonstrates significant analgesic and anti-inflammatory properties, making it a valuable tool for research focused on pain management and inflammation. Its partial agonistic effects on the CB1 receptor in in vivo models provide insights into cannabinoid receptor signaling and potential therapeutic applications. -
CB1/CB2 Agonist
Mead ethanolamide is an endogenous agonist of the cannabinoid receptors CB1 and CB2, exhibiting Kd values of 753 nM and 1810 nM, respectively. This compound plays a significant role in modulating cannabinoid receptor activity, making it a valuable tool for researching the endocannabinoid system's physiological and pharmacological effects. Its biological activity contributes to studies on pain management, neuroprotection, and various neurological disorders. -
Anandamide Transport Inhibitor
N-(3-Hydroxyphenyl)-arachidonoyl amide is an anandamide transport inhibitor, exhibiting an IC50 of 21.3 μM. This compound serves as a valuable tool in understanding endocannabinoid signaling and lipid metabolism. It can be utilized in research applications focusing on cannabinoid receptors and the modulation of neuronal activity. -
Anti-Analgesic Agent
Levonantradol hydrochloride is an analog of delta(9)-tetrahydrocannabinol that primarily functions as an anti-analgesic agent. It exhibits significant analgesic properties, making it valuable for research related to pain management and cannabinoid receptor studies. Its role in modulating pain pathways can aid in the development of novel therapeutic strategies for chronic pain conditions. -
CB2R Agonist
PM226 is a selective agonist of the cannabinoid receptor CB2 (Ki = 13 nM; EC50 = 39 nM) with minimal interaction with CB1 (Ki > 40 μM). This compound exhibits neuroprotective effects in both in vitro and in vivo studies, making it a valuable tool for research in neurodegenerative disorders. PM226 may also be applicable in exploring the therapeutic potential of cannabinoid receptors in various biological systems. -
Cannabinoid Receptor Antagonist
NIDA-41020 is a potent and selective antagonist of the cannabinoid receptor 1 (CB1), exhibiting a Ki value of 4.1 nM. This compound is designed for use as a radioligand in positron emission tomography (PET) studies. NIDA-41020 facilitates the investigation of CB1 receptor dynamics and its role in various biological processes, making it a valuable tool for cannabinoid research. -
Endocannabinoid
γ-Linolenoyl monoethanolamide is a fatty N-acyl ethanolamine that acts as an endocannabinoid. It is involved in modulating various physiological processes through cannabinoid receptor pathways. This compound has potential applications in research focused on pain management, inflammation, and neuroprotection, making it a valuable tool for exploring the endocannabinoid system in health and disease. -
CB1 Receptor Agonist
RVD-Hpα is a CB1 cannabinoid receptor agonist derived from an α-hemoglobin peptide with three additional amino acids. This compound acts as a positive allosteric modulator of cannabinoid receptor 2. RVD-Hpα is primarily utilized in research focused on the endocannabinoid system and its associated signaling pathways, making it valuable for studies exploring therapeutic effects related to cannabinoid receptors. -
CB1 receptor ligand
JHU-75528 is a selective ligand for the cannabinoid receptor CB1. This compound exhibits high affinity for the CB1 receptor, making it a valuable tool for studies involving cannabinoid signaling pathways. It is particularly useful in imaging research focused on the role of CB1 in various physiological and pathological processes. -
CB2R Antagonist
CB2R Antagonist 4 is a selective antagonist and inverse agonist of the cannabinoid receptor type 2 (CB2R) with a pKi of 6.54. This compound exhibits over 11-fold selectivity for CB2R when compared to CB1R, making it a valuable tool for research involving the endocannabinoid system. Its pharmacological properties allow for the exploration of CB2R's role in various neurological processes and disorders. -
CB-1 Receptor Antagonist
BMS-812204 is a selective antagonist of the cannabinoid receptor type 1 (CB-1). It demonstrates significant potential in research focused on obesity and metabolic disorders by modulating CB-1 signaling pathways. This compound serves as a valuable tool in elucidating the role of cannabinoid receptors in metabolic regulation and may aid in the development of therapeutic strategies for related conditions.

