Cannabinoid Receptors

Cannabinoid receptor agonists, antagonists and inverse agonists act on the CB1 and CB2 receptors. Cannabinoid receptor 1 (CB1) was cloned from rat brain in 1990 and shown to be a G protein-coupled receptor. Cannabinoid receptor 2 (CB2) followed in 1993 as a peripheral receptor found in immune cells and tissues such as spleen. CB1 is abundant in the central nervous system, so the two subtypes are studied in neuroscience and immunology. WIN 55,212-2 mesylate activates both receptors, while AM251 blocks CB1 and AM630 blocks CB2. PF-3845 inhibits fatty acid amide hydrolase (FAAH), the enzyme that breaks down fatty acid amide endocannabinoids.

15 Items

  • Arachidonoyl ethanolamide phosphate
    Cat. No.
    A31126

    Arachidonoyl ethanolamide phosphate

    Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases.

    Out of stock

    All 3 sizes
  • Arvanil
    Cat. No.
    A59187

    Arvanil

    Synonyms: N-Vanillylarachidonamide

    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.

    5 mg
    $70.00
    10 mg
    $135.00
    All 4 sizes
  • S-1 Methanandamide
    Cat. No.
    A59239

    S-1 Methanandamide

    Synonyms: (S)-Methanandamide

    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.

    5 mg
    $55.00
    10 mg
    $90.00
    All 3 sizes
  • CB2R ligand-1
    Cat. No.
    A59294

    CB2R ligand-1

    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.

    Out of stock

    All 3 sizes
  • (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide
    Cat. No.
    A59300

    (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide

    (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.

    Out of stock

    All 3 sizes
  • O-1812
    Cat. No.
    A59322

    O-1812

    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.

    Out of stock

    All 3 sizes
  • CB1/2 agonist 2
    Cat. No.
    A59326

    CB1/2 agonist 2

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • JHU-75528
    Cat. No.
    A59342

    JHU-75528

    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.

    1 mg
    $155.00
    5 mg
    $355.00
    All 7 sizes
  • GAT228
    Cat. No.
    A59347

    GAT228

    GAT228 is an allosteric ligand for cannabinoid receptor 1 (CB1). This compound modulates CB1 receptor activity, influencing cannabinoid signaling pathways. GAT228 is employed in research focused on cannabinoid system mechanisms, neuropharmacology, and potential therapeutic applications in pain management and metabolic disorders.

    1 mg
    $65.00
    10 mg
    $630.00
    All 2 sizes
  • 9β,10β-epoxy Hexahydrocannabinol
    Cat. No.
    A59350

    9β,10β-epoxy Hexahydrocannabinol

    Synonyms: 9β,10β-EHHC; 9β,10β-epoxy HHC

    9β,10β-epoxy Hexahydrocannabinol is a selective ligand for the cannabinoid receptors CB1 and CB2, exhibiting binding affinities of 224 nM and 335 nM, respectively. This compound has demonstrated significant biological activities, including the reduction of locomotor activity, induction of catalepsy, and lowering of body temperature, along with antinociceptive effects in murine models. Its relevant pharmacological profile makes it a valuable tool for research focused on the mechanisms underlying nervous system diseases.

    Out of stock

    All 3 sizes
  • Pirnabine
    Cat. No.
    A59355

    Pirnabine

    Pirnabine is a cannabinoid receptor ligand that selectively interacts with the CB1 and CB2 receptors. This compound has demonstrated potential in modulating intraocular pressure, making it relevant for glaucoma research. Investigating Pirnabine may provide insights into cannabinoid therapeutic strategies for ocular conditions.

    Out of stock

    All 3 sizes
  • Tocrifluor 1117
    Cat. No.
    A59377

    Tocrifluor 1117

    Synonyms: T1117

    Tocrifluor 1117 is a selective fluorescent ligand targeting the GPR55 receptor. This compound serves as a valuable tool in research for visualizing the cellular distribution of cannabinoid receptors, including GPR55, in live tissues. With excitation and emission maxima at 543 nm and 590 nm, respectively, Tocrifluor 1117 enhances the understanding of cannabinoid receptor localization and function in various biological contexts.

    0.1 mg
    $1,105.00
    All 1 sizes
  • Δ8-THC methyl ether
    Cat. No.
    A59437

    Δ8-THC methyl ether

    Δ8-THC methyl ether is a selective ligand for the CB2 receptor, exhibiting a favorable docking score of -10.167 kcal/mol. This compound demonstrates significant antinociceptive activity in murine models, highlighting its potential for research in pain management and cannabinoid receptor studies. Further investigation into its pharmacological properties may support its application in the development of therapeutics targeting the endocannabinoid system.

    Out of stock

    All 3 sizes
  • L-α-lysophosphatidylinositol (Soy) sodium
    Cat. No.
    A60822

    L-α-lysophosphatidylinositol (Soy) sodium

    L-α-lysophosphatidylinositol (Soy) sodium is a potent endogenous ligand for the GPR55 receptor. As a lysophospholipid and endocannabinoid neurotransmitter, it plays a crucial role in various signaling pathways. It is primarily utilized in research applications focusing on cannabinoid receptor modulation, cell signaling processes, and neurobiology studies.

    1 mg
    $360.00
    All 1 sizes
  • Rimonabant carboxylic acid
    Cat. No.
    A81316

    Rimonabant carboxylic acid

    Synonyms: Rimonabat acomplia

    Rimonabant carboxylic acid is a ligand used for the targeted protein degradation (PROTAC) approach by engaging with the target protein. This compound plays a crucial role in synthesizing PROTAC CB1R Degrader-1, facilitating the study of cannabinoid receptor biology and influencing metabolic processes. It serves as a valuable tool for researchers investigating innovative therapeutic strategies for conditions related to the endocannabinoid system.

    1 g
    $20.00
    5 g
    $45.00
    All 6 sizes

15 Items

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