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Cannabinoid Receptor

Cannabinoid receptors are of a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the mammillary body;[citation needed] plant cannabinoids (such as cannabidiol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic, such as fat soluble compounds.

Tetrahydrocannabivarin
TN513131262-37-0
Tetrahydrocannabivarin (CRM) is a neutral cannabis receptor subtype (CB1) receptor antagonist, it can increases neural responding to rewarding and aversive stimuli, this effect profile suggests therapeutic activity in obesity, perhaps with a lowered risk of depressive side effects. Tetrahydrocannabivarin exhibits anticonvulsant effects in a piriform cortical brain slice model of epileptiform activity.
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    CB2R PAM
    T370752244579-87-9
    CB2R PAM is an orally active cannabinoid type 2 receptor (CB2Rs) positive allosteric modulator that enhances CP 55940 and 2-Arachidonylglycerol-stimulated [35S]GTPγS binding to CB2 receptors without affecting receptor activity in the absence of agonists. CB2R PAM shows anti-injury activity in a mouse model of neuropathic pain.
    • $51
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    (±)-Cannabichromene
    TN357520675-51-8
    (±)-Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1), it selectively reduces inflammation-induced hypermotility in vivo in a manner that is not dependent on cannabinoid receptors or TRPA1.
    • $173
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    Anandamide
    T1404694421-68-8
    Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide), an immune modulator, acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18 GPR55) in the central nervous system.
    • $66
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    2-Arachidonoylglycerol
    T1401153847-30-6
    In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand
    • $118
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    AM1241
    T6755444912-48-5
    AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
    • $32
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    AM251
    T1915183232-66-8
    AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).
    • $43
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    Drinabant
    T21861358970-97-5In house
    Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.
    • $79
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    AZD1940
    T30252881413-29-2
    AZD1940 (UNII-0J0035E9FT) is a high affinity CB(1) CB(2) receptor agonist of the cannabinoid with oral activity. Application in the study of orofacial pain.
    • $132
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    Rimonabant hydrochloride
    T1519158681-13-1
    Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.
    • $38
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    Olorinab
    T143021268881-20-4
    Olorinab (APD 371) (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.
    • $51
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    6-Iodopravadoline
    T14204164178-33-0
    6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.
    • $34
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    CB 65
    T41230913534-05-1In house
    CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively.
    • $58
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    (±)-Ibipinabant
    T4654362519-49-1
    (±)-Ibipinabant ((±)-SLV319) has been utilized in clinical trials for the treatment of obesity and type 2 diabetes.
    • $43
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    ML-184
    T8571794572-10-4
    ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with an EC50 of 0.26 μM.
    • $40
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    yangonin
    T3S0738500-62-9
    Yangonin (Y100550) is a novel CB receptor ligand, it exhibits affinity for the human recombinant CB receptor. Yangonin (Y100550) could be a valuable candidate for the intervention of NF-κB-dependent pathological conditions such as inflammation.
    • $64
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    Rimonabant
    T1519L168273-06-1
    Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.
    • $42
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    JHU 75528
    T77634947696-17-5In house
    JHU 75528 (JHU-75528) is a novel PET tracer with inhibitory effects on CB that can be used to study the cannabinoid system in schizophrenic patients.
    • $195
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    ML-193
    T22103713121-80-3
    ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson’s disease (PD) rats.
    • $39
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    SR144528
    T16928192703-06-3
    SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).
    • $36
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    N-Oleoyl glycine
    T138032601-90-3
    N-Oleoyl Glycine, a Lipoamino Acid, Stimulates Adipogenesis Associated With Activation of CB1 Receptor and Akt Signaling Pathway in 3T3-L1 Adipocyte
    • $39
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    GW 405833
    T7705180002-83-9
    GW 405833 (L-768242) is an agonist of cannabinoid-2 (CB(2)) receptor-selective
    • $31
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    AM404
    T39281183718-77-6
    AM404 is an endocannabinoid reuptake inhibitor, a TRPV(1) activator, a paracetamol metabolite, with neuroprotective and anticancer activity that blocks anandamide transport. AM404 inhibits NFAT and NF-kappaB signaling pathways and impairs migration and invasiveness of neuroblastoma cells, preventing prostaglandin synthesis in activated microglia by inhibiting COX activity.
    • $63
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    NESS 0327
    T22114494844-07-4In house
    NESS 0327 is a high selectivity antagonist of the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.
    • $127
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    JD-5037
    T44531392116-14-1
    JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
    • $37
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    JTE-907
    T19705282089-49-0
    JTE-907 is a CB2 receptor inverse agonist with high selectivity and oral activity.JTE-907 exhibits anti-inflammatory activity in vivo.
    • $51
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    AM-1235
    T29930335161-27-8In house
    AM-1235 is a potent and selective cannabinoid receptor CB1 agonist.
    • $350
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    Pregnenolone
    T0851145-13-1
    Pregnenolone (Arthenolone) is an endogenous steroid hormone synthesized from cholesterol, used in the treatment of Alzheimer's disease.
    • $45
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    CB2 modulator 1
    T10696666261-80-9In house
    CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.
    • $30
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    CID 16020046
    T4478834903-43-4
    CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.
    • $33
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    AM6545
    T225631245626-05-4
    AM6545 is a selective and potent peripheral restricted cannabinoid receptor 1 (CB1) antagonist that inhibits the CB2 receptor, ameliorates hypometabolic obesity and improves adipokine secretion in monosodium glutamate-induced obese mice, and may be useful in the study of obesity and diabetes.
    • $89
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    O-1602
    T23097317321-41-8
    O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment of cystitis.O-1602 promotes hepatic steatosis through GPR55 and PI3 kinase / Akt / SREBP-1c signalling in mice.O-1602 induces, in a GPR3-independent manner, in Hep55B cells with elevated intracellular calcium.
    • $41
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    Tetrahydromagnolol
    TN226820601-85-8
    Tetrahydromagnolol can activate cannabinoid (CB) receptors.
    • $50
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    AM-2232
    T21450335161-19-8
    AM-2232 (UNII-40KCH8YIKP) is a potent and unselective agonist of the cannabinoid receptors.
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      GW842166X
      T6527666260-75-9
      GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
      • $30
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      N-Arachidonyldopamine
      T62530199875-69-9
      N-Arachidonyldopamine (NADA) is a selective and potent endogenous CB1 receptor agonist (Ki: 250 nM).N-Arachidonyldopamine is also a potent and selective TRPV1 agonist with an EC50 value of ~50 nM.
      • $44
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      Org 27569
      T2635868273-06-7
      Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity.
      • $31
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      CB1 antagonist 2
      T14881614726-85-1
      CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.
      • $30
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      PSNCBAM-1
      T28468877202-74-9In house
      PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.
      • $48
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      CB2 receptor agonist 2
      T220091314230-75-5In house
      CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.
      • $118
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      CB2R/FAAH modulator-2
      T677452876918-68-0
      CB2R FAAH modulator-2 (compound 26) is a dual modulator targeting CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades in neurodegenerative diseases, and COVID-19 infection.
      • $31
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      AM281
      T2264202463-68-1
      AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.
      • $77
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      CB1 antagonist 4
      T85111253641-65-4
      CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.
      • $41
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      (-)-WIN 55,212-3 mesylate
      T71963131543-25-4
      (-)-WIN 55,212-3 mesylate is a low-activity enantiomer of WIN 55,212-2 mesylate with no neuroprotective activity and reduced intestinal transport. (-)-WIN 55,212-3 mesylate is a cannabinoid receptor agonist and may be used in the study of neurological disorders.
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        Taranabant
        T13080L701977-09-5
        Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence.
        • $99
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        Otenabant hydrochloride
        T1796686347-12-6
        Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).
        • $39
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        Otenabant
        T3530686344-29-6
        Otenabant (CP-945598) has been investigated for the treatment of Obesity.
        • $41
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        GAT211
        T27405102704-40-5
        GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.
        • $30
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