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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.

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.
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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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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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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.
  • $48
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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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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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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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    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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    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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    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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    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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    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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    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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    (±)-Ibipinabant
    T4654362519-49-1
    (±)-Ibipinabant ((±)-SLV319) has been utilized in clinical trials for the treatment of obesity and type 2 diabetes.
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    Tetrahydromagnolol
    TN226820601-85-8
    Tetrahydromagnolol can activate cannabinoid (CB) receptors.
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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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    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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    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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    PSB-SB-487
    T89751399049-81-0
    PSB-SB-487 is antagonist of GPR55.
    • $32
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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.
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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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    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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