Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.


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RTICBM-189

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats[1].

  • CAS Number: 551909-15-0
  • MF: C15H14Cl2N2O
  • MW: 309.19
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-arachidonoylglycerol

2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.

  • CAS Number: 53847-30-6
  • MF: C23H38O4
  • MW: 378.545
  • Catalog: Cannabinoid Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 508.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 163.0±23.6 °C

Rimonabant-d10

Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

  • CAS Number: 929221-88-5
  • MF: C22H11D10Cl3N4O
  • MW: 473.85
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AM841

AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility[1][2].

  • CAS Number: 871978-21-1
  • MF: C26H39NO3S
  • MW: 445.66
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Palmitoyl serinol-d5

Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].

  • CAS Number: 946524-35-2
  • MF: C19H34D5NO3
  • MW: 334.55
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZCZ011

ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain[1].

  • CAS Number: 1998197-39-9
  • MF: C21H18N2O2S
  • MW: 362.44
  • Catalog: Cannabinoid Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 602.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 318.4±31.5 °C

OMDM-6

OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM[1].

  • CAS Number: 616884-67-4
  • MF: C28H42N2O3
  • MW: 454.64
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY320135

LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect[1][2].

  • CAS Number: 176977-56-3
  • MF: C24H17NO4
  • MW: 383.39600
  • Catalog: 5-HT Receptor
  • Density: 1.31g/cm3
  • Boiling Point: 617.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 327.1ºC

Nimacimab

Nimacimab (RYI-018) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases[1][2].

  • CAS Number: 2098636-09-8
  • MF:
  • MW:
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Org 27569

Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.

  • CAS Number: 868273-06-7
  • MF: C24H28ClN3O
  • MW: 409.952
  • Catalog: Cannabinoid Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 660.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 353.2±31.5 °C

TM 38837

TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects[1][2].

  • CAS Number: 1253641-65-4
  • MF: C30H25Cl2F3N4OS
  • MW: 617.512
  • Catalog: Cannabinoid Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anandamide-d11

Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].

  • CAS Number: 2260669-86-9
  • MF: C22H26D11NO2
  • MW: 358.60
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LEI 101 hydrochloride

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors[1][2].

  • CAS Number: 2250025-91-1
  • MF: C23H26ClFN4O4S
  • MW: 508.99
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anandamide

Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).

  • CAS Number: 94421-68-8
  • MF: C22H37NO2
  • MW: 347.535
  • Catalog: Cannabinoid Receptor
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 522.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 269.7±30.1 °C

PSNCBAM-1

PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity[1].

  • CAS Number: 877202-74-9
  • MF: C22H21ClN4O
  • MW: 392.88100
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: 521.5±50.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

CB1R Allosteric modulator 4

CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment[1].

  • CAS Number: 2633686-53-8
  • MF: C20H17N3O2S
  • MW: 363.43
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY 38-7271

BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties[1].

  • CAS Number: 212188-60-8
  • MF: C20H21F3O5S
  • MW: 430.43800
  • Catalog: Cannabinoid Receptor
  • Density: 1.351 g/cm3
  • Boiling Point: 527.206ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 272.645ºC

GW842166X

GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.

  • CAS Number: 666260-75-9
  • MF: C18H17Cl2F3N4O2
  • MW: 449.254
  • Catalog: Cannabinoid Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

WIN 55212-2 mesylate

WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

  • CAS Number: 131543-23-2
  • MF: C28H30N2O6S
  • MW: 522.613
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: 627.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 333.4ºC

KM-233

KM-233 is a classical cannabinoid with good blood brain barrier penetration. KM-233 possesses a selective affinity for the CB2 receptors relative to THC. KM-233 is effective at reducing U87 glioma tumor burden, and can be used for glioma research[1].

  • CAS Number: 628263-22-9
  • MF: C25H30O2
  • MW: 362.50
  • Catalog: Cannabinoid Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 436.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 171.9±23.0 °C

(R)-Monlunabant

(R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease[1]

  • CAS Number: 2765579-76-6
  • MF: C26H22ClF3N6O3S
  • MW: 591.00
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CB1 antagonist 1

CB1 antagonist 1 is an antagonist of CB1 receptor, used in the research of metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, gastrointestinal disorders, and cardiovascular conditions.

  • CAS Number: 890037-68-0
  • MF: C26H22Cl2N4
  • MW: 461.39
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CB1 inverse agonist 1

CB1 inverse agonist 1 is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects[1].

  • CAS Number: 852315-00-5
  • MF: C25H18Cl3N3O3
  • MW: 514.79
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isopropyl 11-dodecen-1-ylphosphonofluoridate

Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM)[1].

  • CAS Number: 623114-64-7
  • MF: C15H30FO2P
  • MW: 292.370
  • Catalog: Cannabinoid Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 351.5±11.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 166.4±19.3 °C

Voacamine

Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity[1]. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells[1].

  • CAS Number: 3371-85-5
  • MF: C43H52N4O5
  • MW: 704.89700
  • Catalog: Cannabinoid Receptor
  • Density: 1.309g/cm3
  • Boiling Point: N/A
  • Melting Point: 223℃
  • Flash Point: N/A

CB1R Allosteric modulator 2

CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs[1].

  • CAS Number: 2513102-64-0
  • MF: C19H15ClFN3O
  • MW: 355.79
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Arachidonylcyclopropylamide

Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM)[1].

  • CAS Number: 229021-64-1
  • MF: C23H37NO
  • MW: 343.546
  • Catalog: Cannabinoid Receptor
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 502.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 311.3±15.1 °C

N-Arachidonoyl dopamine

N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM[1]. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM[2].

  • CAS Number: 199875-69-9
  • MF: C28H41NO3
  • MW: 439.630
  • Catalog: Cannabinoid Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 640.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 340.8±31.5 °C

oleoylglycine

N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.

  • CAS Number: 2601-90-3
  • MF: C20H37NO3
  • MW: 339.513
  • Catalog: Cannabinoid Receptor
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 525.6±43.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 271.7±28.2 °C

AM281

AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].

  • CAS Number: 202463-68-1
  • MF: C21H19Cl2IN4O2
  • MW: 557.212
  • Catalog: Cannabinoid Receptor
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A