Cannabinoid Receptor
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Isoform-specific Inhibitors
Cannabinoid Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
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| S9413New |
YangoninYangonin is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
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| S3021 |
RimonabantRimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. |
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| S2819 |
AM251AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
Effect of AM251 treatment on the CORT response to stress. Group-housed and socially isolated rats were intraperitoneally injected with AM251 or vehicle 30 min before exposure to foot-shock stress, and were sacrificed 30 min thereafter. Non-shocked controls were sacrificed 60 min after injection. Data are mean ± SEM of values from 10 rats per group and are expressed as ng/ml of plasma. Data were analyzed by three-way ANOVA (housing × drug treatment × stress conditions) followed by Newman-Keuls post-hoc test. ap<0.01 vs. the respective non-shocked controls; bp < 0.01 vs. group-housed vehicle-treated rats; cp < 0.01 vs. group-housed vehicle-treated + foot-shock rats.
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| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1. |
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| S8694New |
CID16020046 (CID 16020046)CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. |
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| S1544 |
AM1241AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
The expression of cannabinoid receptor type II, Akt, p-Akt, HO-1, Nrf2 in cytosol and Nrf2 in nucleus were detected by Western blot.
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| S2854 |
BML-190BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
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| S2778 |
GW842166XGW842166X 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. |
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| S1534 |
Org 27569Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. |
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| S9048New |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S5119 |
OlivetolOlivetol is a naturally occurring organic compound being a precursor in various syntheses of tetrahydrocannabinol. It acts as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9413New |
YangoninYangonin is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3021 |
RimonabantRimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. |
||
| S2819 |
AM251AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
Effect of AM251 treatment on the CORT response to stress. Group-housed and socially isolated rats were intraperitoneally injected with AM251 or vehicle 30 min before exposure to foot-shock stress, and were sacrificed 30 min thereafter. Non-shocked controls were sacrificed 60 min after injection. Data are mean ± SEM of values from 10 rats per group and are expressed as ng/ml of plasma. Data were analyzed by three-way ANOVA (housing × drug treatment × stress conditions) followed by Newman-Keuls post-hoc test. ap<0.01 vs. the respective non-shocked controls; bp < 0.01 vs. group-housed vehicle-treated rats; cp < 0.01 vs. group-housed vehicle-treated + foot-shock rats.
|
|
| S8012 |
Otenabant (CP-945598) HClOtenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1. |
||
| S8694New |
CID16020046 (CID 16020046)CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1544 |
AM1241AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
The expression of cannabinoid receptor type II, Akt, p-Akt, HO-1, Nrf2 in cytosol and Nrf2 in nucleus were detected by Western blot.
|
|
| S2854 |
BML-190BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
The effect of BML-190 on DSS-treated Rassf1a +/- mice. DSS-treated Rassf1a+/- mice were given 3% DSS in drinking water for 7 days followed by fresh water for recovery for another 7 days. BML-190 was administrated orally (100µg/g body weight) on days 2, 4, 5and 7. BML-190 did not protect DSS-treated Rassf1a+/- from inflammation induced injury. n=6-10 for all. |
|
| S2778 |
GW842166XGW842166X 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. |
||
| S1534 |
Org 27569Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9048New |
(+)-Gallocatechin(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
