| S8012 |
Otenabant (CP-945598) HCl |
Otenabant (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. |
Selective |
hCB1, Ki: 0.7 nM; rCB1, Ki: 2.8 nM |
| S6735 |
JD-5037 |
JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor. |
Selective |
CB1 receptor, IC50: 2 nM |
| S3021 |
Rimonabant (SR141716) |
Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3. |
Selective |
hCB1, IC50: 13.6 nM |
| S1534 |
Org 27569 |
Org 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. |
Selective |
|
| S2819 |
AM251 |
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. |
Selective |
|
| S0412 |
Bay 59-3074 |
Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. Bay 59-3074 displays analgesic properties. |
Pan |
rat CB1 receptor, Ki: 55.4 nM; human CB1 receptor, Ki: 48.3 nM |
| S1544 |
AM1241 |
AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor. |
Pan |
CB1, Ki: 280 nM |
