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. |
-
Pharmacol Res, 2023, 194:106864
-
Physiol Rep, 2023, 11(1):e15565
-
Sci Rep, 2021, 11(1):11515
|
|
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. |
-
Toxicol Lett, 2023, 374:48-56
-
Int J Biol Sci, 2022, 18(4):1401-1414
-
Mol Metab, 2022, 65:101597
|
|
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. |
-
Nat Commun, 2020, 11(1):71
-
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
|
|
S2854 |
BML-190
|
BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
-
Int J Mol Sci, 2020, 21(7)
-
University of Alberta, 2014, Yahya Muhammad Fiteih
|
|
S8033 |
6-Iodopravadoline (AM630)
|
6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM. |
-
Brain Behav Immun, 2023, 110:60-79
-
Pharmacol Res, 2023, 194:106864
|
|
S2778 |
GW842166X
|
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. |
-
Nat Commun, 2020, 11(1):71
|
|
S8017 |
WIN 55, 212-2 mesylate
|
WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. |
-
Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
|
|
E4945New |
Pregnenolone monosulfate sodium
|
Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC). |
|
|
E0458 |
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. |
|
|
E1841New |
Monlunabant
|
Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
|
E4585New |
N-Arachidonyldopamine
|
N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. |
|
|
E4858New |
Rimonabant hydrochloride
|
Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors. |
|
|
S9048 |
(+)-Gallocatechin
|
(+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant. |
|
|
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. |
|
|
S9413 |
Yangonin
|
Yangonin (Y100550) 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. |
|
|
S8694 |
CID16020046
|
CID16020046 (C390-0219) 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. |
-
Pharmacol Res, 2024, 203:107176
|
|
A2574 |
Nimacimab (Anti-CB1 / CNR1)
|
Nimacimab (Anti-CB1/CNR1) is a negative-allosteric modulating monoclonal antibody targeting CB1 receptor. Nimacimab can be used for research of metabolic diseases. MW:145.5 KD. |
|
|
A2575 |
Anti-CB1 / CNR1
|
Anti-CB1 / CNR1 (GFB-024) is a recombinant humanised monoclonal antinody that is used for targeting of CB1 receptor. MW:145.5 KD. |
|
|
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. |
|
|
S2854 |
BML-190
|
BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
-
Int J Mol Sci, 2020, 21(7)
-
University of Alberta, 2014, Yahya Muhammad Fiteih
|
|
S2778 |
GW842166X
|
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. |
-
Nat Commun, 2020, 11(1):71
|
|
S8017 |
WIN 55, 212-2 mesylate
|
WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. |
-
Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
|
|
E1841New |
Monlunabant
|
Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
|
E4585New |
N-Arachidonyldopamine
|
N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. |
|
|
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. |
|
|
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. |
- Pharmacol Res, 2023, 194:106864
- Physiol Rep, 2023, 11(1):e15565
- Sci Rep, 2021, 11(1):11515
|
|
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. |
- Toxicol Lett, 2023, 374:48-56
- Int J Biol Sci, 2022, 18(4):1401-1414
- Mol Metab, 2022, 65:101597
|
|
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. |
- Nat Commun, 2020, 11(1):71
- Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
|
|
S8033 |
6-Iodopravadoline (AM630)
|
6-Iodopravadoline (AM630) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM. |
- Brain Behav Immun, 2023, 110:60-79
- Pharmacol Res, 2023, 194:106864
|
|
E4858New |
Rimonabant hydrochloride
|
Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors. |
|
|
S8694 |
CID16020046
|
CID16020046 (C390-0219) 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. |
- Pharmacol Res, 2024, 203:107176
|
|
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. |
|
|
S2854 |
BML-190
|
BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
- Int J Mol Sci, 2020, 21(7)
- University of Alberta, 2014, Yahya Muhammad Fiteih
|
|
S2778 |
GW842166X
|
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. |
- Nat Commun, 2020, 11(1):71
|
|
S8017 |
WIN 55, 212-2 mesylate
|
WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission. |
- Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
|
|
E1841New |
Monlunabant
|
Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
|
E4585New |
N-Arachidonyldopamine
|
N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. |
|
|
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. |
|
|
E4945New |
Pregnenolone monosulfate sodium
|
Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC). |
|
|
E1841New |
Monlunabant
|
Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
|
E4585New |
N-Arachidonyldopamine
|
N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. |
|
|
E4858New |
Rimonabant hydrochloride
|
Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors. |
|
|
E1841New |
Monlunabant
|
Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
|
E4585New |
N-Arachidonyldopamine
|
N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. |
|
|