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AM 4113
- Soluble in DMSO
- MF: C17H12Cl3N3O
- MW: 380.66
Description
AM4113 is a high-affinity neutral antagonist of the cannabinoid CB1 receptor, with Ki values of 0.89 nM for CB1 and 92 nM for human CB2. It therefore displays approximately 100-fold binding selectivity for CB1 over CB2.
Unlike CB1 inverse agonists, AM4113 shows little effect on basal cyclic-AMP signaling in the absence of agonist, allowing blockade of endocannabinoid responses without strong inverse efficacy. It is used to investigate CB1 receptor function in feeding, reward, substance-use and metabolic behavior.
Key Features
- High-affinity CB1 neutral antagonist
- Ki: 0.89 nM for CB1
- Approximately 100-fold selectivity over human CB2
- Minimal inverse agonist activity in cAMP assays
Applications
- CB1 receptor pharmacology
- Endocannabinoid signaling studies
- Neutral antagonist versus inverse agonist comparisons
- Feeding and metabolic behavior
- Reward and addiction research
More Information
| Parent CAS No. | 614726-85-1 |
|---|---|
| Chemical Name | 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide |
| SMILES | C1(N2N=C(C(N)=O)C(C)=C2C2C=CC(Cl)=CC=2)C=CC(Cl)=CC=1Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C17H12Cl3N3O/c1-9-15(17(21)24)22-23(14-7-6-12(19)8-13(14)20)16(9)10-2-4-11(18)5-3-10/h2-8H,1H3,(H2,21,24) |
| InChiKey | BBUKVPCUOHFAQN-UHFFFAOYSA-N |
| CID | 66844170 |
| Short Description | CB1 antagonist |
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