AM251

SKU: orb1307120

Description

AM251 is a potent and selective cannabinoid receptor 1 (CB1) antagonist (IC50: 8 nM; Ki: 7.49 nM) with a 306-fold selectivity over CB2. It also acts as an effective GPR55 agonist (EC50: 39 nM). This compound is widely used in vitro and in vivo to investigate the endocannabinoid system in metabolic, neurological, and pain research.

Research Area

Neuroscience

Key Properties

• CAS Number: 183232-66-8
• MW: 555.24
• Purity: >98%
• Formula: C₂₂H₂₁Cl₂IN₄O
• SMILES: CC1=C(N(N=C1C(NN2CCCCC2)=O)C3=C(Cl)C=C(Cl)C=C3)C4=CC=C(I)C=C4
• Target: GPCR
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 13 mg/ml)

Bioactivity

• Target IC50:
  CB1:8 nM|GPR55:39 nM
• In Vivo:
  AM251 inhibits equilibrium binding by accelerating the dissociation of the [3H]-batrachotoxinin A 20-α-benzoate: sodium channel complex through a conformational change. It increases the dissociation constant (Kd) of the radioligand by 2.3 times without affecting the maximum binding capacity (Bmax). Furthermore, AM251 reduces the release of tetrodotoxin-inhibitory L-glutamate (IC50: 8.5 μM) and GABA (IC50: 9.2 μM) from synaptosomes in a veratridine-dependent manner. It also decreases unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, along with reducing the synthesis of cholesteryl esters in both CB2+/+ and CB2-/- peritoneal macrophages.
• In Vitro:
  AM251 inhibits memory consolidation in avoidance tasks. Compared to the control group, AM251 significantly reduces latency in tested subjects, yet no difference is observed in open field adaptive tasks, including the number of crossroads. In related fear memory tests, animals pre-treated with AM251 (4.0/8.0 mg/kg) exhibit enhanced rigidity. AM251 consistently decreases daily food intake in rats, induces selective feeding, and behaviors associated with nausea, without affecting the rate of consumption.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AM 251, AM251, AM-251, Cannabinoid Receptor, CannabinoidReceptor, CB1, CB, inhibit, Inhibitor, GPR55

Compound Identifiers

PubChem CID

2125