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AM-1241 is a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 3.4nM at CB2 and 80x selectivity over the related CB1 receptor. AM1241 exhibits high affinity and selectivity for CB2 receptors. It also exhibits high potency in vivo. AM1241 dose-dependently reversed tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM1241 also inhibited flinching and thermal hyperalgesia produced by hind paw capsaicin injection. AM1241 was also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM1241 reverses sensory hypersensitivity independent of actions at CB1 receptors. Treatment with AM-1241 reduced both spontaneous and evoked pain, as well as reducing the bone loss and subsequent fractures due to the tumor.
| Molecular Weight | 503.33 |
| Formula | C22H22IN3O3 |
| CAS Number | 444912-48-5 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cannabinoid Products |
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| Org 27569
Org 27569 is a potent and selective allosteric modulator of the cannabinoid CB1 receptor. |
| CP 945598 hydrochloride
CP 945598 hydrochloride is a selective and high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively). |
| AM-2201
AM-2201 is a potent synthetic cannabinoid (CB) with Ki values of 1.0 and 2.6 nM for the CB1 and CB2 receptors, respectively. |
| 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. |
| BML-190
BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor. |
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