(R,S)-AM1241 Property

Boiling point:

630.7±55.0 °C(Predicted)

Density 

1.60±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: ~18mg/mL at 60°C

pka

9.73±0.10(Predicted)

form 

solid

color 

yellow

Safety

Hazard Codes 

Xn

Risk Statements 

36/37/38-42/43

Safety Statements 

22-26-36/37-45

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H334May cause allergy or asthma symptoms or breathing difficulties if inhaled

H335May cause respiratory irritation

Precautionary statements

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

(R,S)-AM1241 Chemical Properties,Usage,Production

Description

AM1241 is a cannabinoid (CB) receptor agonist that is selective for CB₂ over CB₁ with K_i values of 7.1 and 580 nM for human recombinant receptors transfected into HEK and CHO cells, respectively, in a radioligand binding assay. It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized. It is also acts in a species-dependent manner in vitro, acting as an agonist at human CB₂ receptors (EC₅₀ = 190 nM) but an inverse agonist at rat and mouse CB₂ receptors (EC₅₀s = 216 and 463 nM, respectively). AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB₂ receptor-selective antagonist AM630 but not by the CB₁ receptor-selective antagonist AM251 . AM1241 is neuroprotective, preventing HIV-1 glycoprotein Gp120-induced apoptosis in primary human and murine neural progenitor cells and increasing cell survival and differentiation. It increases hippocampal neurogenesis and decreases astro- and gliogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days. AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).

Uses

(R,S)-AM1241 has been used as a cannabinoid CB2 agonist:

• to study its inhibitory effect on bone cancer-induced pain and bone loss
• to study the effect of its interaction with 17βestradiol on proliferation activity in primary human osteoblasts
• to evaluate the sites of CB2 mediated antinociception in vivo.

Uses

(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone is a compound from the aminkalkylindole family which exerts potent and selective agonist activity for the cannabinoid receptor CB2.

Biochem/physiol Actions

AM1241 acts as an antinociceptive agent in several animal pain models. It has a potential to delay disease progression in amyotrophic lateral sclerosis (ALS) mouse model. Intrathecal, intravenous or intraperitoneal administration of AM1241 reduces hyperalgesia and allodynia in neuropathic rats.

target

CB2