(R,S)-AM1241

化学名:(R,S)-AM1241

CAS番号.444912-48-5

英語名:(R,S)-AM1241

CBNumberCB4972473

MFC22H22IN3O3

MW503.33

MOL File444912-48-5.mol

(R,S)-AM1241物理性質

沸点	630.7±55.0 °C(Predicted)
比重(密度)	1.60±0.1 g/cm3(Predicted)
貯蔵温度	Store at -20°C
溶解性	DMSO: 60°Cで~18mg/mL
酸解離定数(Pka)	9.73±0.10(Predicted)
外見	個体
色	黄色

安全性情報

主な危険性	Xn
Rフレーズ	36/37/38-42/43
Sフレーズ	22-26-36/37-45
WGK Germany	3

危険有害性情報のコード(GHS)

(R,S)-AM1241 価格

製品番号	包装	価格	製品説明	購入
Sigma-Aldrich Japan A6478	5mg	￥57500	≥98% (HPLC), solid	購入
Sigma-Aldrich Japan A6478	25mg	￥195900	≥98% (HPLC), solid	購入

(R,S)-AM1241 化学特性,用途語,生産方法

説明
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).
使用
(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.

(R,S)-AM1241 生産企業

444912-48-5, (R,S)-AM1241 キーワード

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