Arachidonoyl Serinol

A CB1 receptor agonist

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库存: 现货

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5mg

￥612.00

490.00

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10mg

￥1050.00

840.00

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50mg

￥3325.00

2660.00

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100mg

￥5487.00

4390.00

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货号: ajci20436
CAS: 183718-70-9
别名:
分子式: C23H39NO3
分子量: 377.6
纯度: >98%
溶解度: ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

Arachidonoyl Serinol is an amide bond-containing analogue of 2-arachidonoylglycerol, exhibited only weak CB1 receptor agonistic activity. 2-Arachidonoyl glycerol (2-AG), a product of increased inositol phospholipid metabolism, is the natural endocannabinoid ligand for the CB1 receptor [1][2][3].

Cannabinoid receptor (CB1) was first identified in rat brain in 1988. N-arachidonoylethanolamine (anandamide) binds to the cannabinoid receptor and exhibits various cannabimimetic activities. Anandamide inhibits calcium currents in N18 neuroblastoma cells, inhibits forskolin-stimulated adenylase cyclase activity, electrically evokes twitch response of the mouse vas deferens, and causes analgesia, hypothermia, hypoactivity, and catalepsy [3]. Anandamide acts as a weak agonist and 2-arachidonoylglycerol may be an endogenous cannabinoid receptor agonist in nervous tissues [1].

Replacement of the sn-2 oxygen in the glycerol moiety of 2-AG with a nitrogen atom produces Arachidonoyl Serinol. In NG108-15 cells, Arachidonoyl Serinol induced a weak elevation of [Ca2+]I [1][2].

参考文献:
[1].? Sugiura T, Kodaka T, Kondo S, et al. 2-Arachidonoylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ in neuroblastoma x glioma hybrid NG108-15 cells. Biochem Biophys Res Commun. 1996 Dec 4;229(1):58-64.
[2].? Sugiura T1, Kodaka T, Kondo S, et al. Is the cannabinoid CB1 receptor a 2-arachidonoylglycerol receptor? Structural requirements for triggering a Ca2+ transient in NG108-15 cells. J Biochem. 1997 Oct;122(4):890-5.
[3].? Khanolkar AD, Abadji V, Lin S, et al. Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand. J Med Chem. 1996 Oct 25;39(22):4515-9.