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Tetrahydromagnolol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tetrahydromagnolol图片
CAS NO:20601-85-8
规格:98%
分子量:270.4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
peripheral CB2 receptor agonist
CAS:20601-85-8
分子式:C18H22O2
分子量:270.4
纯度:98%
存储:Store at -20°C

Background:

Tetrahydromagnolol is a major metabolite of magnolol and acts as a peripheral CB2 receptor agonist. Tetrahydromagnolol also acts as an antagonist at GPR55 [1].


Cannabinoid (CB) receptors belong to the G protein-coupled receptor (GPCR) superfamily and are divided into CB1 and CB2. CB1 activation mediates analgesia, stimulation of appetite, and euphoria, among other effects. CB2 receptor activation results in analgesic and antiinflammatory effects. GPR55, a CB-related orphan receptor, is reported to interact with certain CBs [1].


Tetrahydromagnolol is a highly selective peripheral CB2 receptor agonist that is 19-fold more potent than magnolol with EC50 and Ki values of 0.17 μM and 0.42 μM, respectively. Magnolol is a bioactive compound isolated from the bark of Magnolia officinalis that is used in Asian traditional medicine for the treatment of anxiety, sleeping disorders, and allergic diseases. Magnolol behaved as a partial agonist with selectivity for the CB2 subtype (EC50 = 3.28 μM; Ki = 1.44 μM). In β-arrestin translocation assay, Tetrahydromagnolol inhibited LPI-induced GPR55 activation with KB value of 13.3 μM [1].


Reference:
[1].  Rempel V, Fuchs A, Hinz S, et al. Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55. ACS Med Chem Lett. 2012 Nov 14;4(1):41-5.