Cannabigerol

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Cannabigerol 

Cannabigerol 是一种主要的植物大麻素，在 CB1 和 CB2 受体上表现为弱部分激动剂。Cannabigerol 也是一种相对有效和高效的 TRPA1 激动剂(EC50=0.7 μM)，TRPV1 和 TRPV2 的弱激动剂 (分别为 1.3 和 1.72 μM)，以及有效的 TRPM8 (0.16 μM) 和 5-HT1A 受体拮抗剂。Cannabigerol是一种有效的 α2-肾上腺素受体激动剂 (0.2 nM)。Cannabigerol促进 CRC 细胞凋亡 (apoptosis)，刺激 活性氧 ROS 产生，上调 CHOP mRNA，减少细胞生长。

Cannabigerol

Cannabigerol Chemical Structure

CAS No. : 25654-31-3

规格 价格 是否有货
1 mg ￥1500 询问价格 & 货期
5 mg ￥3750 询问价格 & 货期

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生物活性

Cannabigerol, one of the major phytocannabinoids, behaves as a weak partial agonist at CB1 and CB2 receptors. Cannabigerol is also a relatively potent and highly effective TRPA1 agonist (EC50=0.7μM), a weak agonist at TRPV1 and TRPV2 (1.3 and 1.72 μM, respectively), and a potent TRPM8 (0.16 μM) and 5-HT1A receptor antagonist. Cannabigerol is a potent α2-adrenoceptor agonist (0.2 nM). Cannabigerol promotes apoptosis, stimulates reactive oxygen species (ROS) production, upregulates CHOP mRNA and reduces cell growth in CRC cells[1][2][3][4].

体外研究
(In Vitro)

Cannabigerol (CBG) antagonizes the 5-HT1A receptor agonist, R-(+)-8-hydroxy-2-(di-n-propylamino)tetralin (apparent KB=51.9 nM)[1].
In CHO cells stably expressing human receptors, Cannabigerol is a weak partial agonist of both CB1R- and CB2R-dependent inhibition of cAMP that displaying a low affinity for CB1R and comparatively higher affinity for CB2R (Ki= 1300 and 490 nM, respectively)[3]. Cannabigerol (1-30 μM; 3-48 hurs) reduces cell viability in human colorectal cancer (Caco-2) cells in a time- and serum protein concentration-dependent manner[3].
Cannabigerol (10 μM; 24 hours) induces apoptosis in colorectal cancer (Caco-2) cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Cannabigerol (1-10 mg/kg; intraperitoneally; every day for 5 days; athymic female mice bearing HCT 116 cells) reduces colon carcinogenesis in vivo[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

316.48

Formula

C21H32O2
CAS 号

25654-31-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Cascio MG, et al. Evidence that the plant cannabinoid cannabigerol is a highly potent alpha2-adrenoceptor agonist and moderately potent 5HT1A receptor antagonist. Br J Pharmacol. 2010;159(1):129-141.

    [2]. De Petrocellis L, et al. Effects of cannabinoids and cannabinoid-enriched Cannabis extracts on TRP channels and endocannabinoid metabolic enzymes. Br J Pharmacol. 2011;163(7):1479-1494.

    [3]. Borrelli F, et al. Colon carcinogenesis is inhibited by the TRPM8 antagonist cannabigerol, a Cannabis-derived non-psychotropic cannabinoid. Carcinogenesis. 2014;35(12):2787-2797.

    [4]. Zagzoog A, et al. In vitro and in vivo pharmacological activity of minor cannabinoids isolated from Cannabis sativa. Sci Rep. 2020;10(1):20405. Published 2020 Nov 23.

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