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1,3-二邻甲苯胍 /Ditolylguanidine {[allProObj[0].p_purity_real_show]}

货号:A656782 同义名: 二邻甲苯胍 / 1,3-Di-o-tolylguanidine;DTG Ambeed 开学季,买赠积分,赢豪礼

Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor)[1].

Ditolylguanidine 化学结构 CAS号:97-39-2
Ditolylguanidine 化学结构
CAS号:97-39-2
Ditolylguanidine 3D分子结构
CAS号:97-39-2
Ditolylguanidine 化学结构 CAS号:97-39-2
Ditolylguanidine 3D分子结构 CAS号:97-39-2
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Ditolylguanidine 纯度/质量文件 产品仅供科研

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Ditolylguanidine 生物活性

描述 Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor)[1]. The effects of σ receptor agonists on the Müller cell swelling were abrogated in the presence of blockers of metabotropic glutamate and purinergic P2Y1 receptors, respectively, suggesting that σ receptor activation triggers activation of a glutamatergic-purinergic signaling cascade which is known to prevent the osmotic Müller cell swelling[2].Ditolylguanidine (DTG) is a ligand which binds with high affinity to neuronal sigma receptors. DTG and (+)-SKF10047 (N-allylnormetazocine) produced a concentration-dependent suppression of the depolarization of enteric neurons evoked by ionophoresis of ACh. The EC50 values for DTG and (+)-SKF10047 were 4.7 and 3.8 microM, respectively, and were similar to that for hexamethonium (3.2 microM). DTG and hexamethonium (each at 1 microM) were more effective blockers of ACh-induced inward currents at a holding potential of -100 mV than at -40 mV[3]. DTG totally blocked the female sex hormone-induced inhibition on ET-1 release, whereas testosterone-induced stimulation was not affected[4].

Ditolylguanidine 参考文献

[1]Glennon RA. Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach. Mini Rev Med Chem. 2005 Oct;5(10):927-40

[2]Vogler S, Winters H, Pannicke T, Wiedemann P, Reichenbach A, Bringmann A. Sigma-1 receptor activation inhibits osmotic swelling of rat retinal glial (Müller) cells by transactivation of glutamatergic and purinergic receptors. Neurosci Lett. 2016 Jan 1;610:13-8

[3]Galligan JJ, Campbell BG, Kavanaugh MP, Weber E, North RA. 1,3-Di(2-tolyl)guanidine blocks nicotinic response in guinea pig myenteric neurons. J Pharmacol Exp Ther. 1989 Oct;251(1):169-74

[4]Wilbert-Lampen U, Seliger C, Trapp A, Straube F, Plasse A. Female sex hormones decrease constitutive endothelin-1 release via endothelial sigma-1/cocaine receptors: an action independent of the steroid hormone receptors. Endothelium. 2005 Jul-Aug;12(4):185-91

Ditolylguanidine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.18mL

0.84mL

0.42mL

20.89mL

4.18mL

2.09mL

41.79mL

8.36mL

4.18mL

Ditolylguanidine 技术信息

CAS号97-39-2
分子式C15H17N3
分子量 239.316
别名 二邻甲苯胍 ;1,3-Di-o-tolylguanidine;DTG;NSC 473;NSC 132023
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 145 mg/mL(605.89 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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