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DOI hydrochloride

 
Catalog No.
B5321
脑通透性、混合型5-HT2A/5-HT2C受体激动剂
组合的产品项目
规格价格库存 数量
10mg
¥ 2,545.00
Ship with 10-15 days
50mg
¥ 11,158.00
Ship with 10-15 days

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A

背景

DOI hydrochloride is a brain-permeable agonist of 5-HT2A and 5-HT2C receptors, with Ki values being 0.7, 2.4 and 20 nM for 5-HT2A, 5-HT2C and 5-HT2B receptors, respectively. The 5-HT2 receptor consists of three distinct subpopulations, i.e. 5-HT2A, 5-HT2B, and 5-HT2C receptors, among which the 5-HT2A receptor contributes to the major part of the behavioral effects evoked by hallucinogens. DOI, as a phenylisopropylamine hallucinogen, can thus be used to explore 5-HT2 receptor mediated biological events due to its high affinity for the 5-HT2 receptor. In addition, DOI has also been used as an analytical reference standard categorized as a phenethylamine and amphetamine.

References:

1. Nelson DL, Lucaites VL, Wainscott DB, et al. Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors. Naunyn-Schmiedeberg's Archives of Pharmacology, 1999, 359(1): 1-6.

2. Kerrigan S, Banuelos S, Perrella L, et al. Simultaneous detection of ten psychedelic phenethylamines in urine by gas chromatography-mass spectrometry. Journal of Analytical Toxicology, 2011, 35(7): 459-469.

3. Yu B, Becnel J, Zerfaoui M, et al. Serotonin 5-hydroxytryptamine2A receptor activation suppresses tumor necrosis factor-α-induced inflammation with extraordinary potency. Journal of Pharmacology and Experimental Therapeutics, 327(2): 316-323.

4. Monti JM, Jantos H. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. European Journal of Pharmacology, 2006, 553(1-3): 163-170.

化学属性

Physical AppearanceA crystalline solid
StorageStore at RT
M.Wt357.62
Cas No.42203-78-1
FormulaC11H16INO2·HCl
SolubilitySoluble in H2O
Chemical Name(S)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine hydrochloride
SDFDownload SDF
Canonical SMILESIC1=C(C=C(C(OC)=C1)C[C@H](C)N)OC.Cl
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试验操作

Cell experiment:[3]

Cell lines

Rat aortic smooth muscle (RASM) cells

Reaction Conditions

1 nM DOI

Applications

DOI rapidly blocked TNF-α-induced ICAM1 expression in RASM cells. Moreover, the effect of DOI at blocking proinflammatory gene expression remained many hours after addition of TNF-α.

Animal experiment:[4]

Animal models

Male Wistar rats, 350–400 g

Dosage form

0.35 ~ 0.7 mmol/kg

Subcutaneous administration

Applications

DOI significantly increased waking and light sleep, and reduced slow wave sleep, rapid-eye-movement (REM) sleep, and the number of REM periods in rats.

Note

The technical data provided above is for reference only.

References:

1. Nelson DL, Lucaites VL, Wainscott DB, et al. Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors. Naunyn-Schmiedeberg's Archives of Pharmacology, 1999, 359(1): 1-6.

2. Kerrigan S, Banuelos S, Perrella L, et al. Simultaneous detection of ten psychedelic phenethylamines in urine by gas chromatography-mass spectrometry. Journal of Analytical Toxicology, 2011, 35(7): 459-469.

3. Yu B, Becnel J, Zerfaoui M, et al. Serotonin 5-hydroxytryptamine2A receptor activation suppresses tumor necrosis factor-α-induced inflammation with extraordinary potency. Journal of Pharmacology and Experimental Therapeutics, 327(2): 316-323.

4. Monti JM, Jantos H. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. European Journal of Pharmacology, 2006, 553(1-3): 163-170.

质量控制

质量控制和MSDS

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化学结构

DOI hydrochloride