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Metabolite Synthesis

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T1 - Synthesis and resolution of a Tolperisone metabolite

AB - 1α,25(OH) 2-16-ene-20-cyclopropyl-vitamin D 3 (13) is several fold more potent than the natural hormone 1α,25- dihydroxyvitamin D 3 (1) as an anti-inflammatory agent. Here, we have further analyzed the antiinflammatory properties of 13, confirming it as the most potent analogue tested within this family. We then determined the structures of all the natural metabolites of 13, including the 24-oxo metabolite 14, and carried out its synthesis. A comparison of 13 with 14 showed a similar induction of the primary VDR target genes CYP24A1 and CAMP and comparable anti-inflammatory properties as revealed by a similar inhibition of TNF-α, IL-12/23p40, IL-6, and IFN-γ production. Interestingly, 14 displays a 3-fold lower calcemic activity in vivo compared to 13. Collectively, these findings indicate that the strong potency of 13 can be explained by the accumulation of its stable 24-oxo metabolite, which shows immunoregulatory and anti-inflammatory properties superimposable to those exerted by 13 itself.

Specialists in Stable Isotope & Metabolite Synthesis

AB - The synthesis and resolution of a Tolperisone metabolite ((3'-hydroxy- 4'-methylphenyl)-2-methyl-3-(piperidine-1-yl)-1-propane-1-one, M1) is described. Racemic M1 was subjected to resolution by the enantiomers of camphor-10-sulfonic acid. Absolute configuration was determined by X-ray diffraction analysis. Enantiomeric excesses were determined by 1H NMR spectroscopy. (C) 2000 Elsevier Science Ltd.

HepatoChem » Metabolite Synthesis » HepatoChem

Expertise in synthesizing Vitamin D metabolites: 25-Hydroxy, 1,25 & 24,25-Dihydroxy & v3-EPI Vitamin D.

Cannabidiol 1 is the major nonpsychotropic, neutral constituent in most cannabis preparations. It is devoid of the psychoactive properties typical of cannabis; however, it produces numerous, potentially therapeutic pharmacological effects, some of which may be due to its metabolites. We report now the first total synthesis of 7-hydroxycannabidiol 2, a primary metabolite of cannabidiol, in an eight-step procedure.

We prepare metabolites of drug and food ingredient using mammalian tissue homogenates or genetically modified microorganisms. We also provide standard samples to meet your needs in any phases of drug development.
Employment of phase II metabolism enzyme, UDP-glucuronosyltransferase for instance, in genetically modified microorganism or mammalian tissue homogenate can give milligrams to grams of metabolites. Glucuronate conjugate, which is hard to synthesize chemically, has been prepared successfully. If chemical synthesis is easier, we will do so.

Safety study of drug metabolites has been required and standard samples of metabolites are necessary for the study. We are ready to prepare metabolites formed by cytochrome P-450 and glucuronate conjugates including acylglucuronides using enzyme. We provide standard samples of metabolites to meet your needs in drug development phases such as structure determination, measurement of blood concentration, safety testing, and medicinal effect testing.

Metabolite Synthesis - Chicago Discovery Solutions

1α,25(OH) 2-16-ene-20-cyclopropyl-vitamin D 3 (13) is several fold more potent than the natural hormone 1α,25- dihydroxyvitamin D 3 (1) as an anti-inflammatory agent. Here, we have further analyzed the antiinflammatory properties of 13, confirming it as the most potent analogue tested within this family. We then determined the structures of all the natural metabolites of 13, including the 24-oxo metabolite 14, and carried out its synthesis. A comparison of 13 with 14 showed a similar induction of the primary VDR target genes CYP24A1 and CAMP and comparable anti-inflammatory properties as revealed by a similar inhibition of TNF-α, IL-12/23p40, IL-6, and IFN-γ production. Interestingly, 14 displays a 3-fold lower calcemic activity in vivo compared to 13. Collectively, these findings indicate that the strong potency of 13 can be explained by the accumulation of its stable 24-oxo metabolite, which shows immunoregulatory and anti-inflammatory properties superimposable to those exerted by 13 itself.

Stitt M, Lunn J and Usadel B (2010) Arabidopsis and primary photosynthetic metabolism ‐ more than the icing on the cake. The Plant Journal 61: 1067–1091.

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  • Inhibitors of Metabolite Synthesis: How Sulfa Drugs …

    Metabolite Synthesis Research

  • Metabolite Standards Synthesis Center | SRI International

    Metabolite Standards Synthesis Center | RTI

  • Synthesis of a Primary Metabolite of Cannabidiol - …

    Synthetic routes have been developed for synthesis of potential metabolites of 25C-NBOMe and 25I-NBOMe

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Synthesis of a primary metabolite of cannabidiol.

The synthesis and resolution of a Tolperisone metabolite ((3'-hydroxy- 4'-methylphenyl)-2-methyl-3-(piperidine-1-yl)-1-propane-1-one, M1) is described. Racemic M1 was subjected to resolution by the enantiomers of camphor-10-sulfonic acid. Absolute configuration was determined by X-ray diffraction analysis. Enantiomeric excesses were determined by 1H NMR spectroscopy. (C) 2000 Elsevier Science Ltd.

Synthesis of JHW-250 4-hydroxypentyl Metabolite

N2 - 1α,25(OH) 2-16-ene-20-cyclopropyl-vitamin D 3 (13) is several fold more potent than the natural hormone 1α,25- dihydroxyvitamin D 3 (1) as an anti-inflammatory agent. Here, we have further analyzed the antiinflammatory properties of 13, confirming it as the most potent analogue tested within this family. We then determined the structures of all the natural metabolites of 13, including the 24-oxo metabolite 14, and carried out its synthesis. A comparison of 13 with 14 showed a similar induction of the primary VDR target genes CYP24A1 and CAMP and comparable anti-inflammatory properties as revealed by a similar inhibition of TNF-α, IL-12/23p40, IL-6, and IFN-γ production. Interestingly, 14 displays a 3-fold lower calcemic activity in vivo compared to 13. Collectively, these findings indicate that the strong potency of 13 can be explained by the accumulation of its stable 24-oxo metabolite, which shows immunoregulatory and anti-inflammatory properties superimposable to those exerted by 13 itself.

Specialists in Stable Isotope & Metabolite Synthesis

T1 - Synthesis and anti-inflammatory properties of 1 α,25-dihydroxy-16- ene-20-cyclopropyl-24-oxo-vitamin d 3, a hypocalcemic, stable metabolite of 1α,25-dihydroxy-16-ene-20-cyclopropylvitamin D 3

Synthesis and identification of an important metabolite …

N2 - The synthesis and resolution of a Tolperisone metabolite ((3'-hydroxy- 4'-methylphenyl)-2-methyl-3-(piperidine-1-yl)-1-propane-1-one, M1) is described. Racemic M1 was subjected to resolution by the enantiomers of camphor-10-sulfonic acid. Absolute configuration was determined by X-ray diffraction analysis. Enantiomeric excesses were determined by 1H NMR spectroscopy. (C) 2000 Elsevier Science Ltd.

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