• فهرست مقالات Codeine

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        1 - Trials of phenanthrene opioids functionalization with hindered polycyclic carboxylic acids
        Alessandro Venditti Ambra Pallotti Armandodoriano Bianco
        In the last decades, the number of patients undergoing pain relief for chronic or degenerative diseases has observed a significant increase, also due to an increase in the average age of the population. Morphine, the widely used opioid in pain therapy, is known to produ چکیده کامل
        In the last decades, the number of patients undergoing pain relief for chronic or degenerative diseases has observed a significant increase, also due to an increase in the average age of the population. Morphine, the widely used opioid in pain therapy, is known to produce over time tolerance with the appearance of hyperalgesia and allodynia, conditions which may affect patient compliance. These phenomena have been re-conducted to one of its metabolite, the 3-O-glucuronide (accounting in humans for 80% of the dose administered), which was found to be an effective neuro-excitatory and a potent activator of microglia, so resulting to be responsible of the development of both hyperalgesia and allodynia. Therefore, the inhibition of glucuronidation represents an interesting pharmacological target to achieve greater therapeutic efficacy by morphine and the synthesis of new active compounds useful in the pain control therapy is still in the limelight. In this context, we observed that codeine and some codeine derivatives (in particular the acetyl and pivaloyl esters) are able to inhibit the formation of morphine-3-O-glucuronide so, in continuation of the previous work, we projected new codeine derivatives as potential useful compounds in the modulation of morphine glucuronidation. In this paper, we report the optimization of the synthetic procedure to obtain codeine esters with hindered polycyclic carboxylic acids by using a suitable alcohol (allyl alcohol) with the same configuration of 6-OH function of the codeine skeleton. Together with the allyl ester derivatives of these acids also the 1-adamantaneacetic acid ester derivative of codeine (4), a new codeine derivative, was finally synthesized following the reported synthetic approach. پرونده مقاله
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        2 - Determination of alkaloids amount from Iranian Papaver bracteatum Lindl. by HPLC
        زهره کدخدا سجاد صداقت شمس علی رضازاده حسن علی نقدی بادی رحیم تقی زاد فرید ‏فرهاد ‏حریری اکبری
        Background & Aim: Papaver bracteatum Lindl. (Papaverace) is an important pharmaceutical plant which contains isoqinoline alkaloids. Isoqinoline alkaloids constitute one distinct group of secondary metabolites of the Papaverace family. Codeine and thebaine are import چکیده کامل
        Background & Aim: Papaver bracteatum Lindl. (Papaverace) is an important pharmaceutical plant which contains isoqinoline alkaloids. Isoqinoline alkaloids constitute one distinct group of secondary metabolites of the Papaverace family. Codeine and thebaine are important alkaloids of Papaver bracteatum which use widely due to its medicinal properties. Therefore it is necessary to determination the contents of these alkaloids in different parts of Iran. In order to determine the best natural habitat of Papaver bracteatum, containing the highest concentration of thebaine and codein different sample collected from different parts of Iran.Experimental: Using high performance liquid chromatography (HPLC) standard curve with the presence of two major alkaloids (thebaine and codeine) were drawn and alkaloids were extracted from capsule Papaver bracteatum and were determined by HPLC.Results & Discussion: Codeine contents in the sample of dry capsule Zanjan, Plour, Chalus road, Siah Bisheh, and Mazandaran were determined 0.04, 0.04, 0.03, 0.01 and 0.02% respectively. Thebaine content was determined 3.3, 0.61, 0.34, 0.31 and 0.06% respectively. Amounts of codeine for different regions ranged between 0.001 to 0.004% and, 0.06 to 3.3% for thebaine. The accessions collected from Zanjan has highest percentage of codeine and thebaine (3.34%)Industrial/Practical recommendation: The capsules collected from region of Zanjan in Iran have more contents of thebaine and codeine which possess many pharmaceutical applications, therefore it is highly recommended using accessions from the region of Zanjan to extract thebaine and codeine consumed in the pharmaceutical industry. پرونده مقاله