Since the synthesis of Fentanyl in 1961, many narcotics have appeared which are not yet available in France. Among agonists, all are Fentanyl derivates but are different by either more powerful (sufentanyl, lofentanyl), and longer-acting effects (lofentanyl), or less powerful and shorter-acting effects (alfentanyl). All would have a greater security index and minimal cardiovascular side effects. Among agonists-antagonists, only pentazocine is available in France for analgesic therapy. The interest of other new molecules as butorphenol, nalbuphine and buprenorphine, which are available in other countries, still remains a matter of discussion.
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Curr Med Chem
September 2002
Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University at Lublin, 6 Staszica Str., Lublin, PL-20081, Poland.
Developments in the domain of non-peptide opioid receptor agonists, beginning from the first evidence of opiate binding to definite receptors, are briefly summarized. The recent achievements are in a more detailed way depicted and discussed. Novel agonists for each of three opioid receptor basic types (delta, kappa and micro) are presented with the special emphasis on one-type-selective ligands.
View Article and Find Full Text PDFLife Sci
October 1994
Institute of Biochemistry, Hungarian Academy of Sciences, Szeged.
Morphine is the most widely used compound among narcotic analgesics and remains the gold standard when the effects of other analgetic drugs are compared. Apart from its presence in the poppy plant Papaver somniferum, morphine has been shown to be present in milk, cerebrospinal fluid and also in nervous tissue extracts. Recent evidence suggests that biosynthetic pathways for morphine exist in animal and even human tissues such as liver, blood and brain.
View Article and Find Full Text PDFSince the synthesis of Fentanyl in 1961, many narcotics have appeared which are not yet available in France. Among agonists, all are Fentanyl derivates but are different by either more powerful (sufentanyl, lofentanyl), and longer-acting effects (lofentanyl), or less powerful and shorter-acting effects (alfentanyl). All would have a greater security index and minimal cardiovascular side effects.
View Article and Find Full Text PDFl-1, 4-Dimethyl-10-hydroxy-2, 3, 4, 5, 6, 7-hexahydro-1, 6-methano-1H-4-benzazonine hydrobomide (l-ST-2121) is a new narcotic-antagonist analgesic possessing remarkable analgesic activity, and this activity is equal to or more potent than that of pentazocine. A single administration of l-ST-2121 produced a moderate CNS depression in rats, such as sedation, systemic muscle relaxation and decrease in motor activity. Rats were intermittently mediated for 1 to 6 days at one hour intervals through an implanted intravenous cannula.
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