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Chemical synthesis of analogs of the glycopeptide contulakin-G, an analgetically active conopeptide from Conus geographus.
Carbohydr Res
January 2006
Department of Chemistry, Swedish University of Agricultural Sciences, SE-750 07 Uppsala, Sweden.
Cone snails are marine predators that use immobilizing venoms for catching prey. Chemical analysis of the venoms has revealed a variety of biologically active small and intermediate size peptides rich in post-translational modifications (modified amino acids, glycosylation). The glycopeptide contulakin-G (pGlu-Ser-Glu-Glu-Gly-Gly-Ser-Asn-Ala-[beta-D-Galp-(1-->3)-alpha-D-GalpNAc-(1-->]Thr-Lys-Lys-Pro-Tyr-Ile-Leu-OH) is a potent analgesic from Conus geographus venom.
View Article and Find Full Text PDFAnalgetically active substances derived from structures of anpirtoline and epibatidine.
Gen Physiol Biophys
June 1998
Research Institute for Pharmacy and Biochemistry, Prague, Czech Republic.
Opiates increase plasma catecholamines in humans.
Psychoneuroendocrinology
June 1993
Department of Psychiatry, University of Munich, Germany.
Evidence from animal studies suggests that centrally acting opiates and opioid peptides increase catecholamine (CA) plasma concentrations, reflecting a central activation of sympathetic outflow. We describe here similar opiate actions in humans. Increasing doses of the potent mu opioid receptor agonist fentanyl (FE), 0.
View Article and Find Full Text PDFUptake, 3-, and 6-glucuronidation of morphine in isolated cells from stomach, intestine, colon, and liver of the guinea pig.
Drug Metab Dispos
April 1993
Allgemeine Pharmakologie, Medizinische Hochschule Hannover.
Orally administered morphine undergoes a considerable first-pass glucuronidation in animals and humans. However, the respective contribution of the gastrointestinal tract and the liver to the formation of the analgetically highly potent morphine-6-glucuronide (M6G) and the inactive morphine-3-glucuronide (M3G) is still debated. In this study, morphine uptake and biotransformation to M3G and M6G were compared in isolated cells from stomach, intestine, colon, and liver of the guinea pig.
View Article and Find Full Text PDFSilent--asymptomatic--ischaemia is one of the forms of ischaemic heart disease. Present possibilities of non-invasive diagnostics are based primarily on long-term ECG monitoring. With regards to the hypothesis that the raised algesic threshold at high level of analgetically reacting beta endorphins seems to be the pathophysiologic basis of this particular syndrome, we tried to verify the presumption by administering a beta-endorphin antagonist-naloxon.
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