Structure (London, England : 1993), 19(11), 1683-1690 (2011-11-15)
Opioids that stimulate the μ-opioid receptor (MOR1) are the most frequently prescribed and effective analgesics. Here we present a structural model of MOR1. Molecular dynamics simulations show a ligand-dependent increase in the conformational flexibility of the third intracellular loop that
Kappa(kappa) opioid agonists slow gastrointestinal transit in the guinea pig and the mouse but not the rat. Opioid antagonists naloxone and naltrexone are mu (mu) preferring, while the antagonist nalmefene has more kappa binding activity. When administered orally, the specific
Journal of chromatography. A, 1262, 214-218 (2012-09-25)
In the present work, pulsed electromembrane extraction (PEME) is introduced for the first time as an efficient and inexpensive method for the extraction of ionizable compounds from different matrices. The setup proposed for electromembrane extraction (EME) provides a very stable
Methods and findings in experimental and clinical pharmacology, 7(4), 175-177 (1985-04-01)
Nalmefene (6-methylene-naltrexone) is a potent, orally active, opiate antagonist. IC50's were obtained for nalmefene, naloxone and naltrexone using radiolabelled prototype ligands for mu, kappa and delta receptors in homogenates of rat brain minus cerebellum. Nalmefene antagonized the bindings of [3H]-dihydromorphine
Expert opinion on investigational drugs, 19(11), 1451-1459 (2010-09-28)
Alcohol use and dependence are frequent disorders. Despite numerous established psychosocial approaches, relapse to heavy drinking is common in alcohol-dependent patients after detoxification and relapse prevention remains a significant medical challenge. The opioidergic system plays a crucial role in mediating
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