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J Pharm Biomed Anal
February 2019
National Centre on Drug Addiction and Doping, Istituto Superiore di Sanità, Rome, Italy.
J Pharm Biomed Anal
February 2017
Semmelweis University, Department of Pharmaceutical Chemistry, Research Group of Drugs of Abuse and Doping Agents, Hungarian Academy of Sciences, Hőgyes E. u. 9., H-1092 Budapest, Hungary.
Species-specific acid-base and partition equilibrium constants were experimentally determined for the therapeutically important semisynthetic opioid receptor agonist hydromorphone, dihydromorphine, and mixed agonist-antagonist nalorphine and nalbuphine. The acid-base microequilibria were characterized by combining pH-potentiometry and deductive methods using synthesized auxiliary compounds. Independent of the pH, there are approximately 4.
View Article and Find Full Text PDFJ Chem Inf Model
March 2015
‡College of Chemistry, Beijing Normal University, Beijing, 100875, People's Republic of China.
Human kappa opioid receptor (κ-OR), a G protein-coupled receptor (GPCR), has been identified as a drug target for treatment of such human disorders as pain perception, neuroendocrine physiology, affective behavior, and cognition. In order to find more selective and active agonists, one would like to do structure based drug design. Indeed, there is an X-ray structure for an antagonist bound to κ-OR, but structures for activated GPCRs are quite different from those for the inactive GPCRs.
View Article and Find Full Text PDFInt J Neuropsychopharmacol
December 2014
Peking University Sixth Hospital/Institute of Mental Health (Dr Li, Ms C.-Y. Sun, Dr Luo, Ms Meng, Mr Xu, Ms Deng, Drs Lu, and H.-Q. Sun), and National Institute on Drug Dependence, Peking University, Beijing, China (Drs Dr Li, Ms C.-Y. Sun, Dr Luo, Dr Xue, Ms Meng, Mr Xu, Ms Chen, Ms Deng, Drs Zhai, Shi, and Lu); Institute for Food and Drug Safety Evaluation, National Institutes for Food and Drug Control, Beijing, China (Dr Li); Key Laboratory of Mental Health, Ministry of Health (Peking University), Beijing, China (Drs Lu and H.-Q. Sun); Menninger Department of Psychiatry and Behavioral Sciences, Baylor College of Medicine, Houston, Texas (Dr Kosten)
Background: Currently approved medications for opioid addiction have shown clinical efficacy, but undesired side effects, dependence induced by the medications themselves, and low treatment compliance necessitate the need for novel therapies.
Methods: A novel morphine-keyhole limpet hemocyanin conjugate vaccine was synthesized with 6-glutarylmorphine as the hapten and a lengthened linker of 6 carbon atoms. The titer and specificity of the triggered antibody were assessed by enzyme-linked immunosorbent assay.
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