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A liquid chromatography-mass spectrometry (LC-MS) method has been developed for simultaneous quantification of buprenorphine and its three metabolites, namely norbuprenorphine, buprenorphine glucuronide, and norbuprenorphine glucuronide. Chromatographic separation was achieved on a C18 column with a gradient of acetonitrile over ammonium acetate buffer (25 mM, pH 6.6). The method run time was 7.5 min. Quantification was performed by selected ion monitoring of [M+H]+ ions of norbuprenorphine glucuronide (590), norbuprenorphine (414), buprenorphine glucuronide (644), and buprenorphine (468). Naloxone (328) (328 ng/mL) was used as an internal standard. The samples were processed by protein precipitation and extraction recovery was >95% with minimal observed matrix effects (<11%). Linear calibration curves were obtained over a range of 25 or 100 ng/mL to 4000 ng/mL, depending on the analyte. The lower limit of quantitation for buprenorphine and norbuprenorphine was 25 ng/mL and for buprenorphine glucuronide and norbuprenorphine glucuronide it was 100 ng/mL. The intraday and interday precision and accuracy determinations were <15% coefficient of variation and <15% bias, respectively. The method was successfully applied to in vitro enzymatic metabolism studies of buprenorphine. [ABSTRACT FROM AUTHOR]

The article reports on a study which examined the signaling pathway responsible for side effects of opioids. Laura Bohn of the Scripps Research Institute Florida discussed the study at the American Chemical Society (ACS) national meeting in Washington, D.C., in August 2017. Her team of researchers examined biased agonists for the better-known µ-opioid receptor.

The article discusses scientists at the California and Florida branches of Scripps Research Institute and the University of Southern California, report a synthesis of norsalvinorin A. It mentions the compound differs from salvinorin A by a single methyl group and binds to the kappa opioid receptor with an affinity similar to that of the natural product. It presents views of synthetic chemist Mark Rizzacasa on molecules' propensity to epimerize.

The article offers information on the acquisition of selective kappa opioid receptor antagonist CERC-501 from Baltimore-based Cerecor by Janssen Pharmaceuticals, and it mention about the announcement of Cerecor regarding failure of CERC-501 in trials as a treatment for nicotine withdrawal.

The article discusses the negative impact of opioids on the patients undergoing multiple treatments for a long period of time, which includes constipation and respiratory depression, provides information on opioid receptors affecting the neurons, NFEPP, fentanyl's fluorinated version.

The article informs that researchers have determined the X-ray crystal structures of opioid receptors which are the member of G-protein-coupled receptors (GPCRs) that mediates pain and pleasure in the body.

The article discusses research on crystal structures of four types of opioid receptors that would help elucidate how drugs bind these receptors and could lead to optimization of the growing list of opioid therapeutics.

The article focuses on two studies published in a March 2012 issue of "Nature" which examined the X-ray crystal structures of the µ- and κ-opioid receptors, members of the G protein-coupled receptor family. One of the studies, led by Raymond C. Stevens of Scripps Research Institute, found that the κ receptor features a large binding pocket. Both studies found that the µ and κ receptors are dimerized.

The article reports that AstraZeneca PLC will license the two opioid-induced constipation drugs of Nektar Therapeutics which are the NKTR-118 and NKTR-119. It states that Nektar's deal is worth 125 million dollars along with possible milestone payments. Meanwhile, it also mentions the deal between Eli Lilly & Co. Ltd and Adolor Corp. for the opioid-receptor OpRA III, wherein the gastrointestinal issues treatment is worth 2 million dollars along with 70 million dollars for milestone payments.

The article focuses on the discovery of receptor's endogenous ligand called N,N-dimethyltryptamine (DMT) by Arnold E. Ruoho and colleagues of the University of Wisconsin in Madison. It notes that sigma-1 receptor which is a hallucinogenic compound found in psychoactive snuffs and sacramental teas was known to bind many synthetic compounds. It mentions that Ruoho's team discovered that DMT suppresses voltage-gated sodium ion channel activity after binding to sigma-1 receptors on cells.

The article reports on the approval by the U.S. Food and Drug Administration (FDA) of methylnaltrexone bromide subcutaneous injection for the treatment of opioid-induced constipation in patients receiving palliative care. According to Joyce Korvick of the FDA, the new drug will be helpdul to patients who experience severe constipation linked with the use or morphine or other opioids. The drug displaces opioids from the mu-opioid receptors outside of the central nervous system to reduce constipation.

The article reports on the presentation of the 2006 Nauta Award in Pharmacochemistry by the European Federation for Medicinal Chemistry, to Philip S. Portoghese of the department of medicinal chemistry at the University of Minnesota and editor-in-chief of the "Journal of Medicinal Chemistry." He proposed the existence of multiple opioid receptors from the analysis of the structure-activity relationship of analgesics.