An efficient amine-/ruthenium-catalyzed three-step process for the synthesis of Nefopam analogues was achieved through combinations of cascade enamine amination/iso-aromatization/allylation and diene or enyne metathesis as key steps starting from functionalized Hagemann's esters. In this communication, we discovered the application of ruthenium-catalysis on olefins containing free amines without in situ formation of salts.
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http://dx.doi.org/10.1039/b910397j | DOI Listing |
Minerva Anestesiol
October 2023
Department of Anesthesia and Intensive Care, University Hospital Marburg, Marburg, Germany.
Pharm Nanotechnol
July 2023
Department of Pharmacology, Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Background: Bioavailability is the dissimilarity between the total amount of drug exposure to a person and the actual dose received by his body. The difference in bioavailability between formulations of a given drug can have clinical implications.
Methods: Poor aqueous solubility, inappropriate partition coefficient, high first-pass metabolism, narrow absorption window, and acidic pH of the stomach are the main reasons behind the low bioavailability of drugs.
Org Biomol Chem
July 2021
The affiliated Obstetrics and Gynecology Hospital with Nanjing Medical University, Nanjing Maternity and Child Health Care Hospital, Center of Genetic Medicine, Nanjing 210004, Jiangsu, P.R. China.
Phenylalanine hydroxylase (PAH) deficiency (PAHD) is an autosomal recessive disorder that causes severe injury to the nervous system, the treatment of which mainly depends on dietary therapy. The limited treatment options for PAHD are an incentive to develop new methods to identify more efficient therapeutic drugs, such as agonists which could improve PAH activity. In this study, we aimed to establish a rapid and convenient method for the screening and verification of PAH agonists.
View Article and Find Full Text PDFCrit Care Explor
July 2020
Department of Medicine, McMaster University, Hamilton, ON, Canada.
Unlabelled: This systematic review and meta-analysis addresses the efficacy and safety of nonopioid adjunctive analgesics for patients in the ICU.
Data Sources: We searched PubMed, Embase, the Cochrane Library, CINAHL Plus, and Web of Science.
Study Selection: Two independent reviewers screened citations.
Neurosci Lett
July 2020
Department of Anesthesiology and Pain Medicine, Chonnam National University Medical School, Gwangju, Republic of Korea; Chonnam National University Hwasun Hospital Biomedical Research Institute, Gwangju, Republic of Korea. Electronic address:
The present study investigated the effects of intrathecal nefopam on the pain behavior and on the extracellular levels of serotonin (5-HT), norepinephrine (NE), and glutamate in the spinal cord, in a rat model of pain induced by formalin. Nefopam was intrathecally administered 10 min prior to the formalin test to assess its antinociceptive effects. In another cohorts of animals, dihydroergocristine, yohimbine, or (RS)-α-Methylserine-O-phosphate (MSOP), a serotonergic, α-2 adrenergic receptor, or group III metabotropic glutamate receptor antagonist, respectively, were administered prior to the application of nefopam in the formalin test.
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