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Tricyclic Antidepressant Structure-Related Alterations in Calcium-Dependent Inhibition and Open-Channel Block of NMDA Receptors.
Front Pharmacol
February 2022
Sechenov Institute of Evolutionary Physiology and Biochemistry of the Russian Academy of Sciences, Saint-Petersburg, Russia.
-methyl-D-aspartate receptors (NMDARs) are an essential target for the analgetic action of tricyclic antidepressants (TCAs). Their therapeutic blood concentrations achieve 0.5-1.
View Article and Find Full Text PDFAnalgesia in pediatric trauma patients in physician-staffed Austrian helicopter rescue: a 12-year registry analysis.
Scand J Trauma Resusc Emerg Med
November 2021
Department of Anaesthesiology and Critical Care Medicine, Medical University of Innsbruck, Anichstrasse 35, 6020, Innsbruck, Austria.
Background: As pediatric patients are typically rare among helicopter emergency medical systems (HEMS), children might be at risk for oligo-analgesia due to the rescuer's lack of experience and the fear of side effects.
Methods: In this retrospective analysis, data was obtained from the ÖAMTC HEMS digital database including 14 physician staffed helicopter bases in Austria over a 12-year timeframe. Primary missions involving pediatric trauma patients (< 15 years) not mechanically ventilated on-site were included.
DARK Classics in Chemical Neuroscience: Etonitazene and Related Benzimidazoles.
ACS Chem Neurosci
April 2021
European Monitoring Centre for Drugs and Drug Addiction, 1249-289 Lisbon, Portugal.
Etonitazene and related 2-benzylbenzimidazoles are potent analgetics invented in the research laboratories of the Swiss pharmaceutical giant CIBA in the late 1950s. Though the unprecedented structure distinguishes this class of compounds from poppy-derived and other synthetic analgetics, a range of studies indicate that these drugs are selective μ opioid receptor agonists possessing morphine-like pharmacotoxicological properties in animals as well as humans. Several unscheduled members of this synthetically readily accessible class of opioids that are not controlled under the international and national drug control systems have recently emerged on the illicit drug market.
View Article and Find Full Text PDFNicotinic Acetylcholine Receptor Accessory Subunits Determine the Activity Profile of Epibatidine Derivatives.
Mol Pharmacol
October 2020
Department of Pharmacology and Therapeutics, College of Medicine (L.W.C., C.S., R.L.P.) and Department of Pharmacodynamics, College of Pharmacy, (J.L.W., L.R.M.), University of Florida, Gainesville, Florida; and Center for Drug Discovery, Research Triangle Institute, Durham, North Carolina (F.I.C.)
Epibatidine is a potent analgetic agent with very high affinity for brain nicotinic acetylcholine receptors (nAChR). We determined the activity profiles of three epibatidine derivatives, RTI-36, RTI-76, and RTI-102, which have affinity for brain nAChR equivalent to that of epibatidine but reduced analgetic activity. RNAs coding for nAChR monomeric subunits and/or concatamers were injected into oocytes to obtain receptors of defined subunit composition and stoichiometry.
View Article and Find Full Text PDFInsights into the Chemical Discovery of Remifentanil.
Anesthesiology
May 2020
From Discovery and Translational Medicine, Intarcia Therapeutics, Inc., Research Triangle Park, North Carolina.
Design, Synthesis, and Pharmacological Evaluation of Ultrashort- to Long-acting Opioid Analgetics. By Feldman PL, James MK, Brackeen MF, Bilotta JM, Schuster SV, Lahey AP, Lutz MW, Johnson MR, Leighton HJ. J Med Chem 1991; 34:2202-8.
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