The authors studied the pharmacodynamics of four nondepolarising relaxants, d-tubocurarine (dTC), pancuronium, metocurine, and gallamine, at 25 degrees C, 31 degrees C, and 37 degrees C. The rat phrenic nerve-hemidiaphragm preparation with vascular perfusion was used for these investigations. For each drug at each temperature, a dose-response curve for twitch depression was constructed. ED50 values were calculated using probit-log dose regression. dTC, metocurine, and gallamine each demonstrated a near twofold increase in ED50 at 25 degrees C compared with 37 degrees C. No such relationship was apparent with pancuronium. In addition, the slopes of the dose-response curves were analyzed for effects due to temperature or drug. Slopes were not influenced by temperature; however, the slopes for metocurine and dTC were lower than those for pancuronium and gallamine. The authors conclude that in the rat, pancuronium retains potency at hypothermia, whereas the other relaxants decrease potency. In addition, metocurine and dTC exhibit less steep dose-response curves under these experimental conditions.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1097/00000542-198304000-00010 | DOI Listing |
Antiviral Res
January 2025
Institute of Human Virology, Zhongshan School of Medicine, and Key Laboratory of Tropical Disease Control of Ministry of Education, Sun Yat-sen University, Guangzhou 510080, China. Electronic address:
The Omicron BA.2.86 subvariants, JN.
View Article and Find Full Text PDFViruses
January 2025
Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA.
Second-generation integrase strand transfer inhibitors (INSTIs) are strongly recommended for people living with HIV-1 (PLWH). The emergence of resistance to second-generation INSTIs has been infrequent and has not yet been a major issue in high-income countries. However, the delayed rollouts of these INSTIs in low- to middle-income countries during the COVID-19 pandemic combined with increased transmission of drug-resistant mutants worldwide are leading to an increase in INSTI resistance.
View Article and Find Full Text PDFJ Med Chem
January 2025
School of Pharmaceutical Sciences, University of Geneva, 1206 Geneva, Switzerland.
Inhibition of the adenosine 2A receptor (AR) is recognized as a promising immunotherapeutic strategy but is challenged by the ubiquity of AR function in the immune system. To develop a safe yet efficacious immunotherapy, the discovery of a novel negative allosteric modulator (NAM) was preferred. Leveraging an in-house, sensitive, high-throughput screening cellular assay, novel AR NAM scaffolds were identified, followed by an extensive structure-activity relationship (SAR) study, leading to the discovery of potent 2-amino-3,5-dicyanopyridine derivatives.
View Article and Find Full Text PDFPoult Sci
January 2025
Food Technology and Innovation Research Center of Excellence, School of Agricultural Technology and Food Industry, Walailak University, Nakhon Si Thammarat 80160, Thailand.
This study evaluated the antioxidant potential of Mon-Pu (Glochidion wallichianum Mull. Arg.) leaf extract (MPLE) as a natural antioxidant in Ligor chicken meat gels.
View Article and Find Full Text PDFBiotechnol Prog
January 2025
Department of Biotechnology, School of Bioengineering, SRM Institute of Science and Technology, Kattankulathur, Tamil Nadu, India.
Type 2 diabetes mellitus (T2DM) and obesity are critical global health issues with rising incidence rates. Glucagon-like peptide-1 (GLP-1) analogues have emerged as effective treatments due to their ability to regulate blood glucose levels and gastric emptying through central nervous signals involving hypothalamic receptors, such as leptin. To address the short plasma half-life of native GLP-1, a C-16 fatty acid was conjugated to lysine in the GLP-1 analogue sequence to enhance its longevity.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!