Background: The primary purpose of this investigation was to determine the relative potency of eltanolone, a new steroid hypnotic, and propofol and thiopental when used for induction of general anesthesia. In addition, the induction characteristics of propofol and eltanolone were compared.
Methods: One hundred seventy-five patients, premedicated with lorazepam 1 mg orally, randomly received one of six different doses of either eltanolone or propofol. The probability of successful induction (defined as not responsive to verbal commands within 2 min) was related to the logarithm of the dose for each drug by means of logistic regression analysis. Estimates of ED50 and ED95 for each drug were obtained. The incidence of side effects was compared for eltanolone and propofol. The potency of thiopental was determined in a parallel study, using an identical methodology in 105 patients receiving one of seven different doses of the barbiturate.
Results: The relative potency of eltanolone was 3.2 times (95% confidence interval 2.7-3.8) greater than propofol and 6.0 times (5.3-6.9) greater than thiopental. ED50 and ED95 values for eltanolone were 0.46 (0.40-0.52) and 0.82 (0.68-1.28) mg.kg-1, respectively. Compared to propofol, induction of anesthesia with eltanolone is characterized by a lower incidence of injection pain (3.5% vs. 58%) and apnea (1.2% vs. 11.2%).
Conclusions: Eltanolone appeared to be an effective induction agent that is 3.2 times more potent than propofol and 6 times more potent than thiopental. Its use was associated with less pain on injection than was propofol.
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http://dx.doi.org/10.1097/00000542-199401000-00009 | DOI Listing |
RSC Adv
January 2025
ICMR-Regional Medical Research Centre, Department of Health Research, Ministry of Health & Family Welfare, Govt. of India Bhubaneswar 751023 Odisha India.
Palladium-catalyzed reactions between imidazo[1,2-]pyridine derivatives and 4-bromo-2,2-dialkyl-substituted 2-chromenes under microwave irradiation at 100 W, 120 °C for 20-30 min provided a series of new 3-(2,2-dialkyl-2-chromen-4-yl)-2-phenylimidazo[1,2-]pyridine derivatives in good to excellent yields. The structures of the synthesized compounds were confirmed through spectroscopic techniques (NMR and HRMS). The X-ray single-crystal structure of compound 16e was also determined.
View Article and Find Full Text PDFJ Chem Inf Model
January 2025
Department of Modeling and Informatics, Merck & Co., Inc., Rahway, New Jersey 07065, United States.
Potency optimization of macrocyclic peptides can include both modifying intermolecular interactions and modifying the conformational stability of the bioactive conformation. However, the number of possible modifications is vast. To identify modifications that enhance the stability of the binding conformations in a cost-effective manner, there is a need for a high-throughput in-silico method that scores the conformational stability of these modified molecules.
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2025
Department of Chemistry and Biochemistry, Baylor University, 101 Bagby Ave., Waco, TX 76798, United States. Electronic address:
To gain further insights into the importance of the unsaturated 1,4-ketoaldehyde moiety of ophiobolin A (OpA) for the potency and selectivity observed toward cancer stem cells, several derivatives were synthesized through controlled reduction and oxidations of the unsaturated aldehyde and ketone moieties. Structure elucidation of these new OpA derivatives was achieved through detailed NMR studies and comparison to OpA and known isolated congeners possessing variations in these regions. The relative stereochemistry of the newly generated stereocenters was determined by coupling constants in conjunction with conformational analyses (DFT) of the synthetic derivatives.
View Article and Find Full Text PDFJ Sci Food Agric
January 2025
Bee and Natural Products R&D and P&D Application and Research Center, Bingöl University, Bingöl, Turkey.
Background: Phlomis capitata is an endemic species of flowering aromatic and medicinal plant in the family Lamiaceae, native to regions of the Mediterranean and nearby areas. Understanding the chemical compounds present in P. capitata can reveal potential medicinal properties.
View Article and Find Full Text PDFJ Anal Toxicol
January 2025
Center for Forensic Science Research and Education, Fredric Rieders Family Foundation, Horsham, PA.
Identification of N,N-dimethylpentylone (DMP) in counterfeit "Ecstasy" and "Molly" tablets poses risk to public health due to its adverse effects. Little information is available regarding the pharmacological activity or relevant blood or tissue concentrations of DMP, and even less is known about other structurally related beta-keto methylenedioxyamphetamine analogues on recreational drug markets, such as N-propyl butylone. Here, a novel toxicological assay utilizing liquid chromatography-tandem quadrupole mass spectrometry (LC-QQQ-MS) was developed and validated for the quantitation of DMP and five related synthetic cathinones (eutylone, pentylone, N-ethyl pentylone (NEP), N-propyl butylone, and N-cyclohexyl butylone), with chromatographic resolution from isomeric variants and quantitation performed by standard addition.
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