Metabolic acidosis
Shaun Phillips in Fatigue in Sport and Exercise, 2015
An important question to answer when discussing the biochemistry of lactic acid is ‘What does the body produce during exercise – lactic acid or lactate’? Reading lay articles, or even scientific papers on the subject, you will often see that the terms lactic acid and lactate are used interchangeably as though they mean the same thing. Importantly, they do not. Lactic acid is, as the name suggests, an acidic compound that has the potential to release a proton (hydrogen ion, H+) into a solution, thereby making that solution more acidic (Figure 3.1). Conversely, lactate does not release H+ ; therefore, it is termed an acid salt. As lactate does not have a H+ to donate, it does not directly make its environment more acidic (Figure 3.1).
Atazanavir
M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson in Kucers’ The Use of Antibiotics, 2017
Atazanavir (ATV) sulfate, (3S,8S,9S,12S)-3,12-bis(1,1-dimethyl-ethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,6,10,13-pentaazate-tradecanedioic acid dimethyl ester sulfate (1:1), previously known as BMS-232632, is an azapeptide inhibitor of HIV-1 protease. The trade name for atazanavir is Reyataz (access-data.fda.gov/drugsatfda_docs/label/2007/021567s012lbl. pdf). The molecular formula is C38H52N6O7 H2SO4; the molecular weight of the sulfuric acid salt is 802.9; the molecular weight of the free base is 704.9. The structure is shown in Figure 246.1. Atazanavir sulfate is a white-yellow crystalline powder and slightly soluble in water; the pH of a saturated solution in water is 1.9 (at 24 ± 3°C). Atazanavir belongs to the protease inhibitor class of antiretroviral agents.
Venous anatomy and pathophysiology
Helane S Fronek in The Fundamentals of Phlebology: Venous Disease for Clinicians, 2007
Sodium tetradecyl sulfate (sodium l-isobutyl-4-ethyloctyl sulfate) is a synthetic long-chain fatty acid salt that has seen extensive industrial use as a synthetic surfactant (soap). It is sold for medical use as a solution of up to 3% concentration with 2% benzoyl alcohol used as a stabilizer. It is effective as a venous sclerosing agent in concentrations from 0.1% to 3%. Like sodium morrhuate and ethanolamine oleate, it was "grandfathered" by the FDA for sale in the United States, but its approval was rescinded at the request of the manufacturer, not for reasons of product safety. In the United States, it is currently available only through compounding pharmacies. Unlike sodium morrhuate, sodium tetradecyl sulfate has proven to be a reliable, safe and effective sclerosant. The principal clinical problems with the drug are a tendency to cause hyperpigmentation in up to 30% of patients, a significant incidence of epidermal necrosis upon extravasation of higher concentrations, and occasional cases of anaphylaxis.
RETRACTED ARTICLE: Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Hyung Chul Ryu, Marc Windisch, Jee Woong Lim, Inhee Choi, Eun Kyu Lee, Hye Hyun Yoo, Tae Kon Kim
Thiophen urea derivatives were synthesised in three steps as follows: a reaction of 4-nitrophenyl chloroformate, urea synthesis by amine substitution, and final deprotection (Scheme 1). In each step all products were easily obtained as a pure solid by a simple work-up method (precipitation or filtration) without further purification. Two starting materials that have a thiophen ring with various substituents were utilised to achieve structural diversity. Several compounds including J2H-1701, HCV-2602, and HCV-2694 were prepared as an acid salt to enhance aqueous solubility using an additional method. For example, J2H-1701 was prepared as a HCl salt by treatment of HCl solution in 1,4-dioxane. Almost all the test compounds showed good chemical stability and crystallinity. J2H-1701, a representative compound as a HCl salt, has a long-term stability (purity >98% for 3 months) at room temperature, and so do the other compounds. This stability is supposed to come from its crystallinity that would be intrinsic property of thiophen urea structure, based on their high melting point and differential scanning calorimetry data (data not shown). When the drug-like properties of TU derivatives were assessed by Lipinski’s rule of five15, most of the compounds were shown to be applicable for orally available drugs; for example, J2H-1701, it has 3 hydrogen bond donors, 6 hydrogen bond acceptors, logP (experimental) of 4.21, and molecular weight of 515.62 and the number of violation is 1. Therefore, J2H-1701 is considered as an orally available drug.
Evaluation of a tiered in vitro testing strategy for assessing the ocular and dermal irritation/corrosion potential of pharmaceutical compounds for worker safety
Published in Cutaneous and Ocular Toxicology, 2018
Jessica C. Graham, Nathan Wilt, Gertrude-Emilia Costin, Caren Villano, Jackie Bader, Lindsay Krawiec, Elizabeth Sly, Janet Gould
Twenty-four solid PCs were evaluated as part of the post-qualification (confirmatory) phase of this study. First, the pH of each PC was determined. The pH values for four PCs were determined to be ≤2 (PCs A–D), therefore the Corrositex® assay was conducted, and all PCs were predicted to be corrosive (packing groups II or III) (Table 2). These four PCs were not subjected to any further testing, except for PC-D which was further tested in the BCOP to confirm the tiered testing strategy. Although the pH determined for PC-E was 13.0 (Table 2), this PC was not tested in Corrositex® but tested in the BCOP assay and SIT since the testing strategy was still being finalized. For the sake of the post-qualification test items, a pH of ≤2 was indicative of corrosivity and consistent with the Corrositex® results for these compounds. Not surprisingly the PCs which were positive in the Corrositex® assay were acidic salts consisting of hydrochloride salts (PC-A and PC-B), a trimethanesulfonic acid salt (1/1, PC-C) and a hydrobromide salt (1/1, PC-D).
Isovitexin alleviates acute gouty arthritis in rats by inhibiting inflammation via the TLR4/MyD88/NF-κB pathway
Published in Pharmaceutical Biology, 2021
Xiujiang Sun, Peng Li, Xiaoyi Qu, Wenguang Liu
When the level of serum uric acid in patients with GA increases, the supersaturated uric acid salt precipitates, forming crystals and deposits in the synovial tissue. Sodium urate is recognized by TLR4 and activates the TLR4 signal pathway, resulting in the transcription, synthesis, and release of a series of downstream pro-inflammatory factors, such as IL-1 β, which leads to acute inflammatory reaction in joints. This acute inflammatory attack is accompanied by a process of severe pain in which neutrophils enter the joint or the tissues around the joint, phagocytize the deposited MSU microcrystals, release inflammatory cytokines and mononuclear macrophage membranes dissolve, leading to joint swelling and skin reddening (Sabina et al. 2010). In this study, the swelling of the right ankle joint in the model group occurred gradually after the establishment of the model, and reached the peak at 72 h. The swelling index of the joint in the positive, isovitexin, TAK-242 and isovitexin + TAK-242 groups at each time point after the establishment of the model was significantly higher than that in the sham group, but was lower than in the model group, indicating that colchicine, and isovitexin can alleviate the swelling of joints.
Related Knowledge Centers
- Acid
- Atom
- Deprotonation
- Hydrolysis
- Hydroxide
- Salt
- Neutralization
- Hydrogen
- Acid–Base Reaction
- Ammonium Chloride