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Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
The chemoenzymatic synthesis of Rasagiline has been described before by means of practical lipase-catalysed KR of racemic 1-indanol (Sousa et al., 2015; Fonseca et al., 2015). Alternatively, the DKR of racemic 1-indanamine has been described in a 73.2 g scale (200 g/L) using CAL-B, isopropyl methoxyacetate and a palladium nanocatalyst as racemisation agent (Scheme 9.39, top), isolating with 80% yield the (R)-amide in enantiopure form (Ma et al., 2014). Interestingly, the possibility of recycling the enzymatic and metal catalysts was demonstrated with little loss of the efficiency after 4 cycles. Similarly, the DKR of the commercially available 1,2,3,4-tetrahydro-1-naphthylamine has allowed the synthesis of the selective serotonin reuptake inhibitor Norsertraline, which is the chief metabolite of Sertraline marketed as Zoloft® by Pfizer, and supplied as antidepressant (Scheme 9.38, bottom). The combination of CAL-B, isopropyl acetate and a ruthenium dimeric catalyst for amine racemisation led to the (R)-amide in 70% yield and 99% ee after 72 h at 90°C (Thalén et al., 2009). DKR of racemic 1-indanamine and 1,2,3,4-tetrahydro-1-naphthylamine using CAL-B.
Pulmonary hypertension induced by drugs and toxins
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Kim Bouillon, Yola Moride, Lucien Abenhaim, Marc Humbert
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI), as are aminorex and fenfluramines (see Fig. 29.2). However, we are not aware of any report of a relationship between the chronic intake of SSRI antidepressants and PAH in adults. It is estimated that 2–3 per cent of pregnant women receive anti-depressive medication of which the SSRI class of drugs is the most commonly utilized.114 In 1996, Chambers et al. observed in a prospective small cohort an increased risk for perinatal complications among women who took fluoxetine in the third trimester.115 They suggested a possible association between maternal use of fluoxetine late in the third trimester of pregnancy and the risk of PPHN in the infant. Recent data from a retrospective case–control study conducted between 1998 and 2003 by Chambers et al. support the association between the maternal use of SSRIs after the completion of the 20th week of gestation and PPHN in the offspring: 14 infants with PPHN had been exposed to an SSRI compared with 6 in a control group (adjusted odds ratio of 6.1; 95% CI: 2.2–16.8).116 Another cohort study based on the Swedish Medical Birth Register was in favour for this association.117
Heart Rate Variability and Eating Disorders
Published in Herbert F. Jelinek, David J. Cornforth, Ahsan H. Khandoker, ECG Time Series Variability Analysis, 2017
Depression comorbidity was the focus of another study involving 30 patients with a mean BMI of 17.9 (AN as defined by DSM-5) and 44 healthy age-matched controls (Jelinek et al. in press). Thirteen patients were clinically diagnosed with depression and 11 of these met diagnostic criteria on the Beck Depression Inventory (BDI) for moderate-to-severe depressive disorder. HRV changes were accentuated in the depressed group particularly using nonlinear parameters and the possibility of increased cardiac risk was inferred. Medication, mainly antidepressant medication of the selective serotonin reuptake inhibitor (SSRI) type, was found to exert no significant effect on HRV.
A single exposure to sub-lethal concentrations of a glyphosate-based herbicide or fluoxetine-based agent on growth performance in Nile tilapia
Published in Journal of Toxicology and Environmental Health, Part A, 2023
Amanda Carolina Cole Varela, Suelen Mendonça Soares, Milena Fortuna, Vitória Cadore Costa, Ísis Piasson Barletto, Mateus Timbola Mozatto, Lisiane Siqueira, Heloísa Helena de Alcantara Barcellos, Rodrigo Egydio Barreto, Leonardo José Gil Barcellos
It is evident that serotonin plays a key role in fish with respect to feed anticipatory behavior and feed intake, a marker of growth performance (Silva et al. 2014). Faria et al. (2021) noted an association between GBH exposure and increase in serotoninergic activity in fish, which may consequently affect food intake and growth. Similarly, Mennigen et al (2010, 2011), reported that fluoxetine (FLU), a selective serotonin reuptake inhibitor modulated diverse physiological processes including reproduction, food intake, growth and stress in fish. Further, Lim, Soga, and Parhar (2023) showed that dysfunction of serotoninergic system in O. niloticus was associated with social stress. Thus, the second aim was to compare the effects of GBH with FLU on growth performance in O. niloticus.
Production of stable amorphous form by means of spray drying
Published in Particulate Science and Technology, 2019
Igor Nežić, Aleksandra Sander, Ernest Meštrović, Dražen Čavužić
5-(4-(4-(5-Cyano-1H-indol-3-yl)butyl)piperazin-1-yl)benzofuran-2-carboxamide is an API of a drug, antidepressant agent, developed by Forest Laboratories Inc. (licensed from Merck) under the brand name VIIBRYDTM as a dual-acting and selective serotonin-reuptake inhibitor and 5-HT1A receptor partial agonist for treatment of major depressive disorder (Figure 1). Active substance is present in the form of hydrochloride salt.
Combined effects of high temperature and pesticide mixture exposure on free-swimming behaviors and hepatic cytochrome P450 1A expression in goldfish, Carassius auratus
Published in Journal of Toxicology and Environmental Health, Part A, 2023
Brittney Lacy, Michelle Rivera, Leinady Flores, Md Saydur Rahman
Environmental contaminants, like pesticides, are of growing environmental concern, as these compounds are ubiquitous globally and across United States waterways (Casado et al. 2019; Hageman et al. 2019; Mac Loughlin, Peluso, and Marino 2022; Stehle et al. 2019; Stone 2013). Numerous environmental contaminants are currently detected in aquatic environments including conventional pesticides (usage in the United States illustrated in Figure 1a). These are associated with a variety of reported adverse effects in aquatic species such as diminished growth, mobility, and altered behavior in invertebrates (Morrissey et al. 2015); as well as reduced tadpole mass and zooplankton abundance (Lewis et al. 2021), impaired swimming performance and disrupted hormonal and signaling pathways in Chinook salmon (Fuller et al. 2022; Giroux, Gan, and Schlenk 2019). As environments change as in global climate change and species face marked declined populations, animal behavior is increasingly intertwined with conservation biology (Berger‐tal et al. 2016; Blumstein and Fernandez-Juricic 2010; Buchholz 2007; Fuller et al. 2022). Behavioral analysis elucidates how stress levels attributed to heat, toxicants, or trauma, can negatively alter social behaviors, including courtship behaviors, and cause disorientated erratic swimming (Firth 1986; Vogt et al. 2022). Chronic stress alters the central nervous system by producing structural changes, such as reduced brain weight, oxidant responses, inhibition of brain acetylcholine esterase (AChE) activity, a marker of neurotoxicity, as well as atrophy, affecting cognition, memory, neuronal functions, and behavior (Lupien et al. 2009; Moreira et al. 2021; Sager et al. 2022; Sarahian et al. 2014; Schetter and Dolbier 2011). Investigators demonstrated that stressors, such as pesticides, alter animal behaviors in ways that negatively impact organismal, population, and ecosystem health, by reducing survival rates and reproduction (Araujo et al. 2018; McDonald, Gonzalez, and Sloman 2011; Tudi et al. 2021). For example, selective serotonin reuptake inhibitor pollution interrupted the courtship behaviors of the Gulf toadfish (Opsanus beta), potentially impacting their reproductive abilities (McDonald, Gonzalez, and Sloman 2011). In goldfish (Carassius auratus), the pesticidal compound, diuron, triggered an insidious attraction response initiating fish to seek out the chemical and consequently enhancing exposure levels (Saglio and Trijasse 1998). In contrast, in the guppy (Poecilia reticulate), the pesticide atrazine triggers avoidance behaviors, suggesting pollutants might fragment aquatic habitats and isolate breeding populations, potentially decreasing the fitness of the species (Araujo et al. 2018; Sandoval-Herrera et al. 2019).