pharmacological control
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2022 ◽  
Author(s):  
Jessica Raper ◽  
Mark A.G. Eldridge ◽  
Scott Sternson ◽  
Jalene Y Shim ◽  
Grace P Fomani ◽  
...  

Chemogenetics is a technique for obtaining selective pharmacological control over a cell population by expressing an engineered receptor that is selectively activated by an exogenously administered ligand. A promising approach for neuronal modulation involves the use of Pharmacologically Selective Actuator Modules (PSAMs); these chemogenetic receptors are selectively activated by ultrapotent Pharmacologically Selective Effector Molecules (uPSEMs). To extend the use of PSAM/PSEMs to studies in nonhuman primates it is necessary to thoroughly characterize the efficacy and safety of these tools. We describe the time course and brain penetrance in rhesus monkeys of two compounds with promising binding specificity and efficacy profiles in in vitro studies, uPSEM792 and uPSEM817, after systemic administration. Rhesus macaques received subcutaneous (s.c.) or intravenous (i.v.) administration of uPSEM817(0.064 mg/kg) or uPSEM792 (0.87 mg/kg) and plasma and CSF samples were collected over the course of 48 hours. Both compounds exhibited good brain penetrance, relatively slow washout and negligible conversion to potential metabolites - varenicline or hydroxyvarenicline. In addition, we found that neither of these uPSEMs significantly altered heart rate or sleep. Our results indicate that both compounds are suitable candidates for neuroscience studies using PSAMs in nonhuman primates.


2022 ◽  
Vol 8 ◽  
Author(s):  
Angela Klain ◽  
Cristiana Indolfi ◽  
Giulio Dinardo ◽  
Marcella Contieri ◽  
Fabio Decimo ◽  
...  

Exercise-induced bronchoconstriction (EIB) is a transient airflow obstruction, typically 5–15 min after physical activity. The pathophysiology of EIB is related to the thermal and osmotic changes of the bronchial mucosa, which cause the release of mediators and the development of bronchoconstriction in the airways. EIB in children often causes an important limitation to physical activities and sports. However, by taking appropriate precautions and through adequate pharmacological control of the condition, routine exercise is extremely safe in children. This review aims to raise awareness of EIB by proposing an update, based on the latest studies, on pathological mechanisms, diagnosis, and therapeutic approaches in children.


2021 ◽  
Vol 61 ◽  
pp. 69-76
Author(s):  
Damiana Scuteri ◽  
Maria Tiziana Corasaniti ◽  
Paolo Tonin ◽  
Pierluigi Nicotera ◽  
Giacinto Bagetta

Biomolecules ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 1600
Author(s):  
Emily M. Huntsman ◽  
Rachel M. Cho ◽  
Helen V. Kogan ◽  
Nora K. McNamara-Bordewick ◽  
Robert J. Tomko ◽  
...  

The microsporidia Nosema ceranae is an obligate intracellular parasite that causes honey bee mortality and contributes to colony collapse. Fumagillin is presently the only pharmacological control for N. ceranae infections in honey bees. Resistance is already emerging, and alternative controls are critically needed. Nosema spp. exhibit increased sensitivity to heat shock, a common proteotoxic stress. Thus, we hypothesized that targeting the Nosema proteasome, the major protease removing misfolded proteins, might be effective against N. ceranae infections in honey bees. Nosema genome analysis and molecular modeling revealed an unexpectedly compact proteasome apparently lacking multiple canonical subunits, but with highly conserved proteolytic active sites expected to be receptive to FDA-approved proteasome inhibitors. Indeed, N. ceranae were strikingly sensitive to pharmacological disruption of proteasome function at doses that were well tolerated by honey bees. Thus, proteasome inhibition is a novel candidate treatment strategy for microsporidia infection in honey bees.


Author(s):  
Shi Cheng ◽  
Marcel M. van Gaalen ◽  
Mathias Bähr ◽  
Enrique Garea-Rodriguez ◽  
Sebastian Kügler

2021 ◽  
Vol 8 (4) ◽  
pp. 1280
Author(s):  
Srinivas Kalabhavi ◽  
Revanasiddappa Kanagali ◽  
Pramod Makannavar ◽  
Sangamanth Benthur ◽  
Bhuvanesh Aradhya

We present our experience of 15 cases of adrenal tumours who underwent adrenalectomy procedure in last 5 years at our institute and analysed retrospectively clinical outcome. Pre-operative, intra-operative and post-operative data from 15 patients who underwent adrenalectomy between August2015 and July 2020 at our institution were retrospectively collected and reviewed. Diagnosis was obtained on the basis of clinical examination, laboratory values and imaging techniques. Prazosin was preoperatively administered in case of pheochromocytoma. All adrenalectomies were performed by team of urologists. A multidisciplinary management involving endocrinologists, urologists, oncologists, onco-surgeons and anaesthesiologists was carried at our institute. Fifteen patients were evaluated retrospectively in our study. Functioning tumours were diagnosed in 08(53.3%) patients, 06 patients were affected by pheochromocytomas, 2 cases by adrenal cortical carcinoma (ACC). 3 (20%) patients had incidentalomas. 11 (73.3%) patients underwent open adrenalectomy and in 04 (26.6%) patients, laparoscopic adrenalectomy (LA) was performed. An accurate preoperative examination (radiological and biochemical evaluation) is mandatory to select eligible patients to LA or open adrenalectomy (OA). LA is safe and feasible for benign lesions up to 6 cm. A skilled operative team, composed by surgeons experienced in LA after adequate learning curve, is required. Preoperative alfa blockade does not prevent PCC hypertensive crises but, facilitating their pharmacological control, must be recommended.


2020 ◽  
Vol 24 (21) ◽  
pp. 2508-2523
Author(s):  
Johana Gómez ◽  
Diego Sierra ◽  
Constanza Cárdenas ◽  
Fanny Guzmán

One area of organometallic chemistry that has attracted great interest in recent years is the syntheses, characterization and study of organometallic complexes conjugated to biomolecules with different steric and electronic properties as potential therapeutic agents against cancer and malaria, as antibiotics and as radiopharmaceuticals. This minireview focuses on the unique structural diversity that has recently been discovered in α- amino acids and the reactions of metallocene complexes with peptides having different chemical behavior and potential medical applications. Replacing α-amino acids with metallocene fragments is an effective way of selectively influencing the physicochemical, structural, electrochemical and biological properties of the peptides. Consequently, research in the field of bioorganometallic chemistry offers the opportunity to develop bioactive metal compounds as an innovative and promising approach in the search for pharmacological control of different diseases.


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