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(Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - February 26, 2024 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research

Pharmacology education in the medical curriculum: Challenges and opportunities for improvement
AbstractThe knowledge and application of pharmacology is essential for safe prescribing and administration of drugs. In this narrative review, the challenges to pharmacology education in the medical curricula were broadly identified to include issues around content and pedagogies. The increasing number of approved drugs and drug targets, expanding field of pharmacology and the often-changing treatment guidelines and board-defined competencies can make pharmacology education in the medical curriculum daunting. There has been a consensus around the deployment of innovative medical curricula with emphasis on vertical and hori...
Source: Pharmacology Research and Perspectives - February 20, 2024 Category: Drugs & Pharmacology Authors: Pius S. Fasinu, Teresa W. Wilborn Tags: REVIEW Source Type: research

Inhibition of PDE ‐4 isoenzyme attenuates frequency and overall contractility of agonist‐evoked ureteral phasic contractions
AbstractThe aim of this study was to investigate the functional role of phosphodiesterase enzymes (PDE) in the isolated porcine ureter. Distal ureteral strips were mounted in organ baths and pre-contracted with 5-HT (100 μM). Upon generation of stable phasic contractions, PDE-4 and PDE-5 inhibitors were added cumulatively to separate tissues. PDE-4 inhibitors, such as rolipram (10 nM and greater) and roflumilast (100 nM and greater), resulted in significant attenuation of ureteral contractile responses, whil e a higher concentration of piclamilast (1 μM and greater) was required to induce a significant depressan...
Source: Pharmacology Research and Perspectives - February 11, 2024 Category: Drugs & Pharmacology Authors: Iris Lim, Taishi Masutani, Hikaru Hashitani, Russ Chess ‐Williams, Donna Sellers Tags: ORIGINAL ARTICLE Source Type: research

Role of G protein ‐coupled receptor kinases (GRKs) in β2‐adrenoceptor‐mediated glucose uptake
AbstractTruncation of the C-terminal tail of the β2-AR, transfection of βARKct or over-expression of a kinase-dead GRK mutant reduces isoprenaline-stimulated glucose uptake, indicating that GRK is important for this response. We explored whether phosphorylation of the β2-AR by GRK2 has a role in glucose uptake or if this response is related to the role of GRK2 as a scaffolding protein. CHO-GLUT4myc cells expressing wild-type and mutant β2-ARs were generated and receptor affinity for [3H]-CGP12177A and density of binding sites determined together with the affinity of isoprenaline and BRL37344. Following receptor activat...
Source: Pharmacology Research and Perspectives - February 9, 2024 Category: Drugs & Pharmacology Authors: Seungmin Ham, Saori Mukaida, Masaaki Sato, Peter Keov, Tore Bengtsson, Sebastian Furness, Nicholas D. Holliday, Bronwyn A. Evans, Roger J. Summers, Dana S. Hutchinson Tags: ORIGINAL ARTICLE Source Type: research

2 ‐Deoxyglucose and hydroxychloroquine HPLC‐MS–MS analytical methods and pharmacokinetic interactions after oral co‐administration in male rats
Serum concentration versus time curves after single dose alone or combination dosing. (A) 2-DG; (B) HCQ. AbstractOur previous work has shown a synergistic tumoricidal efficacy of combining the hexokinase (HK) inhibitor 2-deoxyglucose (2-DG) and the autophagy inhibitor chloroquine (CQ) through intraperitoneal injections on HK2-addicted prostate cancers in animal models. The pharmacokinetic (PK) behaviors of these oral drugs after simultaneous oral administration have not been reported. We developed high-performance liquid chromatography –tandem mass spectrometry (HPLC-MS–MS) analytical methods for 2-DG and the clinicall...
Source: Pharmacology Research and Perspectives - February 1, 2024 Category: Drugs & Pharmacology Authors: Dongxiao Sun, Sangyub Kim, Deepkamal Karelia, Yibin Deng, Cheng Jiang, Junxuan L ü Tags: SHORT REPORT Source Type: research

Epigenetics in obesity: Mechanisms and advances in therapies based on natural products
XXXX AbstractObesity is a major risk factor for morbidity and mortality because it has a close relationship to metabolic illnesses, such as diabetes, cardiovascular diseases, and some types of cancer. With no drugs available, the mainstay of obesity management remains lifestyle changes with exercise and dietary modifications. In light of the tremendous disease burden and unmet therapeutics, fresh perspectives on pathophysiology and drug discovery are needed. The development of epigenetics provides a compelling justification for how environmental, lifestyle, and other risk factors contribute to the pathogenesis of obesity. ...
Source: Pharmacology Research and Perspectives - January 31, 2024 Category: Drugs & Pharmacology Authors: Peng Chen, Yulai Wang, Fuchao Chen, Benhong Zhou Tags: REVIEW Source Type: research

2 ‐Deoxyglucose and hydroxychloroquine HPLC‐MS–MS analytical methods and pharmacokinetic interactions after oral co‐administration in male rats
Serum concentration versus time curves after single dose alone or combination dosing. (A) 2-DG; (B) HCQ. AbstractOur previous work has shown a synergistic tumoricidal efficacy of combining the hexokinase (HK) inhibitor 2-deoxyglucose (2-DG) and the autophagy inhibitor chloroquine (CQ) through intraperitoneal injections on HK2-addicted prostate cancers in animal models. The pharmacokinetic (PK) behaviors of these oral drugs after simultaneous oral administration have not been reported. We developed high-performance liquid chromatography –tandem mass spectrometry (HPLC-MS–MS) analytical methods for 2-DG and the clinicall...
Source: Pharmacology Research and Perspectives - January 31, 2024 Category: Drugs & Pharmacology Authors: Dongxiao Sun, Sangyub Kim, Deepkamal Karelia, Yibin Deng, Cheng Jiang, Junxuan L ü Tags: SHORT REPORT Source Type: research

Decreased hepatic enzymes reflect the decreased vitamin B6 levels in Parkinson's disease patients
Serum vitamin B6 level was strongly correlated with total levodopa dose in PD patients. AbstractThe study aims to investigate the vitamin B6 levels in Parkinson's disease (PD) patients and their association with liver enzymes and evaluate how much dysregulation is associated with levodopa dose. Furthermore, to evaluate the effect of Opicapone, a catechol-o-methyl-transferase inhibitor, on vitamin B6 levels by monitoring the AST and ALT levels in patients treated with Levodopa –Carbidopa Intestinal Gel Infusion (LCIG). For these aims, serum vitamin B6 levels were measured (PD,n = 72 and controls,n = 31). The vitam...
Source: Pharmacology Research and Perspectives - January 30, 2024 Category: Drugs & Pharmacology Authors: Kensuke Ikenaka, Yuta Kajiyama, C ésar Aguirre, Chi‐Jing Choong, Seira Taniguchi, Junko Doi, Nan Wang, Takahiro Ajiki, Kotaro Ogawa, Keita Kakuda, Yasuyoshi Kimura, Hideki Mochizuki Tags: ORIGINAL ARTICLE Source Type: research

The impact of phosphodiesterase ‐5 inhibition or angiotensin‐converting enzyme inhibition on right and left ventricular remodeling in heart failure due to chronic volume overload
Despite elevated cGMP levels in the lungs of sildenafil-treated rats, PDE5i did not improve survival rate and did not change the cardiac and renal function of ACF rats with advanced HF. In contrast, mortality in the ACF model was reduced by ACEi treatment. AbstractWhile phosphodiesterase-5 inhibition (PED5i) may prevent hypertrophy and failure in pressure-overloaded heart in an experimental model, the impact of PDE5i on volume-overload (VO)-induced hypertrophy is unknown. It is also unclear whether the hypertrophied right ventricle (RV) and left ventricle (LV) differ in their responsiveness to long-term PDE5i and if this t...
Source: Pharmacology Research and Perspectives - January 29, 2024 Category: Drugs & Pharmacology Authors: Tereza Tykvartova, Matus Miklovic, Martin Kotrc, Petra Skaroupkova, Ludmila Kazdova, Jaroslava Trnovska, Vojtech Skop, Michal Kolar, Jiri Novotny, Vojtech Melenovsky Tags: ORIGINAL ARTICLE Source Type: research