Results 61 to 70 of about 4,908 (210)

Potent PDE4 inhibitor activates AMPK and Sirt1 to induce mitochondrial biogenesis.

open access: yesPLoS ONE, 2021
AMP-activated protein kinase (AMPK) is an evolutionarily conserved energy sensor. Activation of AMPK leads to a number of metabolic benefits, including improved mitochondrial function in skeletal muscle and lowering of serum glucose levels in type-2 ...
Sung-Jun Park   +8 more
doaj   +1 more source

The Role of Water Networks in Phosphodiesterase Inhibitor Dissociation and Kinetic Selectivity

open access: yesChemMedChem, Volume 19, Issue 22, November 18, 2024.
Phosphodiesterase (PDE) inhibitor selectivity and binding kinetics can be rationalized with the help of biophysical and computational methods. Water molecules have been found to influence the stability of a key hydrogen bond affecting the kinetic selectivity of inhibitors.
Antoni R. Blaazer   +14 more
wiley   +1 more source

Rolipram und tageszeitliche Rhythmen an Ratten

open access: yes, 2013
Die pharmakologische Wirkung von Rolipram, einem Phosphodiesterase 4 Hemmer, wird an männlichen WISTAR-Ratten mit einer Dosis von 2,5 mg/kg Körpergewicht untersucht. Der Versuchsablauf ist gekennzeichnet durch eine über insgesamt 24 Stunden in jeweils zweistündigem Abstand durchgeführte jeweils sechzigminütige Verhaltensbeobachtung, die unter einem 12 ...
openaire   +1 more source

Innovative pathological network‐based multitarget approaches for Alzheimer's disease treatment

open access: yesMedicinal Research Reviews, Volume 44, Issue 6, Page 2367-2419, November 2024.
Abstract Alzheimer's disease (AD) is the most prevalent neurodegenerative disease and is a major health threat globally. Its prevalence is forecasted to exponentially increase during the next 30 years due to the global aging population. Currently, approved drugs are merely symptomatic, being ineffective in delaying or blocking the relentless disease ...
Paloma Mayo   +5 more
wiley   +1 more source

Differential Effects of PDE4 Inhibitors on Cortical Neurons and T-Lymphocytes

open access: yesJournal of Pharmacological Sciences, 2008
Inhibitors of PDE4 (cAMP-specific phosphodiesterase) induce side effects, including nausea and emesis, that limit their therapeutic potential. We investigated the function of two catalytically active conformations of PDE4 (a low-affinity conformer ...
Ryo Hirose   +4 more
doaj  

Activation of the hypoxia response in the aging cerebrovasculature protects males against cognitive impairment

open access: yesAging Cell, Volume 23, Issue 10, October 2024.
Cerebrovasculature aging leads to blood–brain barrier damage, contributing to the onset of Alzheimer's disease (AD). The male brain produces significant levels of hypoxia‐inducible factors that stimulate angiogenesis and safeguard brain tissue. Increased antigen presentation and decreased angiogenesis capacity during the cerebrovasculature aging in ...
Peihu Li   +12 more
wiley   +1 more source

Journey through the spectacular landscape of melanocortin 1 receptor

open access: yesPigment Cell &Melanoma Research, Volume 37, Issue 5, Page 667-680, September 2024.
Epidermal keratinocytes synthesize and secrete α‐melanocyte stimulating hormone (α‐MSH) and adrenocorticotropic hormone (ACTH). These act as agonists of the melanocortin 1 receptor expressed on the cell surface of human melanocytes. Binding of these physiological agonists or synthetic α‐MSH analogs to human MC1R activates the cAMP pathway, leading to ...
P. R. Upadhyay   +4 more
wiley   +1 more source

Depressive symptom as a risk factor for cirrhosis in patients with primary biliary cholangitis: Analysis based on Lasso‐logistic regression and decision tree models

open access: yesBrain and Behavior, Volume 14, Issue 8, August 2024.
This study demonstrated a high rate of depressive symptoms in patients with PBC. HAMD‐17 score was negatively associated with C4 levels and positively associated with levels of ALP, GGT, TB, IgG, and IgM. Elevated HAMD‐17 score was a discriminating factor for high risk of cirrhosis in Lasso‐logistic regression and decision tree models.
Simin Zhou   +14 more
wiley   +1 more source

Inhibition of phosphodiesterase 4 reduces ethanol intake and preference in C57BL/6J mice

open access: yesFrontiers in Neuroscience, 2014
Some anti-inflammatory medications reduce alcohol consumption in rodent models. Inhibition of phosphodiesterases (PDE) increases cAMP and reduces inflammatory signaling.
Yuri A. Blednov   +3 more
doaj   +1 more source

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