Advances in the development of phosphodiesterase-4 inhibitors

T Peng, B Qi, J He, H Ke, J Shi - Journal of Medicinal Chemistry, 2020 - ACS Publications
Cyclic nucleotide phosphodiesterase 4 (PDE4) specifically hydrolyzes cyclic adenosine
monophosphate (cAMP) and plays vital roles in biological processes such as cancer …

Inhibition of PDE4 by FCPR16 induces AMPK-dependent autophagy and confers neuroprotection in SH-SY5Y cells and neurons exposed to MPP+-induced oxidative …

J Zhong, J Xie, J Xiao, D Li, B Xu, X Wang… - Free Radical Biology …, 2019 - Elsevier
The etiology of Parkinson's disease (PD) is generally not well understood, but it is believed
to involve excessive oxidative insult. Hence, identifying therapeutic targets and compounds …

Rolipram ameliorates memory deficits and depression-like behavior in APP/PS1/tau triple transgenic mice: involvement of neuroinflammation and apoptosis via cAMP …

YF Cong, FW Liu, L Xu, SS Song… - International Journal …, 2023 - academic.oup.com
Background Alzheimer disease (AD) and depression often cooccur, and inhibition of
phosphodiesterase-4 (PDE4) has been shown to ameliorate neurodegenerative illness …

Advances in the discovery of PDE10A inhibitors for CNS-related disorders. Part 2: Focus on schizophrenia

A Świerczek, A Jankowska, G Chłoń-Rzepa… - Current Drug …, 2019 - ingentaconnect.com
Schizophrenia is a debilitating mental disorder with relatively high prevalence (~ 1%), during
which positive manifestations (such as psychotic states) and negative symptoms (eg, a …

Roflumilast promotes memory recovery and attenuates white matter injury in aged rats subjected to chronic cerebral hypoperfusion

A Santiago, LM Soares, M Schepers, H Milani… - …, 2018 - Elsevier
Chronic cerebral hypoperfusion (CCH) has been associated with aging-related vascular
dementia, including Alzheimer's disease. It can be induced by the four-vessel …

Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect

L Tang, C Huang, J Zhong, JP He, J Guo, M Liu… - European Journal of …, 2019 - Elsevier
Growing evidence confirms the potential of PDE4 inhibitors for the treatment of Parkinson's
disease. Our reported PDE4 inhibitors FCPR16 and FCPR03 have displayed …

FCPR16, a novel phosphodiesterase 4 inhibitor, produces an antidepressant-like effect in mice exposed to chronic unpredictable mild stress

Q Zhong, H Yu, C Huang, J Zhong, H Wang… - Progress in Neuro …, 2019 - Elsevier
Abstract The canonical phosphodiesterase 4 (PDE4) inhibitors produce antidepressant-like
effects in a variety of animal models. However, severe side effects, particularly vomiting and …

Homeostatic cAMP regulation by the RGS7 complex controls depression-related behaviors

C Orlandi, LP Sutton, BS Muntean, C Song… - …, 2019 - nature.com
Affective disorders arise from abnormal responses of the brain to prolonged exposure to
challenging environmental stimuli. Recent work identified the orphan receptor GPR158 as a …

Inhibition of PDE4 attenuates TNF-α-triggered cell death through suppressing NF-κB and JNK activation in HT-22 neuronal cells

J Xiao, R Yao, B Xu, H Wen, J Zhong, D Li… - Cellular and molecular …, 2020 - Springer
Tumor necrosis factor-α (TNF-α) is a critical pro-inflammatory cytokine regulating
neuroinflammation. At high concentrations, it is toxic to neurons, and such damage is …

[HTML][HTML] Loss of EPAC2 alters dendritic spine morphology and inhibitory synapse density

KA Jones, M Sumiya, KM Woolfrey… - Molecular and Cellular …, 2019 - Elsevier
EPAC2 is a guanine nucleotide exchange factor that regulates GTPase activity of the small
GTPase Rap and Ras and is highly enriched at synapses. Activation of EPAC2 has been …