phosphodiesterase 4 inhibitors
Summary: Compounds that specifically inhibit PHOSPHODIESTERASE 4.
Chou A, D Urzo A. New therapy for managing moderate to severe chronic obstructive pulmonary disease. Can Fam Physician. 2014;60:352-4 pubmed
Zou Z, Chen J, Feng H, Cheng Y, Wang H, Zhou Z, et al
. Novel Phosphodiesterase 4 Inhibitor FCPR03 Alleviates Lipopolysaccharide-Induced Neuroinflammation by Regulation of the cAMP/PKA/CREB Signaling Pathway and NF-?B Inhibition. J Pharmacol Exp Ther. 2017;362:67-77 pubmed publisher
..Our findings suggest that FCPR03 inhibits the neuroinflammatory response through the activation of cAMP/PKA/CREB signaling pathway and NF-?B inhibition. ..
Eichenfield L, Call R, Forsha D, Fowler J, Hebert A, Spellman M, et al
. Long-term safety of crisaborole ointment 2% in children and adults with mild to moderate atopic dermatitis. J Am Acad Dermatol. 2017;77:641-649.e5 pubmed publisher
..2%). Nine patients (1.7%) discontinued the long-term study because of TEAEs. Long-term efficacy was not analyzed. Crisaborole ointment had a low frequency of treatment-related AEs over 48 weeks of treatment of patients with AD. ..
White W, Cooke G, Kowey P, Calverley P, Bredenbröker D, Goehring U, et al
. Cardiovascular safety in patients receiving roflumilast for the treatment of COPD. Chest. 2013;144:758-765 pubmed publisher
..Potential cardiovascular benefits of roflumilast should be evaluated in future controlled clinical trials. ..
Ahidjo B, Bishai W. Phosphodiesterase inhibitors as adjunctive therapies for tuberculosis. EBioMedicine. 2016;4:7-8 pubmed publisher
Jarnagin K, Chanda S, Coronado D, Ciaravino V, Zane L, Guttman Yassky E, et al
. Crisaborole Topical Ointment, 2%: A Nonsteroidal, Topical, Anti-Inflammatory Phosphodiesterase 4 Inhibitor in Clinical Development for the Treatment of Atopic Dermatitis. J Drugs Dermatol. 2016;15:390-6 pubmed
Kistemaker L, Oenema T, Baarsma H, Bos I, Schmidt M, Facchinetti F, et al
. The PDE4 inhibitor CHF-6001 and LAMAs inhibit bronchoconstriction-induced remodeling in lung slices. Am J Physiol Lung Cell Mol Physiol. 2017;313:L507-L515 pubmed publisher
..The combination of CHF-6001 and anticholinergics was more effective than the individual compounds. This cooperativity might be explained by the distinct mechanisms of action inhibiting TGF-? release and bronchoconstriction. ..
Hasegawa F, Kawamura K, Tsuchikawa H, Murata M. Stable C-N axial chirality in 1-aryluracil scaffold and differences in in vitro metabolic clearance between atropisomers of PDE4 inhibitor. Bioorg Med Chem. 2017;25:4506-4511 pubmed publisher
..This finding demonstrates the potential utility of stable C-N bond atropisomers in the development of chiral drugs. ..
Niccolini F, Wilson H, Pagano G, Coello C, Mehta M, Searle G, et al
. Loss of phosphodiesterase 4 in Parkinson disease: Relevance to cognitive deficits. Neurology. 2017;89:586-593 pubmed publisher
..Our findings demonstrate loss of PDE4 expression in the striato-thalamo-cortical circuit, which is associated with deficits of spatial working memory in patients with PD. ..