BAY 60-7550 is an orally active, potent and selective cGMP-dependent phosphodiesterase PDE2 (PDE2A) inhibitor (human/bovine PDE2 IC50 = 4.7/2.0 nM; bovine PDE1 IC50 = 108 nM, human PDE5/5A/10A/4B IC50 = 240/580/704/940/1830 nM, human PDE3B/7B/8A/9A/11A IC50 >4 μM) with little activity (IC50 >10 μM) toward acetylcholinesterase, mAO-A/B, adenosine deaminase, and many receptor subtypes tested. Bay 60-7550 effectively upregulates cGMP and cAMP level in cultured rat and murine neurons (1 nM-1 μM) exposed to guanylyl cyclase (GC) or adenylyl cyclase (AC) stimulator (1 μM Bay 41-8543 or 2 μM forskolin), respectively, as well as exhibits learning and memory-improving efficacy in rats (0.6-3 mg/kg p.o.) and mice (0.3-1 mg/kg p.o.) in vivo.
Orally active, potent and selective cGMP-dependent phosphodiesterase PDE2 (PDE2A) inhibitor with learning and memory-improving efficacy in vivo.
In patients after acute myocardial infarction (AMI), the initial extent of necrosis and inflammation determine clinical outcome. One early event in AMI is the increased cardiac expression of atrial natriuretic peptide (NP) and B-type NP, with their plasma levels correlating
The Journal of neuroscience : the official journal of the Society for Neuroscience, 36(33), 8562-8573 (2016-08-19)
Hypertension is associated with impaired nitric oxide (NO)-cyclic nucleotide (CN)-coupled intracellular calcium (Ca(2+)) homeostasis that enhances cardiac sympathetic neurotransmission. Because neuronal membrane Ca(2+) currents are reduced by NO-activated S-nitrosylation, we tested whether CNs affect membrane channel conductance directly in neurons
European spine journal : official publication of the European Spine Society, the European Spinal Deformity Society, and the European Section of the Cervical Spine Research Society, 26(7), 1961-1968 (2017-03-12)
Phosphodiesterase inhibitors possess anti-inflammatory properties. In addition, some studies report that phosphodiesterase 2A (PDE2A) are highly expressed in the dorsal horn of the spinal cord. The present study aimed to investigate whether intrathecal administration of Bay 60-7550, a specific PDE2A
Fear behaviors are regulated by adaptive mechanisms that dampen their expression in the absence of danger. By studying circuits and the molecular mechanisms underlying this adaptive response, we show that cholinergic neurons of the medial habenula reduce fear memory expression
The European journal of neuroscience, 45(4), 510-520 (2016-11-05)
Cognitive and affective impairments are the most characterized consequences following cerebral ischemia. BAY 60-7550, a selective phosphodiesterase type 2 inhibitor (PDE2-I), presents memory-enhancing and anxiolytic-like properties. The behavioral effects of BAY 60-7550 have been associated with its ability to prevent
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