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Last update 23 Jan 2025

PDE2A

Last update 23 Jan 2025

Basic Info

Synonyms

cGMP-dependent 3',5'-cyclic phosphodiesterase, CGS-PDE, cGSPDE

+ [5]

Introduction

Regulates mitochondrial cAMP levels and respiration (By similarity). Involved in the regulation of mitochondria morphology/dynamics and apoptotic cell death via local modulation of cAMP/PKA signaling in the mitochondrion, including the monitoring of local cAMP levels at the outer mitochondrial membrane and of PKA-dependent phosphorylation of DNM1L (PubMed:28463107). cGMP-activated cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes (PubMed:9210593, PubMed:29392776, PubMed:15938621). Has a higher efficiency with cGMP compared to cAMP (PubMed:15938621). Plays a role in cell growth and migration (PubMed:24705027).

Drugs associated with PDE2A

Doxofylline

Target

A2aR x PDE x PDE2A

Mechanism

A2aR antagonists [+2]

Active Org.

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd. [+1]

Originator Org.-

Active Indication

Bronchitis [+3]

Inactive Indication

Bronchiectasis

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date01 Oct 1988

PDE2 inhibitor(Dart NeuroScience LLC)

Target

PDE2A

Mechanism

PDE2A inhibitors

Active Org.

Dart NeuroScience LLC

Originator Org.

Dart NeuroScience LLC

Active Indication-

Inactive Indication-

Drug Highest PhasePhase 1

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Lu AF64280

Target

PDE2A

Mechanism

PDE2A inhibitors

Active Org.

H. Lundbeck A/S

Originator Org.

H. Lundbeck A/S

Active Indication

Schizophrenia

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with PDE2A

CTR20244717

/ RecruitingNot Applicable

多索茶碱片在中国健康受试者中空腹给药条件下药代动力学比对研究

[Translation] Comparative study on the pharmacokinetics of doxofylline tablets in Chinese healthy subjects under fasting conditions

主要目的：以药代动力学参数为终点指标，比较空腹给药条件下，合肥合源药业有限公司生产的多索茶碱片与ABC FARMACEUTICI S.P.A.为持证商的多索茶碱片（商品名：ANSIMAR，规格：0.4g）在健康成年人群中吸收程度和速度的差异，对两制剂的生物等效性进行评价。次要目的：评价健康受试者口服受试制剂多索茶碱片（规格：0.4g）和参比制剂多索茶碱片（商品名：ANSIMAR，规格：0.4g）的安全性。

[Translation]

The primary objective was to compare the differences in the extent and rate of absorption of the doxofylline tablets produced by Hefei Heyuan Pharmaceutical Co., Ltd. and the doxofylline tablets (trade name: ANSIMAR, specification: 0.4g) licensed by ABC FARMACEUTICI S.P.A. in healthy adults under fasting conditions using pharmacokinetic parameters as endpoints, and to evaluate the bioequivalence of the two preparations. The secondary objective was to evaluate the safety of the test preparation doxofylline tablets (specification: 0.4g) and the reference preparation doxofylline tablets (trade name: ANSIMAR, specification: 0.4g) in healthy subjects when taken orally.

Start Date06 Jan 2025

Sponsor / Collaborator

Hefei Cosource Pharmaceutical, Inc.

CTR20243176

/ Active, not recruitingNot Applicable

多索茶碱片在健康受试者中空腹状态下的单剂量、随机、开放、四周期、完全重复交叉设计的生物等效性试验

[Translation] A single-dose, randomized, open-label, four-period, completely repeated crossover bioequivalence study of doxofylline tablets in healthy subjects under fasting conditions

主要研究目的：研究空腹状态下单次口服受试制剂多索茶碱片（规格：400mg，黑龙江福和制药集团股份有限公司黑龙江福和制药集团股份有限公司）与参比制剂多索茶碱片（商品名：ANSIMAR®，规格：400mg，ABC FARMACEUTICI S.P.A.）在健康成年受试者体内的药代动力学，评价空腹状态下口服两种制剂的生物等效性。次要研究目的: 评价健康受试者空腹单次口服受试制剂（T）多索茶碱片和参比制剂（R）多索茶碱片（商品名：ANSIMAR®）后的安全性。

[Translation]

Main study objectives: To study the pharmacokinetics of the test preparation Doxofylline Tablets (Specification: 400mg, Heilongjiang Fuhe Pharmaceutical Group Co., Ltd. Heilongjiang Fuhe Pharmaceutical Group Co., Ltd.) and the reference preparation Doxofylline Tablets (Trade name: ANSIMAR®, Specification: 400mg, ABC FARMACEUTICI S.P.A.) in healthy adult subjects after a single oral administration under fasting conditions, and to evaluate the bioequivalence of the two preparations after oral administration under fasting conditions. Secondary study objectives: To evaluate the safety of the test preparation (T) Doxofylline Tablets and the reference preparation (R) Doxofylline Tablets (Trade name: ANSIMAR®) after a single oral administration under fasting conditions in healthy subjects.

Start Date28 Dec 2024

Sponsor / Collaborator

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

CTR20243180

/ CompletedNot Applicable

多索茶碱片在健康受试者中餐后状态下的单剂量、随机、开放、四周期、完全重复交叉设计的生物等效性试验

[Translation] A single-dose, randomized, open-label, four-period, completely repeated crossover bioequivalence study of doxofylline tablets in healthy volunteers in the postprandial state

主要研究目的：研究餐后状态下单次口服受试制剂多索茶碱片（规格：400mg，黑龙江福和制药集团股份有限公司黑龙江福和制药集团股份有限公司）与参比制剂多索茶碱片（商品名：ANSIMAR®，规格：400mg，ABC FARMACEUTICI S.P.A.）在健康成年受试者体内的药代动力学，评价餐后状态下口服两种制剂的生物等效性。次要研究目的: 评价健康受试者餐后单次口服受试制剂（T）多索茶碱片和参比制剂（R）多索茶碱片（商品名：ANSIMAR®）后的安全性。

[Translation]

Main study objectives: To study the pharmacokinetics of the test preparation Doxofylline Tablets (Specification: 400mg, Heilongjiang Fuhe Pharmaceutical Group Co., Ltd. Heilongjiang Fuhe Pharmaceutical Group Co., Ltd.) and the reference preparation Doxofylline Tablets (Trade name: ANSIMAR®, Specification: 400mg, ABC FARMACEUTICI S.P.A.) in healthy adult subjects after a single oral administration in the fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fed state. Secondary study objectives: To evaluate the safety of the test preparation (T) Doxofylline Tablets and the reference preparation (R) Doxofylline Tablets (Trade name: ANSIMAR®) after a single oral administration in healthy subjects.

Start Date28 Oct 2024

Sponsor / Collaborator

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

100 Clinical Results associated with PDE2A

100 Translational Medicine associated with PDE2A

0 Patents (Medical) associated with PDE2A

1,149

Literatures (Medical) associated with PDE2A

01 Aug 2025·Neural Regeneration Research

Central role of altered phosphodiesterase 2-dependent signaling in the pathophysiology of cognition-based brain disorders

Article

Author: Tempio, Alessandra ; Boulksibat, Asma ; Bardoni, Barbara

The second messengers 3′, 5′-cyclic adenosine monophosphate (cAMP) and 3′, 5′-cyclic guanosine monophosphate (cGMP) modulate mol. pathways that are involved in a large variety of cellular processes.In the brain, these processes include neurogenesis, neuronal differentiation, activation and function of microglia, and synaptic plasticity, finally resulting in memory formation.All this implies that the homeostasis of these two mols. must be tightly regulated both at their synthesis-that is catalyzed by adenylate/guanylate cyclase-and at their degradation by phosphodiesterases (PDE).The PDE family is composed of 11 subfamilies of proteins that are all expressed in the brain at different levels (Delhaye et al., 2021).

01 Mar 2025·Journal of Medical Mycology

Zingerone effect against Candida albicans growth and biofilm production

Article

Author: Karuppayil, Sankunny Mohan ; Patil, Shivani ; Basrani, Sargun ; Yankanchi, Shivanand ; Chougule, Sayali ; Gavandi, Tanjila ; Jadhav, Ashwini

BACKGROUNDThe increasing resistance of Candida albicans biofilms underscores the urgent need for effective antifungals. This study evaluated the efficacy of zingerone and elucidated its mode of action against C. albicans ATCC 90028 and clinical isolate C1.EXPERIMENTAL PROCEDUREMinimum inhibitory concentrations (MICs) of zingerone were determined using CLSI methods against planktonic cells, biofilm formation, and yeast-to-hyphal transition. The mode of action was investigated through fluorescent microscopy, ergosterol assays, cell cycle analysis, and RT-PCR for gene expression.KEY RESULTSZingerone inhibited planktonic growth and biofilm formation at in C. albicans ATCC 90028 and clinical isolate C1 at 2 mg/mL 4 mg/mL and 1 mg/mL and 2 mg/mL respectively. Treatment with the MIC concentration caused significant cell cycle arrest at the G0/G1 phase, halting proliferation in both the strains. Propidium iodide Staining revealed compromised membrane integrity in both the strains. Also, acridine orange and ethidium bromide dual staining showed increased dead cell proportions in C. albicans ATCC 90028. RT-PCR studies showed downregulation of BCY1, PDE2, EFG1, and upregulation of negative regulators NRG1, TUP1 disrupting growth and virulence pathways. Zingerone induced elevated reactive oxygen species (ROS) levels, triggering apoptosis, evidenced by DNA fragmentation and upregulation of apoptotic markers. It also inhibited ergosterol synthesis in a concentration-dependent manner, crucial for membrane integrity. Importantly, zingerone exhibited minimal hemolytic activity. In an in vivo silkworm model, zingerone demonstrated significant antifungal efficacy, protecting silkworms from infection. It also modulated stress response genes, highlighting its multifaceted action.CONCLUSIONSIn vitro and in vivo findings confirm the potent antifungal efficacy of zingerone against C. albicans ATCC 90028 and clinical isolate C1, suggesting its promising potential as a therapeutic agent that warrants further exploration.

01 Feb 2025·Neurobiology of Disease

Haploinsufficiency of PDE2A causes in mice increased exploratory behavior associated with upregulation of neural nitric oxide synthase in the striatum

Article

Author: Cutuli, Debora ; Sancesario, Giuseppe ; Petrosini, Laura ; Decandia, Davide ; Pellegrini, Manuela ; D'Angelo, Vincenza ; Landolfo, Eugenia ; Cardarelli, Silvia ; D'Amico, Francesca ; D'Amelio, Marcello ; Mercuri, Nicola Biagio ; Giorgi, Mauro ; do Rêgo, Ana Gabriela de Oliveira

Phosphodiesterase 2 A (PDE2A) function is stimulated by cGMP to catabolize cAMP. However, neurological and neurochemical effects of PDE2A deficiency are poorly understood. To address this gap, we studied behavioral characteristics and cerebral morpho-chemical changes of adult male heterozygous C57BL/6-PDE2A+/- (HET), and wild type C57BL/6-PDE2A+/+ (WT) mice. Behavioral functions of mice were evaluated by a wide test battery. HET mice exhibited greater tendency to explore novel environments in comparison to WT mice, but spatial working memory, anxiety, and sociability were similar in adult HET and WT mice. In HET mice, PDE2A mRNA, PDE2A protein expression, and cGMP hydrolyzing enzymatic activity were consistently reduced by about 50 %. Consequently, the cyclic nucleotide levels were significantly increased in HET mice, but unexpectedly the mean percentage variation was higher for cGMP equal to 153.23 %, and lower for cAMP equal to 16.41 %. Therefore, to try to explain the preponderant increase of cGMP to cAMP we evaluated other PDE enzymes functionally related to PDE2A. Surprisingly, results were quite contradictory: in HET mice protein levels of the other dual-specificity enzyme PDE3A and PDE10A were reduced, whereas the expressions of PDE5A and PDE9A that selectively hydrolyze cGMP were increased. Therefore, we investigated the involvement of neuronal nitric oxide synthase (nNOS) expression, as determinant of a possible increased synthesis of NO/cGMP signaling. Interestingly, in HET mice the expression level of brain nNOS, measured by western blot and immune-histochemistry was significantly increased, particularly in interneurons from the striatum. In conclusion, the deficiency of PDE2A could be compensated in the striatum by upregulating nNOS/NO/cGMP pathway, which in turn likely upregulates PDE2A-dependent cAMP hydrolysis. The neuroanatomical correlation between striatal nNOS upregulation and the behavioral phenotype of increased exploratory behavior in HET mice is advanced.

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PDE2A

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