Last update 01 Nov 2024

PDE3 x COX

Last update 01 Nov 2024

Basic Info

Related Targets

PDE3COX

Drugs associated with PDE3 x COX

Satigrel

Target

COX x PDE3

Mechanism

COX inhibitors [+1]

Active Org.-

Originator Org.

Eisai Co., Ltd.

Active Indication-

Inactive Indication

Thrombosis

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with PDE3 x COX

100 Translational Medicine associated with PDE3 x COX

0 Patents (Medical) associated with PDE3 x COX

Literatures (Medical) associated with PDE3 x COX

02 Nov 2015·Journal of Enzyme Inhibition and Medicinal ChemistryQ2 · MEDICINE

Studies on the antiplatelet and antithrombotic profile of anti-inflammatory coumarin derivatives

Q2 · MEDICINE

ArticleOA

Author: Hadjipavlou-Litina, Dimitra ; Barocelli, Elisabetta ; Patsilinakos, Alexandros ; Tognolini, Massimiliano ; Mangiatordi, Giuseppe Felice ; Kontogiorgis, Christos ; Carotti, Angelo ; Karalaki, Foteini ; Giorgio, Carmine ; Nicolotti, Orazio

The interest towards coumarin-based structures stems from their polypharmacological profile. Herein, we present a series of Mannich bases and 7-azomethine-linked coumarin derivatives exhibiting antiplatelet and antithrombotic activities, in addition to the already known anti-inflammatory and antioxidant activities. Among others, compounds 15 and 16 were found to be the most potent and selective inhibitors of platelet aggregation whereas compound 3 also proved to be the most potent in the clot retraction assay. Structure-activity relationship studies were conducted to elucidate the molecular determinants responsible for the herein observed activities. The chance of inhibiting cyclooxygenase-1 was also investigated for evaluating the platelet aggregation induced by arachidonic acid. Taken together, these results suggest that the investigation of other targets connected to the antiplatelet activity, such as phosphodiesterase-3 (PDE3), could be a viable strategy to shed light on the polypharmacological profile of coumarin-based compounds. Docking simulations towards PDE3 were also carried out.

02 Nov 2015·Expert Opinion on Therapeutic TargetsQ2 · MEDICINE

Ovarian and oocyte targets for development of female contraceptives

Q2 · MEDICINE

Review

Author: Malik, Ankita ; Arukha, Ananta Prasad ; Gupta, Satish Kumar

INTRODUCTIONSteroid hormone-based contraceptives have been used by women for long time since their introduction. Efforts have been made to make steroidal contraceptives cost-effective, safe and improve their users' compliance. In addition, attempts have been made to develop nonsteroidal contraceptives. Contraceptive vaccines have been investigated as an alternate strategy for contraception.AREAS COVEREDThe currently used steroidal contraceptives are reviewed. In addition, status of emerging nonsteroidal contraceptives that inhibit folliculogenesis, oocyte maturation, ovulation and endometrium receptivity targeting phosphodiesterase 3, angiopoietins, gonadotropin-releasing hormone, COX-2, progesterone/estrogen receptor and follicle-stimulating hormone receptor are presented. Various approaches to develop contraceptive vaccines aiming to inhibit ovarian follicle development, ovulation, fertilization and implantation including their current applications and limitations are discussed.EXPERT OPINIONDevelopment of new nonsteroidal contraceptives, in addition to long-acting steroidal contraceptives, is pertinent for offering wider choice to women. It is imperative that basic research to discover new targets in the ovaries must be undertaken to facilitate development of novel contraceptives. Further, efforts on studying the feasibility and safety of contraceptive vaccines may be continued to bring these within the realm of application as contraceptives for humans.

01 Feb 2012·Clinical and Experimental NephrologyQ3 · MEDICINE

Convergence of major physiological stimuli for renin release on the Gs-alpha/cyclic adenosine monophosphate signaling pathway

Q3 · MEDICINE

Review

Author: Josephine P. Briggs ; Soo Mi Kim ; Jurgen Schnermann

Control of the renin system by physiological mechanisms such as the baroreceptor or the macula densa (MD) is characterized by asymmetry in that the capacity for renin secretion and expression to increase is much larger than the magnitude of the inhibitory response. The large stimulatory reserve of the renin-angiotensin system may be one of the causes for the remarkable salt-conserving power of the mammalian kidney. Physiological stimulation of renin secretion and expression relies on the activation of regulatory pathways that converge on the cyclic adenosine monophosphate/protein kinase A (cAMP/PKA) pathway. Mice with selective Gs-alpha (Gsα) deficiency in juxtaglomerular granular cells show a marked reduction of basal renin secretion, and an almost complete unresponsiveness of renin release to furosemide, hydralazine, or isoproterenol. Cyclooxygenase-2 generating prostaglandin E(2) (PGE(2)) and prostacyclin (PGI(2)) in MD and thick ascending limb cells is one of the main effector systems utilizing Gsα-coupled receptors to stimulate the renin-angiotensin system. In addition, β-adrenergic receptors are critical for the expression of high basal levels of renin and for its release response to lowering blood pressure or MD sodium chloride concentration. Nitric oxide generated by nitric oxide synthases in the MD and in endothelial cells enhances cAMP-dependent signaling by stabilizing cAMP through cyclic guanosine monophosphate-dependent inhibition of phosphodiesterase 3. The stimulation of renin secretion by drugs that inhibit angiotensin II formation or action results from the convergent activation of cAMP probably through indirect augmentation of the activity of PGE(2) and PGI(2) receptors, β-adrenergic receptors, and nitric oxide.

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