Results 131 to 140 of about 6,211 (154)

A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor

Bioorganic & Medicinal Chemistry Letters, 2011
A novel series of P2Y(12) antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds showed P2Y(12) antagonistic activities in the sub-micromolar range.
Peter, Bach, Jonas, Boström, Kay, Brickmann, J J J, van Giezen, Ragnar, Hovland, Annika U, Petersson, Asim, Ray, Fredrik, Zetterberg   +7 more
openaire   +2 more sources

The role of purinergic P2Y12 receptor blockers on the angiogenic properties of endothelial cells: an in vitro study.

Journal of physiology and pharmacology : an official journal of the Polish Physiological Society, 2018
Pharmacotherapy with agents that inhibit platelet function has proven to be effective in the treatment of acute coronary syndrome. Proper re-endothelization after angioplasty prevents adverse cardiovascular events. Therefore, in this in vitro study we examined how antiplatelet P2Y12 receptor blockers can affect endothelial cells' angiogenic properties.
K, Korybalska, R, Rutkowski, J, Luczak, N, Czepulis, K, Karpinski, J, Witowski   +5 more
openaire   +2 more sources

Purinergic P2Y12 Receptor Blockade Inhibits Shear-Induced Platelet Phosphatidylinositol 3-Kinase Activation

Molecular Pharmacology, 2003
Pathologically elevated shear stress triggers aspirin-insensitive platelet thrombosis. Signaling mechanisms involved in shear-induced platelet thrombosis are not well understood. To investigate these, we examined the hypothesis that functionally important platelet phosphatidylinositol 3-kinase (PI3-K) activity is stimulated by an in vitro shear stress ...
Julio C, Reséndiz, Shuju, Feng, Guilan, Ji, Ketia A, Francis, Michael C, Berndt, Michael H, Kroll   +5 more
openaire   +2 more sources

Purinergic Receptor P2Y12-Mediated Tau Internalization in Microglia

Microglia are the resident brain macrophage cells that are involved in constant surveillance of brain microenvironment. In Alzheimer's disease, microglia get over activated upon the accumulation of Tau and amyloid-β species in the extracellular space, ultimately leading to neurodegeneration.
Hariharakrishnan Chidambaram, Smita Eknath Desale, Subashchandrabose Chinnathambi   +2 more
openaire   +2 more sources

Functional characterization of purinergic P2Y2 and P2Y12 receptors involved in Japanese flounder (Paralichthys olivaceus) innate immune responses

Fish & Shellfish Immunology, 2018
G-protein-coupled P2Y receptors activated by extracellular nucleotides play important roles under different physiological and pathophysiological conditions in mammals. To investigate the immunological relevance of P2Y receptors in fish, we identified and characterized the P2Y2 and P2Y12 receptors in Japanese flounder Paralichthys olivaceus.
Shuo, Li, Gaixiang, Hao, Yaqi, Xu, Nan, Wang, Jiafang, Li, Xuyun, Geng, Jinsheng, Sun   +6 more
openaire   +2 more sources

The role of the purinergic receptor P2Y12 in Alzheimer's disease

Alzheimer’s disease (AD), the most common cause of dementia, shows a significant rise in prevalence due to increased global life expectancy and represents a major public health, social, and economic burden. Microglia, the resident immune cells of the CNS, have recently moved into prime focus of AD research due to the discovery of risk loci and genes ...
openaire   +1 more source

Toll like receptor 2/1 mediated platelet adhesion and activation on bacterial mimetic surfaces is dependent on src/Syk-signaling and purinergic receptor P2X1 and P2Y12 activation

Biointerphases, 2014
Platelets are considered to have important functions in inflammatory processes as key players in innate immunity. Toll like receptors (TLRs), expressed on platelets, recognize pathogen associated molecular patterns and trigger immune responses. Pathogens are able to adhere to human tissues and form biofilms which cause a continuous activation of the ...
Kristin, Klarström Engström, Caroline, Brommesson, Hanna, Kälvegren, Torbjörn, Bengtsson   +3 more
openaire   +2 more sources

Carba‐nucleosides as Potent Antagonists of the Adenosine 5′‐Diphosphate (ADP) Purinergic Receptor (P2Y₁₂) on Human Platelets

ChemMedChem, 2008
Whereas the activation and aggregation of blood platelets are crucial to normal hemostasis, this ensemble is also a key factor in serious cardiovascular disorders, such as myocardial infarction, unstable angina, transient ischemic attack, stroke, peripheral arterial disease, and artherosclerosis.
Hong, Ye, Cailin, Chen, Han-Cheng, Zhang, Barbara, Haertlein, Tom J, Parry, Bruce P, Damiano, Bruce E, Maryanoff   +6 more
openaire   +2 more sources

Restored response to ADP downstream of purinergic P2Y₁₂ receptor in apheresis platelets after pathogen‐reducing xenon flash treatment

Transfusion, 2018
BACKGROUNDOur previous study revealed that pathogen‐reducing filtered xenon flash‐treated platelets (fXe‐PLTs) showed sustained aggregation in response to adenosine diphosphate (ADP), but apheresis‐collected PLTs (Aph‐PLTs) showed reversible aggregation.STUDY DESIGN AND METHODSAph‐PLTs, fXe‐PLTs, and freshly prepared PLTs (PRP‐PLTs) from whole blood ...
Hideki, Abe, Takaaki, Abe, Masayuki, Shiba, Masahiro, Satake   +3 more
openaire   +2 more sources

Interaction of Tau with G-Protein-Coupled Purinergic P2Y12 Receptor by Molecular Docking and Molecular Dynamic Simulation

Alzheimer's disease, a progressive neurological disorder, is characterized by the accumulation of neurofibrillary tangles and senile plaques by Tau and amyloid-β, respectively, in the brain microenvironment. The misfolded protein aggregates interact with several components of neuronal and glial cells such as membrane lipids, receptors, transporters ...
Hariharakrishnan Chidambaram, Smita Eknath Desale, Subashchandrabose Chinnathambi   +2 more
openaire   +2 more sources