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P2Y 12 is a chemoreceptor for adenosine diphosphate (ADP) [5] [6] that belongs to the G i class of a group of G protein-coupled (GPCR) purinergic receptors. [7] This P2Y receptor family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides.
P2Y 12 structure as generated by PYMOL with color-coded helices. P2Y receptors are membrane proteins belonging to the class A family of G protein-coupled receptors (GPCRs). [5] [6] P2Y receptor proteins display large-scale structural domains typical of GPCRs, consisting of seven hydrophobic transmembrane helices connected by three short extracellular loops and three variably sized ...
This makes it an appealing option for antiplatelet therapy, especially for patients who are unable to take oral drugs (e.g. patient who are unconscious, vomiting or sedated). Like ticagrelor it does not require metabolic conversion to be active and therefore it can directly inhibit the P2Y 12 receptor. [21]
P2Y12 receptors further amplify the response to ADP and draw forth the completion of aggregation. ADP in the blood is converted to adenosine by the action of ecto-ADPases , inhibiting further platelet activation via adenosine receptors .
Microglial processes specifically recognize these purinergic somatic-junctions, and monitor neuronal functions by sensing purine nucleotides via their P2Y12-receptors. In case of neuronal overactivation or injury, microglial processes respond with an increased coverage of neuronal cell bodies, and exert robust neuroprotective effects. [ 38 ]
Ticagrelor (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that is distinct from the mechanism of the thienopyridines in that it reversibly (rather than irreversibly) inhibits the P2Y 12 receptor.
Cangrelor, sold under the brand name Kengreal among others, is a P2Y 12 inhibitor FDA approved as of June 2015 as an antiplatelet drug [5] for intravenous application. Some P2Y 12 inhibitors are used clinically as effective inhibitors of adenosine diphosphate-mediated platelet activation and aggregation. [5]
THP-1 can provide continuous culture when grown in suspension; RPMI 1640 + 10% FBS + 2mM L-Glutamine. The average doubling time is 19 to 50 hours. 1 mM sodium pyruvate, penicillin (100 units/ml) and streptomycin (100 μg/ml) are also commonly added to inhibit bacterial contamination.