Target Validation Information
Target ID T93515
Target Name P2Y purinoceptor 2
Target Type
Clinical Trial
Drug Potency against Target Diquafosol Drug Info EC50 = 100 nM [552642]
PSB-0963 Drug Info IC50 = 10000 nM [530711]
PSB-716 Drug Info IC50 = 9000 nM [529152]
SB-416 Drug Info IC50 = 17000 nM [529152]
Acid blue 25 Drug Info IC50 = 11000 nM [530711]
RB 2 Drug Info IC50 = 5000 nM [529152]
Action against Disease Model Diquafosol In primate lung tissues, the P2Y(2) receptor mRNA was located by in situ hybridization predominantly in epithelial cells and not in smooth muscle or stromal tissue. The pharmacologic profile of INS37217 parallels that of UTP, leading to increased chloride and water secretion, increased cilia beat frequency, and increased mucin release. [552309] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Mice were treated with ticagrelor or vehicle. Platelet aggregation and P-selectin expression were assessed over time, and thrombus formation was assessed in laser-injured cremasteric arterioles of P2Y(12)+/+ and P2Y(12)-/- mice. Neointima formation in FeCl(3)-injured carotid artery was assessed in C57BL/6 mice treated with different regimens of ticagrelor. Ticagrelor inhibited platelet aggregation and P-selectin expression in a dose-dependent, reversible manner. Ticagrelor inhibited thrombus formation to the same extent as seen in P2Y(12)-/- mice. Neointima formation wasmarkedly reduced in mice treated with ticagrelor before and 4 hours after injury (neointima area: control, 39 921???2 749 |?m(2), versus ticagrelor, 3705???600 |?m(2); P<0.01), whereas administrationof ticagrelor either before injury only or from 4 hours postinjury was ineffective.Ticagrelor effectively and reversibly inhibits P2Y(12)-mediated platelet function and thrombosis in mice. P2Y(12) inhibition is required both at the time of and after injury to effectively inhibit neointima formation. [552309]
References
Ref 552309Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis. J Pharmacol Exp Ther. 2002 Sep;302(3):871-80.
Ref 552642Novel nucleotide triphosphates as potent P2Y2 agonists. Bioorg Med Chem Lett. 2007 Jan 15;17(2):562-5. Epub 2006 Sep 29.
Ref 530711J Med Chem. 2010 Mar 11;53(5):2076-86.Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
Ref 529152Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. Epub 2007 Oct 30.Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists.
Ref 529152Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. Epub 2007 Oct 30.Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists.
Ref 530711J Med Chem. 2010 Mar 11;53(5):2076-86.Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
Ref 529152Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. Epub 2007 Oct 30.Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists.

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