Literature DB >> 9630335

Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate.

J L Boyer1, A Mohanram, E Camaioni, K A Jacobson, T K Harden.   

Abstract

The antagonist activity of N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate (N6MABP) has been examined at the phospholipase C-coupled P2Y1 receptor of turkey erythrocyte membranes. N6MABP antagonized 2MeSATP-stimulated inositol phosphate hydrolysis with a potency approximately 20 fold greater than the previously studied parent molecule, adenosine 3',5'-bisphosphate. The P2Y1 receptor antagonism observed with N6MABP was competitive as revealed by Schild analysis (pK(B) = 6.99 +/- 0.13). Whereas N6MABP was an antagonist at the human P2Y1 receptor, no antagonist effect of N6MABP was observed at the human P2Y2, human P2Y4 or rat P2Y6 receptors.

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Year:  1998        PMID： 9630335      PMCID： PMC1565379          DOI： 10.1038/sj.bjp.0701837

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  65 in total

1.  Nucleotide-mediated relaxation in guinea-pig aorta: selective inhibition by MRS2179.

Authors:  Robert A Kaiser; Iain L O Buxton
Journal:  Br J Pharmacol       Date:  2002-01       Impact factor: 8.739

2.  2-Chloro-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y1 receptor antagonist: commentary on Boyer et al.

Authors:  Brian F King
Journal:  Br J Pharmacol       Date:  2002-04       Impact factor: 8.739

Review 3.  Molecular recognition in P2 receptors: ligand development aided by molecular modeling and mutagenesis.

Authors:  K A Jacobson; C Hoffmann; Y C Kim; E Camaioni; E Nandanan; S Y Jang; D P Guo; X D Ji; I von Kügelgen; S Moro; A U Ziganshin; A Rychkov; B F King; S G Brown; S S Wildman; G Burnstock; J L Boyer; A Mohanram; T K Harden
Journal:  Prog Brain Res       Date:  1999       Impact factor: 2.453

4.  Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.

Authors:  E Nandanan; E Camaioni; S Y Jang; Y C Kim; G Cristalli; P Herdewijn; J A Secrist; K N Tiwari; A Mohanram; T K Harden; J L Boyer; K A Jacobson
Journal:  J Med Chem       Date:  1999-05-06       Impact factor: 7.446

5.  (N)-methanocarba-2MeSADP (MRS2365) is a subtype-specific agonist that induces rapid desensitization of the P2Y1 receptor of human platelets.

Authors:  D M Bourdon; S K Mahanty; K A Jacobson; J L Boyer; T K Harden
Journal:  J Thromb Haemost       Date:  2006-04       Impact factor: 5.824

6.  Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.

Authors:  Gary L Waldo; James Corbitt; José L Boyer; Gnana Ravi; Hak Sung Kim; Xiao-Duo Ji; James Lacy; Kenneth A Jacobson; T Kendall Harden
Journal:  Mol Pharmacol       Date:  2002-11       Impact factor: 4.436

7.  Microglia activation triggers astrocyte-mediated modulation of excitatory neurotransmission.

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Journal:  Proc Natl Acad Sci U S A       Date:  2011-12-13       Impact factor: 11.205

8.  Development of a comprehensive set of P2 receptor pharmacological research compounds.

Authors:  R A Felix; S Martin; S Pinion; D J Crawford
Journal:  Purinergic Signal       Date:  2011-11-04       Impact factor: 3.765

9.  The novel suramin analogue NF864 selectively blocks P2X1 receptors in human platelets with potency in the low nanomolar range.

Authors:  Susanne Horner; Kirsten Menke; Caren Hildebrandt; Matthias U Kassack; Peter Nickel; Heiko Ullmann; Martyn P Mahaut-Smith; Günter Lambrecht
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2005-09-13       Impact factor: 3.000

10.  P2Y(1) receptors mediate inhibitory neuromuscular transmission in the rat colon.

Authors:  Laura Grasa; Víctor Gil; Diana Gallego; Maria Teresa Martín; Marcel Jiménez
Journal:  Br J Pharmacol       Date:  2009-11       Impact factor: 8.739
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