Literature DB >> 2466517

The antagonism by BW A868C of PGD2 and BW245C activation of human platelet adenylate cyclase.

D G Trist1, B A Collins, J Wood, M G Kelly, A D Robertson.   

Abstract

1. In glycerol-lysed human platelets, prostaglandin D2 (PGD2) and the hydantoin BW245C both activate adenylate cyclase in a biphasic manner. These activations are qualitatively different from those of carbacyclin, iloprost and prostaglandin E2 (PGE2) whose E/[A] curves can be adequately described by rectangular hyperbolae. 2. Prostaglandin E1 (PGE1) had E/[A] curves of slope significantly lower than that expected for a rectangular hyperbolae. 2. Prostaglandin E1 (PGE1) had E/[A] curves of slope significantly lower than that expected for a rectangular hyperbola. 3. The selective PGD2 antagonist BW A868C shifts the first phase of the PGD2 and BW245C E/[A] curves but has no effect on the second phase. 4. Applying a two-receptor model enables a pKB to be derived for BW A868C of 9.11. 5. BW A868C has no effect on carbacyclin, iloprost, prostacyclin, PGE1 and PGE2 at a concentration 1,000 fold that of its KB against PGD2 and BW245C. 6. These results indicate that PGD2 and BW245C are capable of activating adenylate cyclase in human platelets through the DP-receptor and by another mechanism as yet uncharacterized.

Entities:  

Mesh:

Substances:

Year:  1989        PMID: 2466517      PMCID: PMC1854363          DOI: 10.1111/j.1476-5381.1989.tb11817.x

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


  15 in total

1.  A highly sensitive adenylate cyclase assay.

Authors:  Y Salomon; C Londos; M Rodbell
Journal:  Anal Biochem       Date:  1974-04       Impact factor: 3.365

2.  Evidence for distinct prostaglandin I2 and D2 receptors in human platelets.

Authors:  O V Miller; R R Gorman
Journal:  J Pharmacol Exp Ther       Date:  1979-07       Impact factor: 4.030

3.  An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation.

Authors:  S Moncada; R Gryglewski; S Bunting; J R Vane
Journal:  Nature       Date:  1976-10-21       Impact factor: 49.962

4.  Selective binding site for [3H]prostacyclin on platelets.

Authors:  A M Siegl; J B Smith; M J Silver; K C Nicolaou; D Ahern
Journal:  J Clin Invest       Date:  1979-02       Impact factor: 14.808

5.  Modulation of human platelet adenylate cyclase by prostacyclin (PGX).

Authors:  R R Gorman; S Bunting; O V Miller
Journal:  Prostaglandins       Date:  1977-03

6.  Inhibition of PGE1-stimulated cAMP accumulation in human platelets by thromboxane a2.

Authors:  O V Miller; R A Johnson; R R Gorman
Journal:  Prostaglandins       Date:  1977-04

7.  Comparison of the effects of prostacyclin (PGI2), prostaglandin E1 and D2 on platelet aggregation in different species.

Authors:  B J Whittle; S Moncada; J R Vane
Journal:  Prostaglandins       Date:  1978-09

8.  The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective and potent competitive antagonist.

Authors:  H Giles; P Leff; M L Bolofo; M G Kelly; A D Robertson
Journal:  Br J Pharmacol       Date:  1989-02       Impact factor: 8.739

9.  Studies on the characterisation of prostanoid receptors: a proposed classification.

Authors:  I Kennedy; R A Coleman; P P Humphrey; G P Levy; P Lumley
Journal:  Prostaglandins       Date:  1982-11

10.  Regulation of human platelet adenylate cyclase by epinephrine, prostaglandin E1, and guanine nucleotides. Evidence for separate guanine nucleotide sites mediating stimulation and inhibition.

Authors:  M L Steer; A Wood
Journal:  J Biol Chem       Date:  1979-11-10       Impact factor: 5.157

View more
  10 in total

1.  The role of prostanoid TP- and DP-receptors in the bronchoconstrictor effect of inhaled PGD2 in anaesthetized guinea-pigs: effect of the DP-antagonist BW A868C.

Authors:  S Hamid-Bloomfield; A N Payne; A A Petrovic; B J Whittle
Journal:  Br J Pharmacol       Date:  1990-08       Impact factor: 8.739

2.  Prostaglandin DP receptors positively coupled to adenylyl cyclase in embryonic bovine tracheal (EBTr) cells: pharmacological characterization using agonists and antagonists.

Authors:  J Y Crider; B W Griffin; N A Sharif
Journal:  Br J Pharmacol       Date:  1999-05       Impact factor: 8.739

3.  Albumin-bound docosahexaenoic acid and collagen-induced human platelet reactivity.

Authors:  D C Gaudette; B J Holub
Journal:  Lipids       Date:  1990-03       Impact factor: 1.880

4.  Pharmacology and autoradiography of human DP prostanoid receptors using [(3)H]-BWA868C, a DP receptor-selective antagonist radioligand.

Authors:  N A Sharif; G W Williams; T L Davis
Journal:  Br J Pharmacol       Date:  2000-11       Impact factor: 8.739

5.  Excitotoxicity-induced prostaglandin D2 production induces sustained microglial activation and delayed neuronal death.

Authors:  Kensuke Iwasa; Shinji Yamamoto; Sosuke Yagishita; Kei Maruyama; Keisuke Yoshikawa
Journal:  J Lipid Res       Date:  2017-02-07       Impact factor: 5.922

6.  Molecular characterization of a mouse prostaglandin D receptor and functional expression of the cloned gene.

Authors:  M Hirata; A Kakizuka; M Aizawa; F Ushikubi; S Narumiya
Journal:  Proc Natl Acad Sci U S A       Date:  1994-11-08       Impact factor: 11.205

7.  The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective and potent competitive antagonist.

Authors:  H Giles; P Leff; M L Bolofo; M G Kelly; A D Robertson
Journal:  Br J Pharmacol       Date:  1989-02       Impact factor: 8.739

8.  Modulation of noradrenaline release from the sympathetic nerves of the human saphenous vein and pulmonary artery by presynaptic EP3- and DP-receptors.

Authors:  G J Molderings; E Colling; J Likungu; J Jakschik; M Göthert
Journal:  Br J Pharmacol       Date:  1994-03       Impact factor: 8.739

9.  Antagonism of PGD2 vasodepressor responses in the rat in vivo by the novel, selective antagonist, BW A868C.

Authors:  S Hamid-Bloomfield; B J Whittle
Journal:  Br J Pharmacol       Date:  1989-02       Impact factor: 8.739

10.  Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor.

Authors:  Pascale Labrecque; Sébastien J Roy; Louis Fréchette; Christian Iorio-Morin; Maxime A Gallant; Jean-Luc Parent
Journal:  PLoS One       Date:  2013-06-10       Impact factor: 3.240

  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.