Document Detail

Prostaglandin D2 interacts at thromboxane receptor-sites on guinea-pig platelets.
MedLine Citation:
PMID:  3017497     Owner:  NLM     Status:  MEDLINE    
The anti-aggregatory prostanoid, prostaglandin D2 (PGD2) does not completely inhibit ADP-induced aggregation of guinea-pig platelets and thus produces a bell-shaped dose-inhibition curve. The nature of this bell-shaped curve has now been investigated in guinea-pig platelet-rich plasma. Two selective thromboxane receptor antagonists, 13-aza-prostanoic acid (13-AZA; 16-64.4 microM) and BM 13.177 (5.9-29.8 microM), converted PGD2 to a full inhibitor of aggregation in a dose-related manner. The putative platelet PGD2 receptor antagonist, N-0164 (75 microM) also converted PGD2 to a full inhibitor of platelet aggregation. In contrast to 13-AZA and BM 13.177, higher concentrations of N-0164 (380 and 760 microM) caused a dose-related rightward shift of the PGD2 dose-inhibition curve. The thromboxane receptor antagonism of N-0164 was confirmed in studies in which the dose-aggregation curve to U-46619, a thromboxane mimetic, was competitively antagonized with a pA2 value of 4.67 and a slope of 1.13, comparable to that of 13-AZA. The results show that N-0164 acts as both a platelet PGD2 and thromboxane-receptor antagonist in both human and guinea-pig platelet-rich plasma. The results further indicate that PGD2 can interact at thromboxane receptors in guinea-pig platelets.
S Hamid-Bloomfield; B J Whittle
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  British journal of pharmacology     Volume:  88     ISSN:  0007-1188     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  1986 Aug 
Date Detail:
Created Date:  1986-10-08     Completed Date:  1986-10-08     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  931-6     Citation Subset:  IM    
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MeSH Terms
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Adenosine Diphosphate / pharmacology
Blood Platelets / drug effects,  metabolism*
Guinea Pigs
Organophosphorus Compounds / pharmacology
Phosphonic Acids*
Platelet Aggregation / drug effects
Prostaglandin D2
Prostaglandin Endoperoxides, Synthetic / pharmacology
Prostaglandins D / blood*
Prostanoic Acids / pharmacology
Receptors, Cell Surface / metabolism*
Receptors, Prostaglandin / metabolism*
Receptors, Thromboxane
Sulfonamides / pharmacology
Reg. No./Substance:
0/Organophosphorus Compounds; 0/Phosphonic Acids; 0/Prostaglandin Endoperoxides, Synthetic; 0/Prostaglandins D; 0/Prostanoic Acids; 0/Receptors, Cell Surface; 0/Receptors, Prostaglandin; 0/Receptors, Thromboxane; 0/Sulfonamides; 41598-07-6/Prostaglandin D2; 58-64-0/Adenosine Diphosphate; 60787-00-0/N 0164; 71629-07-7/13-azaprostanoic acid; 72131-33-0/sulotroban; 76898-47-0/15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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