PMID: 7260485Mar 1, 1981

5'-N-ethylcarboxamidoadenosine: a potent inhibitor of human platelet aggregation

British Journal of Pharmacology
N J Cusack, S M Hourani

Abstract

1 5'-N-ethylcarboxamidoadenosine (NECA) is an adenosine analogue which is 22,900 times more potent than adenosine as a vasodilator. Adenosine and some of its analogues are also inhibitors of human platelet aggregation. NECA was tested for its effects on human platelets. 2 NECA (1 microM) inhibited human platelet aggregation induced by adenosine 5'-diphosphate (ADP), adrenaline, 5-hydroxytryptamine (5-HT) and thrombin more powerfully than adenosine. NECA was 5 to 10 times more potent than adenosine at inhibiting ADP- and adrenaline-induced aggregation. 3 NECA, like adenosine, caused dose-dependent increases in levels of platelet adenosine 3',5'-cyclic monophosphate (cyclic AMP), which were competitively inhibited by theophylline, an adenosine antagonist. 4 These effects of NECA, like those of adenosine, were completely stereospecific as the L-enantiomer of NECA was inactive. 5 NECA did not interfere with the inhibition by ADP of prostaglandin E1 (PGE1)-stimulated adenylate cyclase. 6 NECA is the most potent analogue of adenosine tested so far on human platelets, and is the first example of a 5' modification to retain affinity for the platelet adenosine receptor.

References

Jul 20, 1977·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·N J Cusack, G V BORN
Nov 30, 1979·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·N J CusackG V BORN
Jan 1, 1974·British Journal of Pharmacology·L B CobbinM H Maguire
Apr 1, 1973·Journal of Medicinal Chemistry·K KikugawaM Ichino
Dec 1, 1973·Journal of Medicinal Chemistry·K KikugawaM Ichino

Citations

Jan 25, 2000·Archives of Insect Biochemistry and Physiology·C Caruso-NevesA G Lopes
Sep 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·U SchwabeM J Lohse
Oct 29, 1985·European Journal of Pharmacology·D UkenaU Schwabe
Jan 1, 1986·General Pharmacology·T H Swanson, C L Green
Jul 29, 1998·Bioorganic & Medicinal Chemistry·S A Poulsen, R J Quinn
Feb 1, 1996·The Journal of Pharmacy and Pharmacology·N P TomkinsonN D Kindon
Apr 1, 1988·La Ricerca in Clinica E in Laboratorio·S QuattrinG Marone
Jul 1, 1992·The American Journal of Emergency Medicine·S L Orebaugh, M Handy
Mar 1, 1984·British Journal of Pharmacology·G BurnstockC H Hoyle
Jan 1, 1982·British Journal of Pharmacology·C BrownC J Moody
Aug 12, 2015·Purinergic Signalling·Geoffrey Burnstock
May 22, 2016·BMC Biochemistry·Yasunori FukudaJunji Matsui
Aug 1, 1993·Journal of Cardiothoracic and Vascular Anesthesia·J A GatellK Shevde
Dec 21, 2006·ChemMedChem·Gloria CristalliRosaria Volpini
May 31, 2008·Arteriosclerosis, Thrombosis, and Vascular Biology·Melanie L HartHolger K Eltzschig
Dec 1, 1985·Journal of Neurochemistry·M J LohseU Schwabe
Oct 16, 2018·Cardiovascular & Hematological Disorders Drug Targets·Trevor SimardBenjamin Hibbert
Jan 1, 1994·Platelets·W W BakkerD P Mikhailidis
Jan 1, 1992·International Journal of Clinical & Laboratory Research·G MaroneV Casolaro
Jan 8, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nina WolskaMarcin Rozalski
Nov 7, 2019·International Journal of Molecular Sciences·Nina Wolska, Marcin Rozalski

Related Concepts

Adenocard
Adenylate Cyclase
Platelet Aggregation
Prostaglandins E
Vasoactive Antagonists
Adenosine-5'-(N-ethylcarboxamide)

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