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Pharmacology Guide

Neurotransmitters and other chemical signalling agents

PROSTANOIDS (Prostaglandins, prostacyclin and thromboxane)
Precursors: rachidonic acid (i.e. eicosatetraenoic acid;
2-series prostanoids), eicosatri- and
eicosapentaenoic acids
Synthesising enzymes: Prostaglandin synthetase (cyclooxygenase),
PGI2 synthase, TX synthase.
Metabolising enzymes: 15-hydroxyprostaglandin dehydrogenase,
PG-9-keto-reductase
Metabolites: large number of oxidised metabolites
Receptor subtypes
(most potent natural prostanoid)
Agonists Antagonists Second messenger
DP (PGD(2)) BW245C, ZK110841 BWA868C, AH6809 <87>cAMP
EP (PGE(2)), subdivided as shown:
EP(1) sulprostone, iloprost AH6809, SC-19220 PI
EP(2) AY23626, butaprost,
rioprostil
none <87>cAMP
EP(3) sulprostone
AY23626, rioprostil,
enprostil, GR 63799
none PI, <51>cAMP
FP (PGF(2-alpha)) fluprostenol,
cloprostenol
none PI
IP (PGI(2)) iloprost,cicaprost none <87>cAMP
TP (TXA(2)) U-46619, STA2,
EP171
GR32191, EP092,
BM13505, SQ28668
PI

NB: (+ve) indicates increase; (-ve) indicates decrease.

Reviews
Coleman, R.A., Kennedy, I., Humphrey, P.P.A., Bunce, K.T. and Lumley, P. (1990). `Prostanoids and their receptors.' In: Comprehensive Medicinal Chemistry, vol. 3., eds C. Hansch, P.G. Sammes and J.B. Taylor, Pergamon Press, Oxford, pp 643-714.


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