Biomaterial Database

Inhibitory prostanoid EP receptors in human non-pregnant myometrium. 1999

C J Hillock, and D J Crankshaw

Honours Biology and Pharmacology Programme, McMaster University, Hamilton, Ontario, Canada.

Prostanoid EP receptor agonists relaxed cloprostenol-stimulated contraction of human non-pregnant myometrium in vitro with pEC50 values of (n = 4): prostaglandin E2, 7.8+/-0.2 > 1-OH prostaglandin E1, 7.2+/-0.3 > misoprostol, 6.6+/-0.1 > 16,16-dimethyl prostaglandin E2, 6.3+/-0.7 > butaprost, 5.7+/-0.3 > 11-deoxy prostaglandin E1, 5.5+/-0.2 = AH13205 ((+)-trans-2-[4-(1hydroxyhexyl)phenyl]-5-oxocyclopentaneheptano ic acid), 5.5+/-0.2. The EP4 receptor antagonist AH23848B ([1alpha(z), 2beta5alpha]-(+/-)-7-[5-[[(1,1'-biphenyl)-4-yl]methoxy]-2-(4-morph olinyl)-3-oxo-cyclopentyl]-4-heptenoic acid) (29 microM) had no effect on concentration-effect curves to the EP receptor agonists. The mixed prostanoid receptor antagonist AH6809 (6-isopropoxy-9-oxaxanthene-2-carboxylic acid) competitively antagonised prostaglandin E2 with a pA2 of 5.6+/-0.2. AH6809 (42 microM) antagonised misoprostol, 11-deoxy prostaglandin E1, and the prostanoid DP receptor agonist BW245C (5-(6-carboxyhexyl)-1-(3-cyclohexyl-3-hydroxypropyl)hydantoin) with apparent pA2 values of 5.6+/-0.3, 5.1+/-0.9 and 5.9+/-0.4 (n = 4), respectively, but was ineffective against the IP receptor agonist cicaprost (n = 4). The prostanoid DP receptor antagonist BW A868C (3-benzyl-5-(6-carboxyhexyl)-1-(2-cyclohexyl-2-hydroxyethylamino)h ydantoin) (50 nM) had no effect on responses to prostaglandin E2 or misoprostol. The presence of an AH6809-sensitive, AH23848B- and BW A868C-insensitive mechanism is consistent with the hypothesis that inhibitory EP receptor agonists cause relaxation of human non-pregnant myometrium by an EP2 receptor-mediated process.

UI	MeSH Term	Description	Entries
D009126	Muscle Relaxation	That phase of a muscle twitch during which a muscle returns to a resting position.	Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D009215	Myometrium	The smooth muscle coat of the uterus, which forms the main mass of the organ.	Uterine Muscle,Muscle, Uterine,Muscles, Uterine,Uterine Muscles
D011448	Prostaglandin Antagonists	Compounds that inhibit the action of prostaglandins.	Prostaglandin Inhibitors,Antagonists, Prostaglandin,Inhibitors, Prostaglandin,Prostaglandin Antagonist,Prostaglandin Inhibitor,Antagonist, Prostaglandin,Inhibitor, Prostaglandin
D011453	Prostaglandins	A group of compounds derived from unsaturated 20-carbon fatty acids, primarily arachidonic acid, via the cyclooxygenase pathway. They are extremely potent mediators of a diverse group of physiological processes.	Prostaglandin,Prostanoid,Prostanoids
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005260	Female		Females
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000889	Anti-Arrhythmia Agents	Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade.	Anti-Arrhythmia Agent,Anti-Arrhythmia Drug,Anti-Arrhythmic,Antiarrhythmia Agent,Antiarrhythmia Drug,Antiarrhythmic Drug,Antifibrillatory Agent,Antifibrillatory Agents,Cardiac Depressant,Cardiac Depressants,Myocardial Depressant,Myocardial Depressants,Anti-Arrhythmia Drugs,Anti-Arrhythmics,Antiarrhythmia Agents,Antiarrhythmia Drugs,Antiarrhythmic Drugs,Agent, Anti-Arrhythmia,Agent, Antiarrhythmia,Agent, Antifibrillatory,Agents, Anti-Arrhythmia,Agents, Antiarrhythmia,Agents, Antifibrillatory,Anti Arrhythmia Agent,Anti Arrhythmia Agents,Anti Arrhythmia Drug,Anti Arrhythmia Drugs,Anti Arrhythmic,Anti Arrhythmics,Depressant, Cardiac,Depressant, Myocardial,Depressants, Cardiac,Depressants, Myocardial,Drug, Anti-Arrhythmia,Drug, Antiarrhythmia,Drug, Antiarrhythmic,Drugs, Anti-Arrhythmia,Drugs, Antiarrhythmia,Drugs, Antiarrhythmic
D001713	Biphenyl Compounds	Whitish aromatic crystalline organic compounds made up of two conjoined BENZENE rings.	Compounds, Biphenyl
D014966	Xanthenes	Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.	Xanthene