Effects of the thromboxane-receptor antagonist L-636,499 on feline cerebral arteries. 1986

T K Uski, and K E Andersson

The effects of the thromboxane-receptor antagonist L-636,499 on contractions induced by U46619 and prostaglandin (PG)F2 alpha were studied in the isolated feline basilar artery (BA). L-636,499 (10(-6)-3 X 10(-5) mol l-1) shifted concentration-response curves induced by U46619 to the right in a parallel manner. By contrast, concentration-response curves induced by PGF2 alpha were displaced only when L-636,499 concentrations of 10(-5) and 3 X 10(-5) mol l-1 were used. The Schild plot using U46619 as the agonist revealed a slope index (0.69) which was significantly less than unity. PA2-values calculated according to the method of van Rossum differed significantly between different concentration intervals of L-636,499. At 10(-6) to 3 X 10(-6) mol l-1 the PA2-value was 5.99, whereas at 10(-5) to 3 X 10(-5) mol l-1 it was 5.59. Using PGF2 alpha as the agonist the PA2-value at the L-636,499 concentration interval 10(-5) to 3 X 10(-5) mol l-1 was 5.69. It may be concluded that the feline BA contains two receptor sites mediating prostanoid-induced contraction, one of which may be characterized as a thromboxane-sensitive (TP) receptor. L-636,499 can interact with both receptor sites with highest affinity for the TP receptor site.

UI MeSH Term Description Entries
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D011450 Prostaglandin Endoperoxides, Synthetic Synthetic compounds that are analogs of the naturally occurring prostaglandin endoperoxides and that mimic their pharmacologic and physiologic activities. They are usually more stable than the naturally occurring compounds. Prostaglandin Endoperoxide Analogs,Prostaglandin Endoperoxide Analogues,Synthetic Prostaglandin Endoperoxides,Analogues, Prostaglandin Endoperoxide,Endoperoxide Analogues, Prostaglandin,Endoperoxides, Synthetic Prostaglandin
D011460 Prostaglandins F (9 alpha,11 alpha,13E,15S)-9,11,15-Trihydroxyprost-13-en-1-oic acid (PGF(1 alpha)); (5Z,9 alpha,11,alpha,13E,15S)-9,11,15-trihydroxyprosta-5,13-dien-1-oic acid (PGF(2 alpha)); (5Z,9 alpha,11 alpha,13E,15S,17Z)-9,11,15-trihydroxyprosta-5,13,17-trien-1-oic acid (PGF(3 alpha)). A family of prostaglandins that includes three of the six naturally occurring prostaglandins. All naturally occurring PGF have an alpha configuration at the 9-carbon position. They stimulate uterine and bronchial smooth muscle and are often used as oxytocics. PGF
D011982 Receptors, Prostaglandin Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors). Prostaglandin Receptors,Prostaglandin Receptor,Receptor, Prostaglandin,Receptors, Prostaglandins,Prostaglandins Receptors
D002415 Cats The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801) Felis catus,Felis domesticus,Domestic Cats,Felis domestica,Felis sylvestris catus,Cat,Cat, Domestic,Cats, Domestic,Domestic Cat
D003988 Dibenzothiepins
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001488 Basilar Artery The artery formed by the union of the right and left vertebral arteries; it runs from the lower to the upper border of the pons, where it bifurcates into the two posterior cerebral arteries. Arteries, Basilar,Artery, Basilar,Basilar Arteries
D015237 Dinoprost A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions. PGF2,PGF2alpha,Prostaglandin F2,Prostaglandin F2alpha,9alpha,11beta-PGF2,Enzaprost F,Estrofan,PGF2 alpha,Prostaglandin F2 alpha,9alpha,11beta PGF2,F2 alpha, Prostaglandin,F2alpha, Prostaglandin,alpha, PGF2

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