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Department of Physiology and Pharmacology (S.J.H.), Medical School, Queen’s Medical Centre, Nottingham, England; Department of Chemistry (C.R.G.), University College London, Christopher Ingold Laboratories, London, England; Department of Pharmacochemistry (H.T.), Leiden/Amsterdam Center for Drug Research, Vrije Universiteit, Amsterdam, The Netherlands;(More)
Application of arachidonic acid (AA) (0.1-4 mg) to the ears of mice produces immediate vasodilatation and erythema (5 min) followed by the abrupt development of edema which is maximal at 40-60 min. The onset of edema coincides with extravasation of protein and leukocytes. After 1 h, the edema begins to wane rapidly and the inflammatory cells leave the(More)
When freshly drawn, heparinized human whole blood is incubated with 50μM calcium ionophore A23187, platelets are stimulated to produce thromboxane B2 (TxB2) by activation of prostaglandin G/H synthase-1 (PGHS-1). TxB2 concentration, as measured by immunoassay, is maximal at 20–30 min and declines thereafter. Addition of acetylsalicylic acid (IC50=2.8μM) or(More)
1 The synthesis of tritium labelled propylbenzilylcholine mustard ([(3)H]-PrBCM; N-2'-chloroethyl-N-[2'', 3''-(3)H(2)] propyl-2-aminoethyl benzilate) is described.2 The uptake by muscle strips was measured and shown to be considerably increased by previous immersion of the muscle in distilled water.3 A considerable part of the uptake is inhibited(More)
The utilization of circulating maltose was compared to that of glucose in six normal fasting subjects after intravenous injection of 25 g of either sugar. Blood samples were obtained over a 2 hr period and were assayed for free fatty acids (FFA), insulin, glucose, and total reducing substances. Urine was collected for 2 hr after maltose administration and(More)
The temporal patterns of edema and accumulation of the PMN marker enzyme, myeloperoxidase (MPO), were examined following application of tetradecanoylphorbol acetate (TPA) to mouse ears. After application of 2.5 μg TPA, edema peaked at 6 hr, while MPO activity peaked at 24 hr. Pharmacological agents with defined mechanisms of action, delivered orally or(More)
The release of [3H]GABA from slices of rat substantia nigra pars reticulata induced by increasing extracellular K+ from 6 to 15 mM in the presence of 10 microM sulpiride was inhibited by 73 +/- 3% by 1 microM SCH 23390, consistent with a large component of release dependent upon D1 receptor activation. The histamine H3 receptor-selective agonist immepip (1(More)
The extent of the promethazine-sensitive binding of [3H]mepyramine to a washed fraction from guinea pig cerebellum was little altered between 4 degrees and 30 degrees. The dissociation of [3H]mepyramine from the H1 receptor was markedly temperature-sensitive. An Arrhenius plot of the variation of the dissociation rate constant, k-1, with temperature was(More)
1. A study was made of the regulation of [(3)H]-gamma-aminobutyric acid ([(3)H]-GABA) release from slices of rat striatum by endogenous dopamine and exogenous histamine and a histamine H(3)-agonist. Depolarization-induced release of [(3)H]-GABA was Ca(2+)-dependent and was increased in the presence of the dopamine D(2) receptor family antagonist, sulpiride(More)