Effects of local anaesthetics on phospholipases

Kunze, H.; Nahas, Nabeel; Traynor, John R.; Wurl, Michael

doi:10.1016/0005-2760(76)90284-8

Cited by 131 publications

(36 citation statements)

References 16 publications

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“…Mepacrine, chlorpromazine and procaine have previously been reported to inhibit phospholipase, (Vargaftig & Dao Hai, 1972;Kunze, Nahas, Traynor & Wurl, 1976;Flower & Blackwell, 1976). In these experiments the decreasing order of activity was mepacrine > chlorpromazine > procaine.…”

Section: Resultsmentioning

confidence: 61%

PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

Blackwell

Flower

Nijkamp

et al. 1978

British J Pharmacology

303

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1 A simple double-isotope assay for phospholipase A2 activity of perfused organs is described. 2 Guinea-pig lungs perfused through the pulmonary circulation exhibit a low background enzyme activity. This activity is blocked by dexamethasone, betamethasone and hydrocortisone, mepacrine, procaine or chlorpromazine. Aspirin and indomethacin are without effect. 3 Mechanical trauma, antigen challenge or injections of bradykinin, rabbit aorta contracting substance-releasing factor (RCS-RF) or histamine increase 'basal' phospholipase activity. The effect of these agents, except that of bradykinin, is blocked by dexamethasone or mepacrine. 4 The blocking effect of steroids is cumulative and dose-dependent. They do not work in cell-free systems. Inhibition by mepacrine is rapid and is effective in cell-free lung homogenates. 5 It is suggested that agents which liberate prostaglandin endoperoxides and thromboxane A2 from perfused lungs do so by activating phospholipase A2.

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Section: Resultsmentioning

confidence: 61%

PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

Blackwell

Flower

Nijkamp

et al. 1978

British J Pharmacology

303

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“…The local anaesthetic causes relaxations (Altura & Altura, 1974;Wang & Jackson, 1988;Perlmutter, 1990) and, in some preparations, contractions (mainly in venous smooth muscles: Altura & Altura, 1974;Johns et al, 1985;Monuszko et at., .1989). Although inhibition of myosin light-chane kinase (Nosaka et al, 1989) and phospholipase A2 (Kunze et al, 1976;Willman & Hendrickson, 1978), and antagonistic effects on movement of calcium ions (Josephson & Sperelakis, 1976) in smooth muscle by lignocaine have been reported, local anaesthetics are generally believed to induce nonspecific inhibition of vascular tone (Altura & Altura, 1974).…”

Section: Discussionmentioning

confidence: 99%

Vasorelaxant effect of mexiletine in mesenteric resistance arteries of rats

Dohi

Kojima

Sato

1994

British J Pharmacology

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1 The vascular action of mexiletine, a class Ib antiarrhythmic agent, was investigated in the mesenteric resistance arteries of rats. 2 The second order branch of the mesenteric artery was cut into rings and changes in isometric tension were recorded.3 Mexiletine (10-6 10-1 M) evoked concentration-dependent, endothelium-independent relaxations in arteries contracted with noradrenaline. 4 Mexiletine (10-4 M) did not affect the contraction induced by noradrenaline in Ca2"-free solution, while the compound inhibited the contraction induced by CaCl2 in noradrenaline-activated arteries. 5 The relaxation induced by mexiletine was less pronounced in arteries contracted with high KCl than in those contracted with noradrenaline. 6 Mexiletine induced identical relaxations in arteries contracted with noradrenaline in high KCl solution containing verapamil and in Krebs solution. 7 Thus, mexiletine induces relaxations by inhibiting transmembrane Ca2' movement, but not Ca2' release from the intracellular store site in mesenteric resistance arteries of rats. It is speculated that mexiletine possesses greater inhibitory effects against noradrenaline-activated, verapamil-insensitive (receptor-operated) Ca2+ channels than against verapamil-sensitive (voltage-dependent) channels.

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“…The drugs employed here were kindly supplied by Bayer (Leverkusen). Synthesis of radioactive substrates was performed as described in [4]. 1 -Acyl-2-[ 1-14C]lino1eoyl-sn-glycero-3-phosphorylethanolamine had a specific activity of 2214 dpm/nmol, 1-[l-'4C]palmitoyl-2-acyl-snglycero-3-phosphorylethanolamine of 2617 dpm/ nmol, and I-[ 1 -14C]palmitoyl-sn-glycero-3-phosphorylethanolamine of 2055 dpm/nmol.…”

Section: Substancesmentioning

confidence: 99%

“…Lactate dehydrogenase (EC 1.1.1.27) was measured according to Johnson [6], glucosedphosphatase (EC 3.1.3.9) according to Swanson [7], galactosyltransferase (EC 2.4.1.38) according to Beaufay et al [8], monoamine oxidase (EC 1.4.3.4) according to Wurthman and Axelrod [9], cytochrome-c oxidase (EC 1.9.3.1) according to Leighton et Phospholipase Al (EC 3.1.1.32), A2 (EC 3.1.1.4) and C (EC 3.1.4.3) activities were measured as in [4,11]. The standard incubation media contained 25 mM sodium acetate buffer (pH 4.7), various amounts of protein (subcellular fractions) and 30-55 ,uM sonicated radioactive phosphatidylethanolamine substrate in a total volume of 250 ~1.…”

Section: Enzymesmentioning

confidence: 99%

“…Blanks without enzyme were included in each experiment. Determination of hydrolytic activities was performed after thin-layer chromatography of the lipid extracts in order to separate the products (fatty acids and lysophosphatidylethanolamine) from the phosphatidylethanolamine substrate [4,18]. For analysis of di-and monoacylglycerols, the lipid extract was chromatographed on borateimpregnated silica gel H thin-layer plates with petroleum ether/diethyl ether/methanol/formic acid (60: 40: 1.5 : 1.6, by vol.).…”

Section: Enzymesmentioning

confidence: 99%

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Fractionation, biochemical characterization and lysosomal phospholipases of human liver

Löffler

Kunze

1987

FEBS Letters

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Human liver was homogenised and fractionated by differential centrifugation, and the s&cellular fractions were characterised biochemically. Absolute values and distribution patterns of protein and marker enzyme activities obtained from human liver have also heen compared with those from rat liver. In addition, acid phospholipase activities have been studied in human liver. On the basis of product formation from stereospecifically radiolaheled phosphatidylethanolamine substrates, lysosomal phospholipases A, and A, with optimal activities at pH 4.7 have heen identified in human liver. Acid phospholipase C and lysophospholipase activities, however, were not found in human liver. Cationic amphiphilic drugs inhibited the activities of the acid phospholipases A in human and rat liver lysosomes to about the same extent.

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Effects of local anaesthetics on phospholipases

Cited by 131 publications

References 16 publications

PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

Vasorelaxant effect of mexiletine in mesenteric resistance arteries of rats

Fractionation, biochemical characterization and lysosomal phospholipases of human liver

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Effects of local anaesthetics on phospholipases

Cited by 131 publications

References 16 publications

PHOSPHOLIPASE A2 ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

PHOSPHOLIPASE A2 ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

Vasorelaxant effect of mexiletine in mesenteric resistance arteries of rats

Fractionation, biochemical characterization and lysosomal phospholipases of human liver

Contact Info

Product

Resources

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PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS

PHOSPHOLIPASE A₂ ACTIVITY OF GUINEA‐PIG ISOLATED PERFUSED LUNGS: STIMULATION, AND INHIBITION BY ANTI‐INFLAMMATORY STEROIDS