The action of local anaesthetics on lipolysis and on adenosine 3':5'-cyclic monophosphate content in isolated rat fat-cells.

  title={The action of local anaesthetics on lipolysis and on adenosine 3':5'-cyclic monophosphate content in isolated rat fat-cells.},
  author={K. Siddle and C. Hales},
  journal={The Biochemical journal},
  volume={142 2},
1. Local anaesthetics inhibited hormone-stimulated lipolysis in isolated rat fat-cells. The most potent anaesthetic was dibucaine, which inhibited adrenaline-stimulated lipolysis by 50% at a concentration of 0.16mm. 2. The amount of inhibition produced by a given concentration of anaesthetic was very similar with adrenaline, theophylline and dibutyryl cyclic AMP, at submaximal and maximal concentrations. 3. The inhibitory effect of dibucaine on lipolysis was apparent within 5 min and was… Expand
Uncoupling of lipolysis from cyclic AMP by procaine: a tool for studying the mechanism of action of antilipolytic agents.
  • M. D'costa, A. Angel
  • Chemistry, Medicine
  • Canadian journal of physiology and pharmacology
  • 1975
The initial rate of net glycerol release in norepinephrine-stimulated adipose tissue fragments was inhibited by procaine-HCl, whereas basal (unstimulated) lipolysis was unaffected, and the inhibitory effect of clofibrate on cyclic AMP could not be attributed to accumulation of products oflipolysis. Expand
The selective effects of charged local anaesthetics on the glucagon- and fluoride-stimulated adenylate cyclase activity of rat-liver plasma membranes.
The glucagon-stimulated enzyme was initially inhibited by the anionic drugs at low concentrations, then activated, and finally inhibited with increasing drug concentration, but there was no evidence from electron spin resonance studies to suggest that the elevations in activity were due to increases in bilayer fluidity. Expand
Inhibition of catecholamine‐stimulated adenylate cyclase in fat cells by local anaesthetics
In view of the preliminary observation of an inhibition of catecholaminestimulated adenylate cyclase in rat heart by lignocaine, it was of interest to extend this finding to the fat cell system. Expand
Stimulation and inhibition of pancreatic phospholipase A2 by local anesthetics as a result of their interaction with the substrate.
The results are interpreted as to support the view that local anesthetics interfere with pancreatic phospholipase activity by means of interaction with the substrate rather than with the enzyme. Expand
The influence of calcium on the antilipolytic action of propranolol, timolol, labetalol, verapamil, procaine, and papaverine in rat adipocytes.
  • P. Nencini
  • Chemistry, Medicine
  • Pharmacological research communications
  • 1979
Ca +2 seems to play a major role in “non-specific” antilipolytic action of the beta-blocking drugs mentioned, although the available data do not indicate the specific points at which the cation pathways are interfered with. Expand
The effect of local anesthetics on arterial lipid metabolism. Inhibition of sterol esterification in vitro.
  • F. Bell
  • Chemistry, Medicine
  • Atherosclerosis
  • 1981
A detailed study of the effects of 5 mM lidocaine on lipid biosynthesis in the rabbit aorta in vitro revealed that lidocane not only inhibited sterol esterification to [14C]oleate but stimulated [14Csoleate incorporation into glycerides. Expand
Stimulation of glucose transport in rat adipocytes by insulin, adenosine, nicotinic acid and hydrogen peroxide. Role of adenosine 3':5'-cyclic monophosphate.
It is suggested that insulin, H(2)O(2), adenosine and nicotinic acid may all stimulate glucose transport in rat adipocytes by lowering the intracellular cyclic AMP concentration. Expand
Relationship between lipolysis and calcium in epididymal adipose tissue of obese-hyperglycaemic mice
The results suggest that the mechanism promoting45Ca uptake in response to lipolytic agents was beyond cyclic AMP production in the adipose tissue of lean mice, but independent of free fatty acid release. Expand
Effects of benzydamine on the lipolytic system of fat cells.
Benzydamine dose-dependently increased cyclic 3',5'-AMP levels in isolated fat cells and competitively inhibited phosphodiesterase activity and the antilipolytic effect appears to result from the direct inhibition of hormone sensitive triglyceride lipase. Expand
Effect of local anesthetics on sterol biosynthesis and sterol esterification in rat liver in vitro.
A comparison of incorportion patterns from labeled acetate and mevalonates suggest that inhibition of sterologenesis occurs at more than one post-mevalonate step in the pathway. Expand