Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.4.1 (phosphodiesterase)
 18,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Carbenoxolone slightly but significantly decreased the release of FFA from rat epididymal fat pads. The antilipolytic action of carbenoxolone was not blocked by 10(-3)M 3-isobutyl-1-methylxanthine, a potent inhibitor of phosphodiesterase. The findings suggest that carbenoxolone exerts its antilipolytic activity by acting on adenylate cyclase, thereby decreasing cyclic AMP concentrations and the activity of the hormone-sensitive lipase in adipose tissue.
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PMID:Effect of carbenoxolone on lipolysis in rat adipose tissue. 2 44

1. The interactions between carbenoxolone and nitric oxide (NO) were examined by investigating their effects on human platelet aggregation, on rat aortic strips precontracted by phenylephrine and on protection of rat gastric mucosa against ethanol-induced injury. 2. Carbenoxolone (100-300 microM) caused a significant and concentration-dependent potentiation of rat peritoneal neutrophil (RPN)- 3-morpholino-syndnonimine (SIN-1)- or iloprost-induced inhibition of platelet aggregation. Higher concentrations (500 microM) of carbenoxolone alone markedly inhibited platelet aggregation. Pretreatment with carbenoxolone (100-300 microM) antagonized the reversal of the RPN- or SIN-1-induced antiaggregatory effect by oxyhaemoglobin (10 microM). 3. Rat aortic strips with intact endothelium precontracted by phenylephrine (0.1-0.3 microM) were relaxed by carbenoxolone (100-300 microM) in a concentration-dependent manner. Relaxations were abolished by mechanical removal of the endothelium or by incubation with methylene blue (10 microM) or NG-nitro-L-arginine (L-NNA, 100 microM). Sodium nitroprusside (10 nM)-induced relaxations of endothelium-denuded rat aortic strips were potentiated by carbenoxolone (100 microM). . The carbenoxolone (200 mg kg-1, p.o.)-induced gastroprotection against ethanol was antagonized by L-NNA (5-40 mg kg-1) in a dose-dependent manner. Pretreatment of rats with indomethacin (10 mg kg-1, s.c.) increased the effect of L-NNA. 5. The results suggest that the activity of carbenoxolone in the experimental systems tested is due to phosphodiesterase inhibition, although radical scavenging properties of the drug could contribute to some of the effects observed. In the rat gastric mucosa both increased prostaglandin levels and effects on the NO system could contribute to the protective action of carbenoxolone.
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PMID:Effect of carbenoxolone on the biological activity of nitric oxide: relation to gastroprotection. 172 64

1. The effects of carbenoxolone on duodenal HCO3- secretion were examined in anesthetized rats and compared with those of prostaglandin E2 (PGE2). 2. After 18-hr fasting, the duodenal loop (1.7 cm) that was made between the pyloric ring and the area just proximal to the outlet of the common bile duct was perfused with saline (pH 4.5), the pH of perfusate and the transmucosal potential difference (PD) were continuously monitored and HCO3- output was determined by titration with 10 mM HCl. 3. Under these conditions, duodenal pH, PD, and HCO3- secretion were increased in response to PGE2 (0.3 and 1.0 mg/kg) given intravenously as a single injection. Carbenoxolone (0.1-1.0 mg/kg, intravenously) also caused an increase in duodenal pH and HCO3- output in a dose-dependent manner, with a concomitant rise in PD; at 1 mg/kg, the magnitude of HCO3- output was almost equivalent to that induced by PGE2 at 0.3 mg/kg. 4. Prior administration of indomethacin, a cyclooxygenase inhibitor (5 mg/kg, subcutaneously), did not affect the HCO3- stimulatory action of carbenoxolone or PGE2. 5. Duodenal HCO3- secretion was also increased by intravenous injection of dibutylyl adenosine 3',5'-cyclic monophosphate (dbcAMP) but not by isobutylmethyl xanthine (IBMX; 10 mg/kg), an inhibitor of phosphodiesterase, but the former action was significantly potentiated in the presence of IBMX. Likewise, the pretreatment of IBMX significantly enhanced the HCO3- stimulatory action of PGE2 but had no effect on the HCO3- response induced by carbenoxolone. 6. These results suggest that carbenoxolone stimulates duodenal HCO3- secretion in rats, similar to PGE2 and this mechanism does not involve endogenous prostaglandins and is not associated with the intracellular accumulation of cAMP.
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PMID:Stimulation of duodenal bicarbonate secretion by carbenoxolone in rats: a comparative study with prostaglandin E2. 955 27