Effect of 4-aminoantipyrine on gastric compliance and liquid emptying in rats

-Context -Gamma-aminobutyric acid (GABA) is a potent inhibitory neurotransmitter. There is evidence that GABA B receptors located in the dorsal complex and in afferent fibers of the vagus nerve participate in the control of gastrointestinal motility. Objectives -To assess the intracerebroventricularly (ICV) and intravenously (IV) effect of baclofen, a GABA B receptor agonist, on liquid and solid gastric emptying in rats. Methods -Adult male Wistar rats weighing 250-300 g (n = 6-8 animals) were used. Gastric emptying of liquid test meals labeled with phenol red was evaluated by the determination of percent gastric retention (%GR) 10 and 15 min after orogastric administration of saline and 10% glucose meals, respectively. Baclofen was injected ICV (1 and 2 mg/animal) through a tube implanted into the lateral ventricle of the brain and was injected IV (1 and 2 mg/kg) into a tail vein. The gastric emptying of liquid was determined 10 or 30 min after ICV and IV baclofen administration, respectively. The gastric emptying of the solid meal was assessed by the determination of percent gastric retention 2 h after the beginning of the ingestion of the habitual ratio by the animal, consumed over a period of 30 min. Baclofen was administered ICV (1 and 2 mg/animal) or IV (1 and 2 mg/kg) immediately after the end of the ingestion of the solid meal. The control groups received vehicle (sterile saline solution) ICV or IV.Results -The group of animals receiving baclofen ICV (2 mg/animal) presented a significantly lower (P<0.05, Tukey test) %GR (mean ± SEM) of the saline (18.1 ± 2.5%) compared to control (33.2 ± 2.2%). In the group receiving the drug IV, the gastric retention of the same test meal did not differ from control. ICV and IV administration of baclofen had no effect on the gastric emptying of the 10% glucose solution compared to control. ICV administration of 1 or 2 mg baclofen/animal significantly increased the gastric retention of the solid test meal (57.9 ± 6.5% and 66.6 ± 6.3%, respectively) compared to control (35.1 ± 4.4%). The same phenomenon was observed only with the IV dose of 2 mg/kg (71.9 ± 2.6%) compared to control (52.7 ± 2.8%). Conclusions -Baclofen administered: 1. ICV (2 mg/animal), but not IV, increased gastric emptying of a non-caloric isotonic liquid test meal (saline); 2. when administered ICV or IV, it had no effect of gastric emptying of a 10% glucose solution; 3) when administered ICV (1 and 2 mg/animal) and IV (2 mg/kg) it delayed the gastric emptying of the solid meal. HEADINGS -Gastric emptying. Baclofen. Rats.

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“…No change, or only a slight but significant increased in GE of this test meal was observed in control animals (12,39,42) .…”

Section: Arq Gastroenterol 291 V 47 -No3 -Jul/set 2010mentioning

confidence: 69%

Effect of baclofen on liquid and solid gastric emptying in rats

Collares

Vinagre

2010

Arq. Gastroenterol.

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“…Section of afferent and efferent fibers by subdiaphragmatic vagotomy abolished the effect of these drugs (1,3,4). Cholecystokinin (CCK) activates the CCK 1 receptors on the Cps-sensitive vagal afferent nerve endings of the intestine and participates in the mechanism of GE control (11,12).…”

Section: Discussionmentioning

confidence: 99%

“…The GE study was conducted on these animals at the age of 8/9 weeks when they weighed 200-300 g. Ten minutes before the study of GE the two groups were treated iv with equivalent doses of 240 μmol/kg Dp (80 mg/kg), AA (48.77 mg/kg), At (45.17 mg/kg), or saline, as described in previous studies (1)(2)(3)(4).…”

Section: Methodsmentioning

confidence: 99%

“…The phenylpyrazolone derivatives dipyrone (Dp), 4-aminoantipyrine (AA) and antipyrine (At) administered intravenously (iv; 240 μmol/kg) delay the gastric emptying (GE) of a saline test meal in rats (1)(2)(3)(4). Taken together, these studies suggest the participation of the central nervous system (CNS) and of the vagus nerve in the phenomenon.…”

Section: Introductionmentioning

confidence: 98%

“…Taken together, these studies suggest the participation of the central nervous system (CNS) and of the vagus nerve in the phenomenon. Considering that among the three drugs only Dp induced the same effect when the drugs were administered intracerebroventricularly (icv, 4 μmol/animal) and the delay in GE induced by these drugs administered iv was abolished by subdiaphragmatic vagotomy (1,3,4), it is possible that the inhibitory stimulus of a drug administered iv on GE reaches the CNS through peripheral afferent pathways.…”

Section: Introductionmentioning

confidence: 99%

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Phenylpyrazolone derivatives inhibit gastric emptying in rats by a capsaicin-sensitive afferent pathway

Vinagre

Collares

2009

Braz J Med Biol Res

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Dipyrone (Dp), 4-aminoantipyrine (AA) and antipyrine (At) administered iv and Dp administered icv delay gastric emptying (GE) in rats. The participation of capsaicin (Cps)-sensitive afferent fibers in this phenomenon was evaluated. Male Wistar rats were pretreated sc with Cps (50 mg/kg) or vehicle between the first and second day of life and both groups were submitted to the eye-wiping test. GE was determined in these animals at the age of 8/9 weeks (weight: 200-300 g). Ten minutes before the study, the animals of both groups were treated iv with Dp, AA or At (240 μmol/kg), or saline; or treated icv with Dp (4 μmol/animal) or saline. GE was determined 10 min after treatment by measuring % gastric retention (GR) of saline labeled with phenol red 10 min after orogastric administration. Percent GR (mean ± SEM, N = 8) in animals pretreated with Cps and treated with Dp, AA or At (35.8 ± 3.2, 35.4 ± 2.2, and 35.6 ± 2%, respectively) did not differ from the GR of saline-treated animals pretreated with vehicle (36.8 ± 2.8%) and was significantly lower than in animals pretreated with vehicle and treated with the drugs (52.1 ± 2.8, 66.2 ± 4, and 55.8 ± 3%, respectively). The effect of icv administration of Dp (N = 6) was not modified by pretreatment with Cps (63.3 ± 5.7%) compared to Dp-treated animals pretreated with vehicle (62.3 ± 2.4%). The results suggest the participation of capsaicin-sensitive afferent fibers in the delayed GE induced by iv administration of Dp, AA and At, but not of icv Dp

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Spectroscopic Investigation on the Toxicological Interactions of 4-aminoantipyrine with Bovine Hemoglobin

et al. 2009

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The effects of 4-aminoantipyrine (AAP) on bovine hemoglobin (BHb) were investigated by fluorescence spectroscopy, synchronous fluorescence spectroscopy, ultraviolet-visible absorption spectroscopy and circular dichroism spectroscopy (CD) under simulated physiological conditions. The experimental results showed that AAP effectively quenched the intrinsic fluorescence of BHb via static quenching. The number of binding sites, the binding constant K(a), and the thermodynamic parameters (DeltaH(o), DeltaS(o) and DeltaG(o)) were measured at two different temperatures. Van der Waals' interactions and hydrogen bonds were the predominant intermolecular forces in stabilizing the BHb-AAP complex. The experiment results confirmed micro-environmental and conformational changes of BHb in the presence of AAP. The alpha-helix content decreased, indicating that AAP destroys some of the hydrogen bonding networks in the polypeptide chain.

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Effect of 4-aminoantipyrine on gastric compliance and liquid emptying in rats

Cited by 18 publications

References 16 publications

Effect of baclofen on liquid and solid gastric emptying in rats

Effect of baclofen on liquid and solid gastric emptying in rats

Phenylpyrazolone derivatives inhibit gastric emptying in rats by a capsaicin-sensitive afferent pathway

Spectroscopic Investigation on the Toxicological Interactions of 4-aminoantipyrine with Bovine Hemoglobin

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