Characterisation of α2-adrenoceptor subtypes involved in gastric emptying, gastric motility and gastric mucosal defence

Fülöp, Katalin; Zádori, Zoltán; Rónai, András Z.; Gyires, Klára

doi:10.1016/j.ejphar.2005.10.025

Cited by 52 publications

(30 citation statements)

References 48 publications

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“…We demonstrated that clonidine and rilmenidine, when given either peripherally (per os, subcutaneously) or centrally (i.c.v. ), inhibited potently the direct necrotizing action of acidified ethanol on gastric mucosa in both rats and mice [12][13][14][15][16][17]. Our results also showed that the site of action is presumably within the CNS [16,17], where the activation of α2B-and α2C-ARs initiates a chain of events resulting in vagally mediated release of mucosal protective factors, such as prostaglandins and nitric oxide [13,16].…”

Section: It Is Well-established That Peptic Ulcers Develop As a Resusupporting

confidence: 53%

“…More importantly, our results clearly showed that this protective effect is mediated by α2B-and α2C-ARs localized in the brain, most probably in the dorsal vagal complex, and α2A-ARs do not have any significant role in it [12,14,17]. Accordingly, we proposed that selective α2B/C-AR agonists may represent a novel group of gastroprotective agents, which are devoid of several side effects mediated by the α2A-AR subtype, such as hypotension, bradycardia or sedation [17].…”

Section: Introductionmentioning

confidence: 54%

“…In the last two decades our research group demonstrated that α2-AR agonists induce a potent defensive effect in the stomach and reduce the extent of mucosal injury in both aciddependent (indomethacin) and independent (ethanol) ulcer models [12][13][14][15][16][17]. More importantly, our results clearly showed that this protective effect is mediated by α2B-and α2C-ARs localized in the brain, most probably in the dorsal vagal complex, and α2A-ARs do not have any significant role in it [12,14,17].…”

Section: Introductionmentioning

confidence: 99%

“…Due to all these actions α2-ARs are considered attractive therapeutic targets for the treatment of a wide range of GI disorders, including functional dyspepsia, irritable bowel syndrome and inflammatory bowel diseases [7,11]. However, most GI effects are mediated mainly by the α2A-AR subtype [4,7,12], and pharmacologic modulation of this subtype in the above mentioned diseases by non-selective or subtype-selective α2-AR ligands may result in numerous undesirable side effects outside the GI tract (see above).…”

Section: Introductionmentioning

confidence: 99%

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Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility

et al. 2016

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Background. Allyphenyline, a novel α2-adrenoceptor (AR) ligand has been shown to selectively activate α2C-adrenoceptors (AR) and 5HT1A receptors, but also to behave as a neutral antagonist of α2A-ARs. We exploited this unique pharmacological profile to analyze the role of α2C-ARs and 5HT1A receptors in the regulation of gastric mucosal integrity and gastrointestinal motility. Methods. Similar inhibition was observed in the colon, however, in this case only ARC 239 reduced this effect, while neither selective inhibition of α2C-ARs and 5HT1A receptors, nor genetic deletion of α2A-and α2B-ARs influenced it. Conclusions. Activation of both central α2C-ARs and 5HT1A receptors contributes to the gastroprotective action of allyphenyline in rats. Its inhibitory effect on fundic contractions is mediated by 5HT1A receptors, but neither α2-ARs, nor 5HT1A receptors take part in its inhibitory effect on colonic contractility in mice.

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Section: It Is Well-established That Peptic Ulcers Develop As a Resusupporting

confidence: 53%

Section: Introductionmentioning

confidence: 54%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility

et al. 2016

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“…24,25 In the present study, we showed that the pretreatment of clonidine significantly reduced motility of the gastric antrum, that is keeping with the previous observations. 26,27 Hypomotility was observed both in the preprandial and postprandial periods. The gastroprokinetic activity of prokinetics may be different among experimental models of gastric dysfunction.…”

Section: Discussionmentioning

confidence: 99%

Effect of DA-9701 on the Normal Motility and Clonidine-induced Hypomotility of the Gastric Antrum in Rats

Kang

Han

Kim

et al. 2016

J Neurogastroenterol Motil

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Background/AimsDA-9701 is a novel prokinetic agent. In the present study, we investigated the effect of DA-9701 on the motility of the gastric antrum in the normal and clonidine-induced hypomotility in an in vivo animal model. MethodsA strain gauge force transducer was sutured on the gastric antrum to measure the contractile activity in rats. A total of 28 rats were subclassified into the 4 groups: (1) the placebo group, (2) the DA-9701 group, (3) the placebo group in the clonidine-pretreated rats, and (4) the DA-9701 group in the clonidine-pretreated rats. After the basal recording, either placebo (3% [w/v] hydroxypropylmethyl cellulose) or DA-9701 was administered. Contractile signals were measured after the administration and after a meal. In the clonidinepretreated rats, either placebo or DA-9701 was administered. Contractile signals were measured after the administration and after a meal. ResultsOral administration of DA-9701 did not significantly alter the motility index of the gastric antrum in the preprandial and postprandial periods, compared with the placebo group. The administration of clonidine decreased the motility index of the gastric antrum in the preprandial and postprandial periods, compared with the administration of placebo. This reduction of the antral motility by the administration of clonidine was not observed in the clonidine-pretreated DA-9701 group. The percentage of the motility index in the postprandial period was significantly greater in the clonidine-pretreated DA-9701 group, compared with the clonidine-pretreated placebo group. Conclusions

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In Vivo Measurement of Intragastric Pressure with a Rubber Balloon in the Anesthetized Rat

Zádori

Gyires

2013

CP Toxicology

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Abstract:The protocols described in this unit are designed to measure the intragastric pressure in anaesthetized rats by a water-filled low-compliance rubber balloon. The balloon is introduced into the stomach either orally (by passing the balloon down the esophagus) or directly via a small incision of the fundus after laparotomy. The effects of both stimulatory (e.g. carbachol) and inhibitory (e.g. oxymetazoline) agents can be evaluated on the gastric tone and phasic contractions. The model allows the evaluation of dose-response curves and also the time-course of the effects. Furthermore, by combining centrally or peripherally acting agents the site of action can also be determined. John Wiley & Sons Current ProtocolsIn vivo measurement of intragastric pressure with a rubber balloon in the anaesthetized rat 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 AbstractThe protocols described in this unit are designed to measure the intragastric pressure in anaesthetized rats by a water-filled low-compliance rubber balloon. The balloon is introduced into the stomach either orally (by passing the balloon down the esophagus) or directly via a small incision of the fundus after laparotomy. The effects of both stimulatory (e.g. carbachol) and inhibitory (e.g. oxymetazoline) agents can be evaluated on the gastric tone and phasic contractions. The model allows the evaluation of dose-response curves and also the timecourse of the effects. Furthermore, by combining centrally or peripherally acting agents the site of action can also be determined.

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Characterisation of α2-adrenoceptor subtypes involved in gastric emptying, gastric motility and gastric mucosal defence

Cited by 52 publications

References 48 publications

Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility

Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility

Effect of DA-9701 on the Normal Motility and Clonidine-induced Hypomotility of the Gastric Antrum in Rats

In Vivo Measurement of Intragastric Pressure with a Rubber Balloon in the Anesthetized Rat

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