The role of the 5-HT4 receptor in Cl− secretion in human jejunal mucosa

Budhoo, Misra; Harris, Robert P.; Kellum, John M.

doi:10.1016/s0014-2999(96)00474-8

Cited by 32 publications

(26 citation statements)

References 15 publications

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“…In the study by Gill et al (2005), inhibition of NHE2 and NHE3 activity by 5-HT in Caco-2 cells was largely due to activation of 5-HT 4 receptors. In the present study, by contrast, the 5-HT 4 receptor antagonist GR 113808 (Budhoo et al, 1996) did not change the stimulatory effect of 5-HT. On the other hand, the stimulation in NHE activity by 5-HT in the present study was partially prevented by WAY 100135 (300 nM) and ketanserin (300 nM), antagonists of 5-HT 1A and 5-HT 2 receptors, respectively.…”

Section: Discussioncontrasting

confidence: 91%

“…The next series of experiments were intended to evaluate which type of 5-HT receptor was involved. The stimulation induced by 5-HT was partially inhibited by WAY 100135 (300 nM) and ketanserin (300 nM), antagonists of 5-HT 1A and 5-HT 2 receptors, respectively, but not in the presence of GR 113808 (300 nM), a specific inhibitor of 5-HT 4 receptors (Budhoo et al, 1996) (Fig. 4E).…”

Section: Effect Of 5-ht On Nhe Activitymentioning

confidence: 94%

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Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

2007

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Section: Discussioncontrasting

confidence: 91%

Section: Effect Of 5-ht On Nhe Activitymentioning

confidence: 94%

Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

2007

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“…In the gastric area, contractile 5-HT 4 receptors have been found on the cholinergic nerves in the guinea-pig (Buchheit & Buhl, 1994), dog (Bingham et al, 1995) and, based on preliminary data, man (Schuurkes et al, 1991). In the small intestine, 5-HT 4 receptors mediate mucosal secretion (Budhoo et al, 1996) and smooth muscle relaxation (Kuemmerle et al, 1995). Coming down to the large intestine, 5-HT 4 receptors were found on circular smooth muscle, mediating relaxation (Meulemans et al, 1995;McLean et al, 1995;Tam et al, 1994;Prins et al, 2000), and on the mucosa mediating secretion (Borman & Burleigh, 1996).…”

Section: Introductionmentioning

confidence: 99%

5‐HT₄ receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle

Prins

Akkermans

Lefebvre

et al. 2000

British J Pharmacology

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1 5-HT 4 receptors mediate circular muscle relaxation in both human and canine large intestine, but this phenomenon alone can not explain the improvement in colonic motility induced by selective 5-HT 4 receptor agonists in vivo. We set out to characterize 5-HT 4 receptor-mediated e ects in longitudinal muscle strips of canine and human large intestine. 2 Electrical ®eld stimulation (EFS) was applied providing submaximal isotonic contractions. L-NOARG (0.1 mM) was continuously present in the organ bath to preclude nitric oxide-induced relaxation to EFS. 3 The selective 5-HT 4 receptor agonist prucalopride (0.3 mM) enhanced EFS-evoked contractions, that were antagonized in both preparations by the selective 5-HT 4 receptor antagonist GR 113808 (0.1 mM). The prucalopride-induced increase was present in canine ascending and descending colon, but absent in rectum. Regional di erences in response to prucalopride were not observed in human ascending and sigmoid colon and rectum. Incubation with atropine (1 mM) or tetrodotoxin (0.3 mM) inhibited EFS-induced contractions, which were then una ected by prucalopride (0.3 mM) in both tissues. 4 In the presence of methysergide (3 mM; both tissues) and granisetron (0.3 mM; only human tissues), 5-HT (0.3 mM) enhanced EFS-induced contractions, an e ect that was antagonized by GR 113808 (0.1 mM). In the presence of atropine or tetrodotoxin, EFS-induced contractions were inhibited, leaving 5-HT (0.3 mM) ine ective in both preparations. 5 This study demonstrates for the ®rst time that in human and canine large intestine, 5-HT 4 receptors are located on cholinergic neurones, presumably mediating facilitating release of acetylcholine, resulting in enhanced longitudinal muscle contractility. This study and previous circular muscle strip studies suggest that 5-HT 4 receptor agonism facilitates colonic propulsion via a coordinated combination of inhibition of circumferential resistance and enhancement of longitudinal muscle contractility.

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“…However, the existence of 5-HT 4 receptors has been demonstrated in the gut (40). In the small intestine, 5-HT 4 receptors mediate mucosal secretion and smooth muscle relaxation (41,42). Furthermore, the 5-HT 4 receptor has an established role in mediating contraction responses via a cholinergic mechanism in the guinea-pig intestine and colon (14,43).…”

Section: Discussionmentioning

confidence: 99%

The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine

2014

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Background:The main source of 5-HT in body is in enterchromafin cells of intestine, different studies mentioned different roles for endogenous 5-HT and receptors involved and it is not clearified the mechanism of action of endogenous 5-HT. Objectives: To study the role of endogenous 5-HT on modulation of contraction and relaxation responses induced by electrical field stimulation (EFS) in different regions of the rat intestine. Materials and Methods: Segments taken from the rat duodenum, jejunum, mid and terminal ileum were vertically mounted, connected to a transducer and exposed to EFS with different frequencies in the absence and presence of various inhibitors of enteric mediators i. e. specific 5-HT receptor antagonists. Results: EFS-induced responses were sensitive to TTX and partly to atropine, indicating a major neuronal involvement and a cholinergic system. Pre-treatment with WAY100635 (a 5-HT 1A receptor antagonist) and granisetron up to 10.0 µM, GR113808 (a 5-HT 4 receptor antagonist), methysergide and ritanserin up to 1.0 µM, failed to modify responses to EFS inall examined tissues. In the presence of SB258585 1.0 µM (a 5-HT 6 receptor antagonist) there was a trend to enhance contraction in the proximal part of the intestine and reduce contraction in the distal part. Pre-treatment with SB269970A 1.0 µM (5-HT 7 receptor antagonist) induced a greater contractile response to EFS at 0.4 Hz only in the duodenum. Conclusions:The application of 5-HT 1A , 5-HT 2 , 5-HT 3 , 5-HT 4 , 5-HT 6 and 5-HT 7 receptor antagonists, applied at concentrations lower than 1.0 µM did not modify the EFS-induced contraction and relaxation responses, whichsuggests the unlikely involvement of endogenous 5-HT in mediating responses to EFS in the described test conditions.

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The role of the 5-HT4 receptor in Cl− secretion in human jejunal mucosa

Cited by 32 publications

References 15 publications

Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

5‐HT₄ receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle

The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine

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The role of the 5-HT4 receptor in Cl− secretion in human jejunal mucosa

Cited by 32 publications

References 15 publications

Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

Short-term effect on intestinal epithelial Na+/H+ exchanger by Giα1,2-coupled 5-HT1A and Gq/11-coupled 5-HT2 receptors

5‐HT4 receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle

The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine

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Product

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5‐HT₄ receptors on cholinergic nerves involved in contractility of canine and human large intestine longitudinal muscle