Role of 5-HT<sub>1B/D</sub> receptors in canine gastric accommodation:  effect of sumatriptan and 5-HT<sub>1B/D</sub> receptor antagonists

Ponti, Fabrizio De; Crema, Francesca; Moro, Elisabetta; Nardelli, G.; Frigo, Gianmario; Crema, A.

doi:10.1152/ajpgi.00280.2002

Cited by 26 publications

(25 citation statements)

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“…30,31) It appears that stimulation of the 5-HT 1B receptor has a relaxation effect on gastric tone in dogs since the antimigraine 5-HT 1B/D receptor agonist sumatriptan induces an immediate gastric relaxation and gastric accommodation mediated by 5-HT 1B receptors. 19) The gastric barostat technique is the most common method for measuring gastric compliance and accommodation in both humans and animals. Corydaline induced gastric accommodation at a dose of 1 mg/kg but had no measurable effect on gastric tone.…”

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“…19) Five female Beagle dogs (7-9 kg) were operated on under general anesthesia with Tiletamine/Zolazepam (Zoletil ® , Virbac Laboratories, Carros, France; i.v., 10 mg/kg). A chronic gastric fistula was inserted via a midline laparotomy in the larger curvature of the stomach between the glandular portion and forestomach and was exteriorized through the anterior aspect of the abdomen.…”

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Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Lee

Son

Kim

2010

Biological & Pharmaceutical Bulletin

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Functional dyspepsia (FD) is a highly prevalent chronic gastrointestinal (GI) disorder that causes a considerable burden to both the patient and society. Although the etiology and pathogenesis of FD are poorly understood, FD is associated with pathophysiologic abnormalities including delayed gastric emptying (GE), impaired gastric accommodation, and visceral hypersensitivity.1,2) Delayed GE has been reported in 30-40% of FD patients, 3) and a number of studies have demonstrated impaired gastric accommodation after meals in approximately 40% of patients. 4) Given these results, we hypothesized that GE of a semi-solid meal, GI transit, and gastric accommodation would be suitable markers for evaluating motor effects in animal models.Corydalis tubers, the roots of Corydalis yahusuo W.T. WANG (Papaveraceae), have long been used as herbal medicine for their analgesic and anti-ulcer effects. It has been reported that Corydalis tuber extracts exhibit several biological activities, acting as both an anti-spasmodic agent in the GI tract and as an analgesic. [5][6][7][8] Previous phytochemical studies reported that Corydalis tubers are made up primarily of alkaloid compounds including corydaline, berberine, protopine, and palmatine. [8][9][10][11][12] These alkaloid compounds are reported to provide the analgesic, anti-spasmodic, and anti-acetylcholinesterase activities associated with Corydalis tubers. Of these compounds, corydaline is considered the marker compound for quality control of Corydalis extract; however, the pharmacological effects of corydaline on GI motor function have not yet been studied.We previously investigated the prokinetic activities of corydaline to determine its potential bioactivity in FD and elucidated the basis of the selection of corydaline as the principal marker compound for quality control. 13) In the present study, we evaluated the effects of corydaline on GE and GI transit in rats and gastric accommodation in conscious dogs. MATERIALS AND METHODS Plant MaterialPlant material was commercially purchased at Kyungdong herbal market (Seoul, Korea) and identified by Dr. S. Choi at the Research Center of Dong-A Pharm. Co., Ltd. (Yongin-si, Korea). A voucher specimen has been deposited in our laboratory at Kyung Hee University.Extraction and Isolation Dried Corydalis tuber (30 kg) was extracted with 50% aqueous ethanol three times at room temperature. Upon removal of the solvent under vacuum, the ethanolic extract yielded 2.85 kg of material (Corydalis tuber extract, CTE; 7.6% by dry weight). We found that the CTE contained corydaline, palmatine, berberine, and other isoquinoline alkaloids. Based on HPLC analysis, the prescribed range of index components including corydaline and palmatine was detected in the CTE. The CTE was suspended in H 2 O and partitioned successively with n-hexane, ethyl acetate (EtOAc), and n-butanol. The EtOAc-soluble fraction (15 g) of the extract was subjected to a silica gel column using mixtures of n-hexane-EtOAc of increasing polarity as eluents to give 12 sub-fraction...

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Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Lee

Son

Kim

2010

Biological & Pharmaceutical Bulletin

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“…1,2) The stimulation of 5-HT 1B/1D receptors induces gastric accommodation in humans 3) and dogs, 4) and delays gastric emptying in humans. 5,6) The blockade of 5-HT 3 receptors inhibits gastrointestinal motility in humans.…”

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Pharmacological Characterization of 5-Hydroxytryptamine-Receptor Subtypes in Circular Muscle from the Rat Stomach

Komada

Yano

2007

Biological & Pharmaceutical Bulletin

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It is generally accepted that gastric emptying is regulated by the coordination of the proximal and distal stomach motilities. 5-HT has proven to be an important mediator of gastrointestinal motility.1,2) The stimulation of 5-HT 1B/1D receptors induces gastric accommodation in humans 3) and dogs, 4) and delays gastric emptying in humans. 5,6) The blockade of 5-HT 3 receptors inhibits gastrointestinal motility in humans. 7) In addition, the stimulation of 5-HT 4 receptors elicits gastrointestinal contractile activity and increases the rate of gastric emptying in humans 8,9) and dogs. [10][11][12] With regard to gastric smooth muscle activity, it is generally accepted that the 5-HT 1B/1D and 5-HT 7 receptors are relaxant whereas the 5-HT 2 , 5-HT 3 and 5-HT 4 receptors are contractile. Although the gastric contractility of 5-HT has been reported in a variety of species and stomach regions, regional and functional differences of 5-HT-receptor subtypes have been fully investigated only in the guinea pig stomach. [13][14][15][16] In the guinea pig stomach, the fundus presents the relaxant 5-HT 1 receptors and the contractile 5-HT 2 and 5-HT 3 receptors, the corpus presents the relaxant 5-HT 1 receptors and the contractile 5-HT 3 and 5-HT 4 receptors, and the antrum presents the contractile 5-HT 2 , 5-HT 3 and 5-HT 4 receptors. However, the in vivo studies for examining gastric motility and gastric emptying using guinea pigs are limited. On the other hand, the rat is widely used as in vivo models to study gastric motility [17][18][19] and gastric emptying rate. [20][21][22] The stimulation of 5-HT 2 receptors increases gastric motility, 17) the blockade of 5-HT 3 receptors accelerates gastric emptying, 20) and the stimulation of 5-HT 4 receptors increases gastric motility 18) and accelerates gastric emptying. 20,21) In in vitro, pharmacological characterization of the contractile response to 5-HT in the rat stomach regions still remains unclear, except for the contractile 5-HT 2B receptors in longitudinal muscle strips of the fundus. [23][24][25] The present study was, therefore, designed to provide further information regarding functions of 5-HT receptor subtypes in circular muscle strips from the antrum, corpus and fundus of the rat stomach. MATERIALS AND METHODSChemicals Carbachol (CCh), atropine sulfate monohydrate and tetrodotoxin (TTX) were purchased from Wako Pure Chemicals (Osaka, Japan). 5-Hydroxytryptamine hydrochloride (5-HT), methysergide maleate, ketanserin tartrate and SB-269970 (selective 5-HT 7 receptor antagonist) were purchased from Sigma (St. Louis, MO, U.S.A.). WAY-100635 maleate (selective 5-HT 1A receptor antagonist), GR127935 hydrochloride (5-HT 1B/1D receptor antagonist) and cinanserin hydrochloride (selective 5-HT 2 receptor antagonist) were purchased from Tocris Cookson (Ellisville, MO, U.S.A.). RS-127445 (selective 5-HT 2B receptor antagonist), ondansetron (selective 5-HT 3 receptor antagonist) and SB-203186 (selective 5-HT 4 receptor antagonist) were synthesized at Pfizer Inc. All the drugs...

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“…The antimigraine drug sumatriptan, which has affinity at different 5-HT 1 -receptor subtypes, was shown to induce feline and human gastric fundus relaxation (27), indicating therapeutic potential in the treatment of patients with functional dyspepsia (FD) (6,26). In dogs, studied with a barostat, sumatriptan shifted gastric pressure-volume curves toward higher volumes and enhanced gastric accommodation, an effect mediated by 5-HT 1B receptors (8). Recently, we showed that flesinoxan induces proximal gastric relaxation in conscious dogs via 5-HT 1A receptors.…”

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Characterization of 5-HT₇-receptor-mediated gastric relaxation in conscious dogs

Janssen¹,

Prins²,

Moreaux³

et al. 2005

American Journal of Physiology-Gastrointestinal and Liver Physi

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We aimed to evaluate the gastric relaxant capacity of the 5-HT 1/7-receptor agonist 5-carboxamidotryptamine (5-CT) in conscious dogs and to clarify the mechanism of action by use of selective antagonists, vagotomy, and in vitro experiments. A barostat enabled us to monitor the intragastric volume in response to different treatments (intravenously administered) before and after supradiaphragmatic vagotomy [results presented as the maximum volume change after treatment (mean; n ϭ 5-11)]. In vitro experiments were performed with isolated muscle strips cut from four different stomach regions of the vagotomized dogs [results were fitted to the operational model of agonism to determine the efficacy parameter (n ϭ 5)]. 5-CT (0.5-10 g/kg) caused a dose-dependent gastric relaxation (29 -267 ml) that was completely blocked by the selective 5-HT7-receptor antagonist SB-269970 (50 g/kg). After vagotomy, the relaxation to 10 g/kg 5-CT was significantly less pronounced (73 vs. 267 ml; P Ͻ 0.05) but still blocked by SB-269970, whereas the response to the nitric oxide donor nitroprusside was similar to that before vagotomy (178 vs. 218 ml). In vitro, 5-CT concentration dependently inhibited the PGF 2␣-contracted muscle strips before and after vagotomy. Although before and after vagotomy the response in every region was mediated by 5-HT7 receptors (apparent affinity dissociation constant: SB-269970, 8.2-8.6 vs. 8.3-8.6, respectively), the response after vagotomy was less efficacious (log : 1.9 to 0.5 vs. 1.4 to Ϫ0.1). The results indicate that the 5-CT-induced proximal stomach relaxation in conscious dogs before and after vagotomy is mediated via 5-HT7 receptors. The decreased efficacy of 5-CT in vitro after vagotomy is probably related to vagotomy-induced changes in receptor density or coupling efficiency and provides a possible explanation for the decreased in vivo response to 5-CT after vagotomy.5-HT7; efficacy distribution; vagotomy; barostat IN BETWEEN MEALS, THE PROXIMAL stomach has a high basal muscle tone. This tone is partially due to the high resting membrane potential of the proximal stomach muscle cells and the vagally mediated cholinergic input (4, 9). The tone of the proximal stomach decreases to accommodate food. This reflex relaxation is believed to be mainly mediated by nitric oxide (NO) release from the nitrergic efferent nerves. Indeed, the NO synthase inhibitor N G -monomethyl-L-arginine impairs gastric accommodation and enhances meal-induced satiety in humans (28).Different studies have shown the possibility of inducing gastric relaxation by activation of 5-HT receptors. The antimigraine drug sumatriptan, which has affinity at different 5-HT 1 -receptor subtypes, was shown to induce feline and human gastric fundus relaxation (27), indicating therapeutic potential in the treatment of patients with functional dyspepsia (FD) (6, 26). In dogs, studied with a barostat, sumatriptan shifted gastric pressure-volume curves toward higher volumes and enhanced gastric accommodation, an effect mediated by 5-HT 1B recepto...

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Role of 5-HT_1B/D receptors in canine gastric accommodation: effect of sumatriptan and 5-HT_1B/D receptor antagonists

Cited by 26 publications

References 36 publications

Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Pharmacological Characterization of 5-Hydroxytryptamine-Receptor Subtypes in Circular Muscle from the Rat Stomach

Characterization of 5-HT₇-receptor-mediated gastric relaxation in conscious dogs

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Role of 5-HT1B/D receptors in canine gastric accommodation: effect of sumatriptan and 5-HT1B/D receptor antagonists

Cited by 26 publications

References 36 publications

Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Effects of Corydaline from Corydalis Tuber on Gastric Motor Function in an Animal Model

Pharmacological Characterization of 5-Hydroxytryptamine-Receptor Subtypes in Circular Muscle from the Rat Stomach

Characterization of 5-HT7-receptor-mediated gastric relaxation in conscious dogs

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Role of 5-HT_1B/D receptors in canine gastric accommodation: effect of sumatriptan and 5-HT_1B/D receptor antagonists

Characterization of 5-HT₇-receptor-mediated gastric relaxation in conscious dogs