Amines: Histamine

Bertaccini, G.

doi:10.1007/978-3-642-68474-6_7

Cited by 6 publications

(6 citation statements)

References 48 publications

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“…Although many studies on the responsiveness to histamine of external smooth muscles of the alimentary tract have been published (Bertaccini, 1982), there are few accounts of the effect of histamine on the muscularis mucosae (Walder, 1953;Hughes, 1955;Bartlet, 1968;Bartlet & Hassan, 1968). The present investigation confirms that histamine produces a tonic contracture of the muscularis mucosae isolated from the guinea-pig oesophagus.…”

Section: Discussionsupporting

confidence: 81%

“…This is supported by the present results showing the relative potencies of histamine agonists and the affinity constants for histamine and the Hireceptor antagonist diphenhydramine ( Table 2). The estimated KA value of histamine and the pA2 value of diphenhydramine are comparable with those obtained in the guinea-pig ileum where histamine interacts preferentially with Hi-receptors (Arunlakshana & Schild, 1959;Furchgott, 1966;Bertaccini, 1982). The KA value of histamine was approximately 14 fold higher than the EC50 value.…”

Section: Discussionsupporting

confidence: 78%

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Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Fujinuma

Kamikawa

Shimo

1985

British J Pharmacology

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1 To characterize the histamine receptors in the muscularis mucosae, the isotonic responsiveness of the isolated muscularis mucosae of the guinea-pig oesophagus to histamine receptor agonists and antagonists was examined in vitro. 2 Histamine (0.1-100 M) produced a concentration-dependent contraction of the muscularis mucosae (EC50 = 1.6 ± 0.2 LM). The contractions were rapid in onset, sustained, reversible by washing and the preparation did not show tachyphylaxis. 3 2-Methylhistamine (2-MH), 2-pyridylethylamine (PEA) and 4-methylhistamine (4-MH) produced similar sustained contractions of the muscularis mucosae. The order of sensitivity was histamine > 2-MH > PEA> 4-MH. Impromidine (10-300 LM) and dimaprit (10-300 gM) caused no response in this tissue. 4 The contractile responses to histamine, 2-MH, and PEA were competitively antagonized by diphenhydramine, and the pA2 values were almost the same (approximately 8.1). Cimetidine (I 00 gM)could not modify the contractile response to these agonists. 5 The contractile response to histamine was slightly inhibited by tetrodotoxin (0.3 JM), atropine (1 LM), indomethacin (0.1-3 jAM) or aspirin (30-300 jM), and the EC50 value was increased about [2][3][4][5][6] times by these drugs. 6 When the preparation was incubated in Tyrode solution containing various calcium concentrations (0, 0.45, 0.9 and 1.8 mM), the concentration-response curve to histamine was shifted to the right and downward; the effect was inversely dependent on the calcium concentration, and in a calcium-free medium the response to histamine was abolished. Verapamil (1-10 M) partially inhibited the contractile response to histamine. 7 The present results indicate that the contraction of the guinea-pig oesophageal muscularis mucosae to histamine is mediated mainly by a direct action on the smooth muscle and partly by indirect actions via the stimulation of either endogenous prostaglandin biosynthesis or intramural cholinergic nerves. The histamine receptors responsible for contractions of this tissue are probably mainly of the H,-subtype with H2-receptors having a negligible role.

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Section: Discussionsupporting

confidence: 81%

Section: Discussionsupporting

confidence: 78%

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Fujinuma

Kamikawa

Shimo

1985

British J Pharmacology

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“…An increasing number of studies suggest that serotonin (5-HT) may act as a neurotrans mitter in the small intestine [1]. It was found that 5-hydroxytryptophan (5-HTP) is taken up by the intestine and converted into 5-HT [2].…”

Section: Introductionmentioning

confidence: 99%

5-Hydroxytryptophan and Cisapride Stimulate Propulsive Jejunal Motility and Transit of Chyme in Dogs

Schemann¹,

Ehrlein²

1986

Digestion

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We investigated in conscious dogs the effects of intravenously administered 5-hydroxytryptophan (5-HTP) and cisapride on the postprandial jejunal mechanical activity by means of six closely spaced extraluminal strain gauge transducers. Drugs were given after administration of a nutrient meal. 5-HTP was given additionally after the administration of a noncaloric cellulose meal. Computer assistance was used to determine the temporal and spatial relationship of contractions and thereby to evaluate the length of spread of contractile waves. Both substances increased the propulsive activity, the contractile force and the motility index and fastened the transit rate of digesta. 5-HTP exhibited the most potent effect when given after administration of the nutrient meal.

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“…In a previous study (Bertaccini, Coruzzi, Molina & Chiavarini, 1977) it was also observed that the H2-blocker, burimamide, exerted a spasmogenic effect on the rat pylorus and other investigations carried out in our department (Scarpignato, Capovilla & Bertaccini, 1980;Bertaccini, De Castiglione & Scarpignato, 1981; have emphasized the importance of the pylorus in the regulation of gastric emptying in the rat. Several non-specific effects of the H2-receptor antagonists have been reported (Bertaccini & Dobrilla, 1980;Bertaccini, 1982): some of these effects concerned gut motility.We decided to investigate more thoroughly the effect of all the available H2-receptor antagonists on gastric emptying in the conscious rat. …”

mentioning

confidence: 99%

HISTAMINE H₂‐ANTAGONISTS MODIFY GASTRIC EMPTYING IN THE RAT

Bertaccini

Scarpignato

1982

British J Pharmacology

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1 Histamine H2-receptor antagonists were tested for their effect on gastric emptying in the rat. 2 At low doses all the compounds were inactive except for burimamide which delayed and ranitidine which accelerated gastric emptying. 3 At high doses burimamide, metiamide, cimetidine and oxmetidine delayed, whereas ranitidine accelerated gastric emptying; tiotidine remained ineffective. 4 Changes in emptying rate were not accompanied by changes in emptying pattern which, with all the compounds examined, proceeded, as in the controls, by apparent first order kinetics. 5 The mechanism of the ranitidine-induced acceleration of gastric emptying seemed to be connected with an interference with the cholinergic system, whereas the mechanism of cimetidineand oxmetidine-induced slowing of gastric emptying was apparently related to cholinolytic and possibly also relaxant effects of the compounds.6 These different effects of the various H2-blockers are consistent with the idea that changes in emptying rate are independent of H2-receptor blockade. IntroductionIn a thorough investigation concerning histamine receptors and gastrointestinal motility we observed that histamine delayed gastric emptying (GE) in the conscious rat through stimulation of HI-receptors (Bertaccini, Scarpignato, Coruzzi & Bertaccini, 1981). In a previous study (Bertaccini, Coruzzi, Molina & Chiavarini, 1977) it was also observed that the H2-blocker, burimamide, exerted a spasmogenic effect on the rat pylorus and other investigations carried out in our department (Scarpignato, Capovilla & Bertaccini, 1980;Bertaccini, De Castiglione & Scarpignato, 1981; have emphasized the importance of the pylorus in the regulation of gastric emptying in the rat. Several non-specific effects of the H2-receptor antagonists have been reported (Bertaccini & Dobrilla, 1980;Bertaccini, 1982): some of these effects concerned gut motility.We decided to investigate more thoroughly the effect of all the available H2-receptor antagonists on gastric emptying in the conscious rat. MethodsMale Wistar rats weighing approximately 200 g and fasted 24 h prior to experiments were used. Gastric emptyingThe test meal consisted of 1.5 ml/rat of a solution of 50 mg phenol red in 100 ml of aqueous methylcellulose (1.5%), given by oral intubation. H2-blockers were injected in a constant volume of saline (1 ml/kg), by the intraperitoneal route, 5 min before administration of the meal. The animals were killed at various time intervals after intubation to evaluate the duration of the pharmacological effects. The effect of the H2-blockers on gastric emptying as well as the interference of other pharmacological compounds was evaluated at a fixed time (20 min). This time was selected because gastric emptying at 20 min (54.5 ± 3.1%) allowed us to evaluate drug-induced acceleration or delay in emptying. Doses employed in this study were selected on the basis of the relative activity of the various drugs on gastric secretion. In each experiment a group of 4 animals was killed immediately after the meal a...

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Amines: Histamine

Cited by 6 publications

References 48 publications

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

5-Hydroxytryptophan and Cisapride Stimulate Propulsive Jejunal Motility and Transit of Chyme in Dogs

HISTAMINE H₂‐ANTAGONISTS MODIFY GASTRIC EMPTYING IN THE RAT

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Amines: Histamine

Cited by 6 publications

References 48 publications

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

5-Hydroxytryptophan and Cisapride Stimulate Propulsive Jejunal Motility and Transit of Chyme in Dogs

HISTAMINE H2‐ANTAGONISTS MODIFY GASTRIC EMPTYING IN THE RAT

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HISTAMINE H₂‐ANTAGONISTS MODIFY GASTRIC EMPTYING IN THE RAT