The calcium channel antagonist, verapamil, potentiates the inhibitory action of morphine on intestinal and biliary motility

Shah, Mohit; Dikshit, R K; Mansuri, Sohil

doi:10.1111/j.2042-7158.1987.tb03157.x

Cited by 6 publications

(4 citation statements)

References 10 publications

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“…The finding that verapamil did not suppress the basal gastrointestinal transit (see Figure 4) is in agreement with the work by di carlo et al . (1993) , while some other studies have revealed decreased gastrointestinal transit following verapamil ( Shah et al ., 1987 ; Calignano et al ., 1992 ). The effectiveness of verapamil in the resting state might vary with experimental conditions such as the strain or size of mice employed.…”

Section: Discussionmentioning

confidence: 92%

In vivo evidence that protease‐activated receptors 1 and 2 modulate gastrointestinal transit in the mouse

Kawabata

Kuroda

Nagata

et al. 2001

British J Pharmacology

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1 Protease-activated receptors (PARs) 1 and 2 modulate the gastric and intestinal smooth muscle motility in vitro. In the present study, we examined if activation of PAR-2 and PAR-1 could alter gastrointestinal transit in mice. 2 Intraperitoneal administration of the PAR-2-activating peptide SLIGRL-NH 2 , but not the inactive control LSIGRL-NH 2 , at 1±5 mmol kg 71 , in combination with the aminopeptidase inhibitor amastatin at 2.5 mmol kg 71 , facilitated gastrointestinal transit in a dose-dependent manner. The human PAR-1-derived peptide SFLLR-NH 2 and the speci®c PAR-1 agonist TFLLR-NH 2 , but not the inactive control FSLLR-NH 2 , at 2.5 ± 10 mmol kg 71 , in combination with amastatin, also promoted gastrointestinal transit. 3 The Ca 2+ -activated, small conductance K + channel inhibitor apamin at 0.01 mmol kg 71 signi®cantly potentiated the actions of SLIGRL-NH 2 and TFLLR-NH 2 at sube ective doses. 4 The increased gastrointestinal transit exerted by either SLIGRL-NH 2 at 5 mmol kg 71 or TFLLR-NH 2 at 10 mmol kg 71 was completely abolished by the L-type Ca 2+ channel inhibitor verapamil at 61.6 mmol kg 71 . In contrast, the tyrosine kinase inhibitor genistein at 18.5 mmol kg 71 failed to modify the e ects of the agonists for PAR-2 or PAR-1. 5 These ®ndings demonstrate that PAR-1 and PAR-2 modulate gastrointestinal transit in mice in vivo. Our data also suggest that the PAR-1-and PAR-2-mediated e ects are modulated by apaminsensitive K + channels and are dependent on activation of L-type Ca 2+ channels, but independent of tyrosine kinase. Our study thus provides novel evidence for the physiological and/or pathophysiological roles of PARs 1 and 2 in the digestive systems, most probably during in¯ammation.

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Section: Discussionmentioning

confidence: 92%

In vivo evidence that protease‐activated receptors 1 and 2 modulate gastrointestinal transit in the mouse

Kawabata

Kuroda

Nagata

et al. 2001

British J Pharmacology

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“…To d o this we studied the effects of clonidine, an az-adrenoceptor agonist which is known to antagonize some withdrawal symptoms in animals and man, and nifedipine, a calcium channel antagonist. There is evidence that calcium plays a role in the antinociceptive action of opiates as well as in the development of tolerance and physical dependence (Harris et al 1976;Bongianni et al 1986;Shah et al 1987a) and binding sites for calcium blocking drugs have been found in intestinal smooth muscles (Bolger et al 1983).…”

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confidence: 97%

“…There is evidence that calcium plays a role in the antinociceptive action of opiates as well as in the development of Correspondence to: P. Valeri, Institute of Pharmacology and Phamacognosy, University of Rome "La Sapienza", 001 85 Rome, Italy. tolerance and physical dependence (Harris et al 1976;Bongianni et al 1986;Shah et al 1987a) and binding sites for calcium blocking drugs have been found in intestinal smooth muscles (Bolger et al 1983).…”

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confidence: 99%

Reproducible Withdrawal Contractions of Isolated Guinea-pig Ileum after Brief Morphine Exposure: Effects of Clonidine and Nifedipine

Valeri

Martinelli

Morrone

et al. 1990

Journal of Pharmacy and Pharmacology

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Guinea-pig ileum stored for 30 min in Krebs solution and then mounted in Tyrode solution gave reproducible contracture responses to naloxone after brief exposure to morphine. The preparation lasted for several hours and a variety of pharmacological tests could be made. Clonidine, an alpha 2-adrenoceptor agonist, and nifedipine, a calcium channel antagonist, both known to interfere with tolerance and physical dependence, inhibited naloxone withdrawal contractures in a dose related way. Their action seemed to be receptor-mediated since yohimbine and Bay k 8644, respectively, reversed their inhibitory effect.

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“…Apigenin, quercetin and other flavonoids inhibit enzymes involved in arachidonate metabolism (Mascolo et al, 1988). However, the (Abdalla and Abu Zarga, 1987;Shah et al, 1987;Meli et al, 1990). Flavonoids are useful in relieving gastrointestinal colic, diarrhoea and/or other gastrointestinal disorders.…”

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confidence: 98%

Reduction of agonist‐induced contractions of guinea‐pig isolated ileum by flavonoids

Capasso

Pinto

Mascolo

et al. 1991

Phytotherapy Research

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The effect of 13 flavonoids on the contraction of guinea-pig isolated ileum induced by prostaglandin E2 (PGE2) and leukotriene D4 (LTD4) have been investigated. Apigenin, quercetin and kaempferol at a concentration of 10-mu-M significantly (p < 0.001) reduced the contraction to either agonist. Crysin and flavone antagonized only PGE2 (p < 0.01). The other flavonoids were inactive. The blocking effect of apigenin, quercetin and kaempferol against PGE2 was also concentration- and time-dependent, and was augmented by the calcium channel blocker verapamil or by lowering the extracellular calcium to 25%, consistent with a calcium-mediated mechanism of protection which these flavonoids, at the same concentration, also showed against barium chloride (BaCl2)- or acetylcholine (ACh)-induced contraction (p < 0.05-0.001)

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The calcium channel antagonist, verapamil, potentiates the inhibitory action of morphine on intestinal and biliary motility

Cited by 6 publications

References 10 publications

In vivo evidence that protease‐activated receptors 1 and 2 modulate gastrointestinal transit in the mouse

In vivo evidence that protease‐activated receptors 1 and 2 modulate gastrointestinal transit in the mouse

Reproducible Withdrawal Contractions of Isolated Guinea-pig Ileum after Brief Morphine Exposure: Effects of Clonidine and Nifedipine

Reduction of agonist‐induced contractions of guinea‐pig isolated ileum by flavonoids

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