| Title | Lower esophageal sphincter relaxing agents: an in vitro comparative study in the rabbit | ||
| Authors | M. Koutsoviti-Papadopoulou, Th.A. Psarra and G.C. Batzias
Laboratory of Pharmacology, Veterinary Faculty, Aristotle University, Thessaloniki, Greece |
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| Citation | Koutsoviti-Papadopoulou, M., Psarra, T.A. and Batzias, G.C.: Lower esophageal sphincter relaxing agents: an in vitro comparative study in the rabbit, Epitheorese Klin. Farmakol. Farmakokinet. 22(2): 203-206 (2008) | ||
| Publication Date | 23-25 May 2008 | ||
| Full Text Language | English | ||
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €)
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| Keywords | Lower esophageal sphincter (LES), milrinone, theophylline, phosphodiesterase (PDE) inhibitors, verapamil, rabbit. | ||
| Other Terms | Review article | ||
| Summary | This study shows that the calcium channel blocker verapamil, the cardiac PDE 3 inhibitor milrinone, and the non-selective PDE inhibitor theophylline, a drug prescribed mainly as a bronchodilator, all produce a concentration-dependent, non-adrenergic non-cholinergic (NANC), post-synaptic, muscle-mediated relaxation on the rabbit LES. The potency rank of order is verapamil > milrinone > theophylline, as the IC50 values are found to be 2.75×10-6 M, 7.6×10-6 M and 3.8×10-4 M for verapamil, milrinone and theophylline, respectively. All three drugs exhibit equal efficacy, which is comparable to that produced by the potent PDE inhibitor papaverine. The theophylline- and milrinone-induced relaxation is not significantly modified either by nicotinic acid, an antagonist of adenylate cyclase, or by the inhibitor of NO-synthetase L-NAME and the purinergic antagonist suramin. The results obtained suggest that PDE 3 seems to play a critical role in the regulation of the rabbit LES tone and that it is the cAMP pathway which appears to be the main determinant of the milrinone- and theophylline-induced relaxation on the rabbit LES. | ||
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| Relative Papers | |||
Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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