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Dihydropyridines on guinea-pig ileum
I Martin1, I Colado, V del Val
1Department of Pharmacology, School of Medicine, Universidad Complutense, Madrid, Spain.
General Pharmacology
|January 1, 1990
Summary
Nifedipine and related dihydropyridine derivatives effectively inhibit guinea-pig ileum contractions. Nisoldipine demonstrated the most potent inhibitory effects among the tested compounds.
Area of Science:
- Pharmacology
- Physiology
Background:
- Dihydropyridine derivatives are known calcium channel blockers.
- Their effects on smooth muscle, specifically the guinea-pig ileum, warrant detailed investigation.
Purpose of the Study:
- To compare the inhibitory effects of three dihydropyridine derivatives (nimodipine, nitrendipine, and nisoldipine) with nifedipine.
- To determine the relative potency of these agents on guinea-pig ileum contractile responses.
Main Methods:
- Experiments were conducted on isolated guinea-pig ileum.
- Dose-dependent contractile responses were measured.
- Inhibition was assessed using single pulse stimulation, acetylcholine (1 microM), and high-potassium (50 mM) induced contractions.
- Nifedipine, nimodipine, and nitrendipine were tested at concentrations of 25-200 nM, while nisoldipine was tested at 10-80 nM.
Main Results:
- Nifedipine, nimodipine, and nitrendipine exhibited dose-dependent inhibition of contractile responses.
- Nimodipine and nitrendipine showed potent inhibitory effects comparable to nifedipine.
- Nisoldipine proved to be the most potent inhibitor among the tested dihydropyridine derivatives.
Conclusions:
- Nimodipine and nitrendipine possess potent inhibitory effects on guinea-pig ileum contractions, similar to nifedipine.
- Nisoldipine is the most active dihydropyridine derivative studied for inhibiting guinea-pig ileum contractility.