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STUDIES ON THE SPASMOLYTIC AND UTERINE RELAXANT ACTIONS OF N -ETHYL AND N -BENZYL-1,2-DIPHENYL ETHANOLAMINES: ELUCIDATION OF THE MECHANISMS OF ACTION
How n-ethyl and n-benzyl-1,2-diphenyl ethanolamines help relax muscles and the uterus and how they work
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Abstract
The compounds N-ethyl- and N-benzyl-1,2-diphenyl ethanolamines inhibited spontaneous contractions in the rabbit jejunum with ID50 values of 0.13 and 0.03 micromol ml-1, respectively.
- Both compounds significantly inhibited contractions induced by various spasmogens, including nicotine and acetylcholine, by 44-100%.
- Compound E was found to be several times more potent than B in inhibiting spontaneous uterine contractions, with an ID50 of 7 nmol ml-1.
- The inhibitory effects of E and B were not reversed by beta2-adrenoceptor or H2-receptor antagonists.
- Both compounds acted competitively to antagonize CaCl2-induced contractions in K+-depolarized uteri, with ID50 values ranging from 1.6 to 10.7 nmol ml-1.
- E and B may function as L-Ca2+ channel blockers with selectivity towards uterine and intestinal smooth muscle, respectively.
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