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Ergoline derivatives with oral, prolonged, alpha-adrenolytic activity
Il Farmaco; Edizione Scientifica
|February 1, 1978
Summary
The novel compound 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate demonstrates potent alpha-adrenolytic activity. Orally administered, it shows superior efficacy and duration compared to dihydroergotamine.
Area of Science:
- Pharmacology
- Medicinal Chemistry
Background:
- Alpha-adrenolytic agents are crucial in managing various cardiovascular conditions.
- Dihydroergotamine is a well-established alpha-adrenolytic drug.
Purpose of the Study:
- To evaluate the alpha-adrenolytic activity of a novel compound, 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate (XV, formula II).
- To compare its efficacy and duration with dihydroergotamine via different administration routes.
Main Methods:
- In vitro assessment of alpha-adrenolytic activity.
- Parenteral administration studies.
- Oral administration studies comparing the new compound to dihydroergotamine.
Main Results:
- Compound XV exhibited alpha-adrenolytic activity comparable to dihydroergotamine in vitro and via parenteral administration.
- Oral administration of compound XV resulted in greater activity and longer duration than dihydroergotamine.
Conclusions:
- 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate is a promising alpha-adrenolytic agent.
- Its oral efficacy and duration offer potential advantages over dihydroergotamine for therapeutic applications.