2-Ethynylbenzenealkanamines. A new class of calcium entry blockers
| Autor: | J R, Carson, H R, Almond, M D, Brannan, R J, Carmosin, S F, Flaim, A, Gill, M M, Gleason, S L, Keely, D W, Ludovici, P M, Pitis |
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| Rok vydání: | 1988 |
| Předmět: |
Inotrope
Tertiary amine Guinea Pigs Cell Pharmacology Structure-Activity Relationship chemistry.chemical_compound Coronary Circulation Rats Inbred SHR Drug Discovery medicine Animals Amines Calcium entry Aryl Biological activity Calcium Channel Blockers In vitro Rats Vasodilation medicine.anatomical_structure chemistry Biochemistry Alkynes Hypertension Molecular Medicine Coronary vasodilator |
| Zdroj: | Journal of Medicinal Chemistry. 31:630-636 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00398a023 |
| Popis: | A series of 2-(aryl- or alkylethynyl)benzenealkanamines were synthesized. They exhibit antihypertensive activity in spontaneously hypertensive rats and coronary vasodilator activity with minimal negative inotropic activity in the "Langendorff" guinea pig heart in vitro. They have been shown to exert their activity by inhibition of Ca2+ influx across cell membranes. Optimal activity is found among the N-(arylethyl)-5-methoxy-alpha-methyl-2-(phenylethynyl)ben zeneethanamines and -propanamines. |
| Databáze: | OpenAIRE |
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