Abstract
The synthesis and pharmacological profiles of some new steroidal mono- and bisquaternary ammonium derivatives have been described. The compounds featured have been conceptually derived structurally from two lead structures: pancuronium bromide 1 and chandonium iodide 2. In vitro and in vivo neuromuscular blocking studies have indicated the monoquaternary compound 15 to be less active than the bisquaternary compounds 10 and 11. The compound 11 has been found to be more active than d-tubocurarine.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding, Competitive
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Carbachol / antagonists & inhibitors
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Cats
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Chickens
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Cholinergic Agonists / metabolism
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Cholinergic Antagonists / chemical synthesis
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Cholinergic Antagonists / pharmacology
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Muscles / drug effects
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Neuromuscular Blocking Agents / chemical synthesis*
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Neuromuscular Blocking Agents / pharmacology
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Steroids / chemical synthesis
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Steroids / pharmacology
Substances
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Cholinergic Agonists
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Cholinergic Antagonists
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Neuromuscular Blocking Agents
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Steroids
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Carbachol