Paper
Effect of 1-adamantyl radicals on curare-like activity
Published May 1, 1975 · D. A. Kharkovich, A. P. Skoldinov
Bulletin of Experimental Biology and Medicine
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Abstract
The importance of hydrophobic 1-adamantyl radicals (Ad) for curare-like activity was investigated in a series of polymethylene bis-ammonium salts R(CH3)2N+(CH2)nN+(CH3)2R·21− (R=CH3 or Ad). Introduction of Ad radicals into the cationic groups of depolarizing agents (n=9–11) changed the mechanism of their action and lowered their activity. Addition of Ad radicals to the quaternary nitrogen atoms of antidepolarizing agents (n=5 and 6) sharply increased their curare-like activity. The results are evidence of the existence of hydrophobic zones in nicotinic cholinergic receptors of skeletal muscles.
Hydrophobic 1-adamantyl radicals significantly influence curare-like activity in skeletal muscles, with their introduction altering depolarizing agents' mechanisms and increasing antidepolarizing agents' activity.
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