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THE NEUROMUSCULAR BLOCKING PROPERTIES OF A SERIES OF BIS‐QUATERNARY TROPEÏNES
Author(s) -
HAINING C. G.,
JOHNSTON R. G.,
SMITH J. M.
Publication year - 1960
Publication title -
british journal of pharmacology and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0366-0826
DOI - 10.1111/j.1476-5381.1960.tb01212.x
Subject(s) - chemistry , stereochemistry , medicinal chemistry , potency , epimer , hydrochloride , organic chemistry , biochemistry , in vitro
Linkage of two tropine esters through their nitrogen atoms by the chain ‐[CH 2 ] m ‐O‐CO‐[CH 2 ] n ‐CO‐O‐[CH 2 ] m ‐, in which m was 2 or 3 and n varied from 0 to 6 , gave compounds which produced neuromuscular block without depolarization. Reversibility by neostigmine was confirmed for a few compounds. Potency was found to depend upon the tropine ester employed and upon the values of n and m . Short duration and hypotensive properties were favoured by the higher values of n . The duration of action of the compound based on the phenylacetic acid ester of tropine, in which n = 4 and m = 2, varied considerably in different species. Epimerization, in which the relative positions of the methyl group and the linking chain on the quaternary tropane nitrogen atom were reversed, did not produce substances having more favourable properties than those possessed by the unepimerized compounds.