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The synthesis and pharmacology of some 1,4,5,6‐tetrahydropyrimidines
Author(s) -
BRIMBLECOMBE R. W.,
HUNT R. R.,
RICKARD R. L.,
TAYLOR JOAN V.
Publication year - 1969
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1969.tb10579.x
Subject(s) - pharmacology , chemistry , toxicity , depolarization , nicotinic agonist , neuromuscular junction , neuromuscular blocking agents , drug , receptor , stereochemistry , toxicology , medicine , biochemistry , biology , anesthesia , neuroscience , organic chemistry
1 . Several 1‐ and 2‐substituted, and 1,2‐disubstituted, 1,4,5,6‐tetrahydropyrimidines have been prepared and their toxicological and pharmacological properties have been investigated. 2 . In general the compounds were neuromuscular blocking agents with the monosubstituted members of the series showing a depolarizing type of activity and the disubstituted compounds a non‐depolarizing type. 3 . The toxicity to mice of some of the monosubstituted compounds was increased by pretreatment of the animals with SKF 525A, but the toxicity of the disubstituted compounds was unaffected. 4 . The results obtained with these compounds are not at variance with a suggestion made previously that nicotinic action at the neuromuscular junction can result from an interaction between drug and receptor at two points separated by about 4 Å.