Potential irreversible inhibitors of acetylcholinesterase: N-trimethyl-N‘-iodoacetyl diaminoalkane iodides
- 1 November 1971
- journal article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 23 (11) , 865-867
- https://doi.org/10.1111/j.2042-7158.1971.tb10204.x
Abstract
Potential irreversible inhibitors of acetylcholinesterase based on N-trimethyl-N'-iodacetyl diaminoalkane iodide Me3N+[CH2]n-NHCO·CH2I·I-, (I; n = 4) and (II; n = 2) have been prepared. (I) and (II) are both competitive inhibitors of the enzyme with Ki, 5·9 times 10−4m and 1·2 times 10−3m respectively. (I) is a partial agonist and (II) is a true agonist at the muscarinic receptor of guinea-pig ileum.Keywords
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