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Literature summary for 3.1.1.8 extracted from

  • Petrov, K.A.; Kharlamova, A.D.; Lenina, O.A.; Nurtdinov, A.R.; Sitdykova, M.E.; Ilyin, V.I.; Zueva, I.V.; Nikolsky, E.E.
    Specific inhibition of acetylcholinesterase as an approach to decrease muscarinic side effects during myasthenia gravis treatment (2018), Sci. Rep., 8, 304 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.8

Inhibitors

Inhibitors Comment Organism Structure
1,3-bis[5(diethyl-o-nitrobenzylammonium)pentyl]-6-methyluracil dibromide compound C547, a fast-binding reversible inhibitor of mixed-type on human BChE. The inhibitor shows a high level of pharmacological selectivity in inhibiting acetylcholinesterase (AChE, EC 3.1.1.7) as compared to butyrylcholinesterase Homo sapiens
bambuterol a selective BChE inhibitor, causing 98% inhibition of BChE Homo sapiens
iso-ompa specific inhibition of BChE Homo sapiens
pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
butyrylcholine + H2O Homo sapiens
-
 choline + butyrate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P06276
-
-

Source Tissue

Source Tissue Comment Organism Textmining
bladder
-
 Homo sapiens
-
smooth muscle
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylcholine + H2O
-
 Homo sapiens choline + butyrate
-
 ?
butyrylthiocholine + H2O
-
 Homo sapiens thiocholine + butyrate
-
 ?

Synonyms

Synonyms Comment Organism
BChE
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00177
-
 1,3-bis[5(diethyl-o-nitrobenzylammonium)pentyl]-6-methyluracil dibromide pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
malfunction compound C547 and pyridostigmine show efficiency to reduce muscle weakness symptoms and ability to activate contractions of urinary bladder in a rat model of autoimmune myasthenia gravis (MG). At a dose effectively reducing MG symptoms, C547 does not affect activity of rat urinary bladder, while at equipotent dose, pyridostigmine causes a significant increase in tonus and force of spontaneous contractions of bladder wall Homo sapiens
physiological function background activity of BChE in the bladder might be sufficient to compensate for partial inhibition of AChE (EC 3.1.1.7), in contrast to skeletal muscle. Functional role of BChE might be different in the urinary bladder of rat and human Homo sapiens