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Literature summary 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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.7 compound C547 a very potent and selective reversible inhibitor of AChE, shows a high level of pharmacological selectivity in inhibiting acetylcholinesterase as compared to butyrylcholinesterase (EC 3.1.1.8) Homo sapiens
3.1.1.7 compound C547 a fast-binding inhibitor of mixed-type and a very potent and selective reversible inhibitor of AChE, shows a high level of pharmacological selectivity in inhibiting acetylcholinesterase as compared to butyrylcholinesterase (EC 3.1.1.8) Rattus norvegicus
3.1.1.7 additional information no inhibition by bambuterol Homo sapiens
3.1.1.7 additional information no inhibition by bambuterol Rattus norvegicus
3.1.1.7 pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Homo sapiens
3.1.1.7 pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Rattus norvegicus
3.1.1.8 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
3.1.1.8 bambuterol a selective BChE inhibitor, causing 98% inhibition of BChE Homo sapiens
3.1.1.8 iso-ompa specific inhibition of BChE Homo sapiens
3.1.1.8 pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.1.7 acetylcholine + H2O Homo sapiens
-
 choline + acetate
-
 ?
3.1.1.7 acetylcholine + H2O Rattus norvegicus
-
 choline + acetate
-
 ?
3.1.1.8 butyrylcholine + H2O Homo sapiens
-
 choline + butyrate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.7 Homo sapiens P22303
-
-
3.1.1.7 Rattus norvegicus P37136
-
-
3.1.1.8 Homo sapiens P06276
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.7 bladder
-
 Homo sapiens
-
3.1.1.7 bladder
-
 Rattus norvegicus
-
3.1.1.7 smooth muscle
-
 Homo sapiens
-
3.1.1.7 smooth muscle
-
 Rattus norvegicus
-
3.1.1.8 bladder
-
 Homo sapiens
-
3.1.1.8 smooth muscle
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.7 acetylcholine + H2O
-
 Homo sapiens choline + acetate
-
 ?
3.1.1.7 acetylcholine + H2O
-
 Rattus norvegicus choline + acetate
-
 ?
3.1.1.7 acetylthiocholine + H2O
-
 Homo sapiens thiocholine + acetate
-
 ?
3.1.1.7 acetylthiocholine + H2O
-
 Rattus norvegicus thiocholine + acetate
-
 ?
3.1.1.8 butyrylcholine + H2O
-
 Homo sapiens choline + butyrate
-
 ?
3.1.1.8 butyrylthiocholine + H2O
-
 Homo sapiens thiocholine + butyrate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.7 AChE
-
 Homo sapiens
3.1.1.7 AChE
-
 Rattus norvegicus
3.1.1.8 BChE
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.8 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

EC Number General Information Comment Organism
3.1.1.7 malfunction compound C547 and pyridostigmine bromide 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. In contrast, almost complete inhibition of butyrylcholinesterase (BChE, EC 3.1.1.8) does not affect either the force of contractions or tonus of EAMG rat bladders in vivo Rattus norvegicus
3.1.1.7 malfunction compound C547 and pyridostigmine bromide show efficiency to reduce muscle weakness symptoms and ability to activate contractions of urinary bladder in autoimmune myasthenia gravis (MG) treatment. At a dose effectively reducing MG symptoms, C547 does not affect activity of human urinary bladder, while at equipotent dose, pyridostigmine causes a significant increase in tonus and force of spontaneous contractions of bladder wall Homo sapiens
3.1.1.7 physiological function both AChE and BChE (EC 3.1.1.8) are involved in cholinergic modulation of rat urinary bladder contractions Rattus norvegicus
3.1.1.8 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
3.1.1.8 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