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Literature summary for 3.1.1.7 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

Inhibitors Comment Organism Structure
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
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
additional information no inhibition by bambuterol Homo sapiens
additional information no inhibition by bambuterol Rattus norvegicus
pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Homo sapiens
pyridostigmine a non-selective inhibitor of cholinesterases (ChEs) Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P22303
-
-
Rattus norvegicus P37136
-
-

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylcholine + H2O
-
Homo sapiens choline + acetate
-
?
acetylcholine + H2O
-
Rattus norvegicus choline + acetate
-
?
acetylthiocholine + H2O
-
Homo sapiens thiocholine + acetate
-
?
acetylthiocholine + H2O
-
Rattus norvegicus thiocholine + acetate
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Homo sapiens
AChE
-
Rattus norvegicus

General Information

General Information Comment Organism
physiological function both AChE and BChE (EC 3.1.1.8) are involved in cholinergic modulation of rat urinary bladder contractions Rattus norvegicus
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
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