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Literature summary for 3.1.1.8 extracted from

  • Jia, P.; Sheng, R.; Zhang, J.; Fang, L.; He, Q.; Yang, B.; Hu, Y.
    Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors (2008), Eur. J. Med. Chem., 44, 772-784.
    View publication on PubMed
Search for more literature for 3.1.1.8

Inhibitors

Inhibitors Comment Organism Structure
10-N-demethyl-10-N-(10-(4-(piperidin-1-ylmethyl)-phenoxy)decan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(12-(4-(piperidin-1-ylmethyl)-phenoxy)dodecan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(2-(4-(piperidin-1-ylmethyl)phenoxy)ethan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(3-(4-(piperidin-1-ylmethyl)phenoxy)propan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(1-benzylpiperidin-4-yloxy)-butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(3-(1-morpholinoethyl)phenoxy)butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(4-((diethylamino)methyl)-phenoxy)butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(4-(morpholinomethyl)phenoxy)butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(4-(piperidin-1-ylmethyl)phenoxy)butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(4-(4-(pyrrolidine-1-carbonyl)-phenoxy)butan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(5-(4-(piperidin-1-ylmethyl)phenoxy)pentan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(1-benzylpiperidin-4-yloxy)-hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(3-(1-morpholinoethyl)phenoxy)hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(4-((diethylamino)methyl)-phenoxy)hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(4-(morpholinomethyl)phenoxy)hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(4-(piperidin-1-ylmethyl)phenoxy)hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(6-(4-(pyrrolidine-1-carbonyl)-phenoxy)hexan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(8-(4-(piperidin-1-ylmethyl)phenoxy)octan-1-yl)-galanthamine
-
 Rattus norvegicus
10-N-demethyl-10-N-(9-(4-(piperidin-1-ylmethyl)phenoxy)nonan-1-yl)-galanthamine
-
 Rattus norvegicus
galanthamine
-
 Rattus norvegicus
additional information design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors, overview Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Rattus norvegicus
-
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
serum
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylthiocholine iodide + H2O detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB Rattus norvegicus butyrate + thiocholine iodide
-
 ?

Synonyms

Synonyms Comment Organism
BChE
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(12-(4-(piperidin-1-ylmethyl)-phenoxy)dodecan-1-yl)-galanthamine
0.0033
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(4-(morpholinomethyl)phenoxy)butan-1-yl)-galanthamine
0.0039
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(4-(morpholinomethyl)phenoxy)hexan-1-yl)-galanthamine
0.0043
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(1-benzylpiperidin-4-yloxy)-butan-1-yl)-galanthamine
0.0055
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(1-benzylpiperidin-4-yloxy)-hexan-1-yl)-galanthamine
0.0056
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(4-(pyrrolidine-1-carbonyl)-phenoxy)butan-1-yl)-galanthamine
0.0058
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(3-(1-morpholinoethyl)phenoxy)hexan-1-yl)-galanthamine
0.0059
-
 pH 7.4, 37°C Rattus norvegicus galanthamine
0.0071
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(3-(1-morpholinoethyl)phenoxy)butan-1-yl)-galanthamine
0.0094
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(4-(pyrrolidine-1-carbonyl)-phenoxy)hexan-1-yl)-galanthamine
0.021
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(2-(4-(piperidin-1-ylmethyl)phenoxy)ethan-1-yl)-galanthamine
0.024
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(3-(4-(piperidin-1-ylmethyl)phenoxy)propan-1-yl)-galanthamine
0.028
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(4-(piperidin-1-ylmethyl)phenoxy)butan-1-yl)-galanthamine
0.029
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(5-(4-(piperidin-1-ylmethyl)phenoxy)pentan-1-yl)-galanthamine
0.033
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(4-(piperidin-1-ylmethyl)phenoxy)hexan-1-yl)-galanthamine
0.034
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(4-(4-((diethylamino)methyl)-phenoxy)butan-1-yl)-galanthamine
0.041
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(6-(4-((diethylamino)methyl)-phenoxy)hexan-1-yl)-galanthamine
0.053
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(8-(4-(piperidin-1-ylmethyl)phenoxy)octan-1-yl)-galanthamine
0.064
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(9-(4-(piperidin-1-ylmethyl)phenoxy)nonan-1-yl)-galanthamine
0.093
-
 pH 7.4, 37°C Rattus norvegicus 10-N-demethyl-10-N-(10-(4-(piperidin-1-ylmethyl)-phenoxy)decan-1-yl)-galanthamine