Application | Comment | Organism |
---|---|---|
additional information | selective inhibitors of phenylethanolamine N-methyltransferase would be useful pharmacological tools for clearly defining the connection between central epinephrine concentrations and peripheral blood pressure | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
human phenylethynolamine N-methyltransferase with a C-terminal hexahistidine tag is expressed in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-(ethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-(N-2,2,2-trifluoroethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-(N-3-methoxypropylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-(N-4-nitrophenylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-(propylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
3-difluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
7-(N-4-chlorophenylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
7-(N-butylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
7-aminosulfonyl-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | - |
Homo sapiens | |
additional information | the rank order of phenylethanolamine N-methyltransferase inhibitory potency for the analysed 3,7-disubstituted-1,2,3,4-tetrahydroisoquinoline is CH2F equal to CHF2 decreases to CF3. The 3-difluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines have the proper balance of steric and pKa properties, they are both potent inhibitors of phenylethanolamine N-methyltransferase and highly selective due to low affinity for the alpha2-adrenoceptor. | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
PNMT | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000067 | - |
3-difluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.000094 | - |
3-difluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.00017 | - |
3-difluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0002 | - |
3-difluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.00025 | - |
3-difluoromethyl-7-(N-2,2,2-trifluoroethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.00068 | - |
7-aminosulfonyl-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0009 | - |
7-(N-4-chlorophenylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0021 | - |
3-difluoromethyl-7-(propylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0031 | - |
3-difluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0032 | - |
3-difluoromethyl-7-(ethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0034 | - |
3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0053 | - |
3-difluoromethyl-7-(N-3-methoxypropylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.0056 | - |
7-(N-butylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.006 | - |
3-difluoromethyl-7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens | |
0.037 | - |
3-difluoromethyl-7-(N-4-nitrophenylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline | radiochemical assay, inhibition constants are determined using four concentrations of phenylethanolamine as the variable substrate, and three concentrations of inhibitor | Homo sapiens |