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(6R)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
(6R)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
(6S)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
(6S)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
(7-nitro-1,2,3,4-tetrahydroisoquinolin-3-yl)methanol
-
-
(R)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
(R)-7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
-
(S)-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
1,2,3,4-tetrahydrobenz[h]isoquinoline
1,2,3,4-tetrahydroisoquinoline
1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid
-
-
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
1,4-diaminonaphthalene-2,6-disulfonic acid
-
-
1-(2,3-dichlorophenyl)ethanamine
-
-
1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)ethanone
-
-
1-aminoisoquinoline
-
Kd: 14 microM
1-thiophen-2-ylmethanamine
-
-
1-thiophen-3-ylmethanamine
-
-
2,3,4,5-tetrahydro-1H-2-benzazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzodiazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzothiazepine
-
-
2,3,4,5-tetrahydro-5H-1,4-benzoxazepine
-
-
2,3-dichloro-alpha-methylbenzylamine
-
2,5-Dimethyl-1-aminobenzimidazole
2-amino-1-methylbenzimidazole
-
Kd: 4.6 microM
2-amino-4(7)-hydroxy-benzimidazole
-
Kd: 20 microM
2-amino-5(6)-chloro-7(4)-hydroxy-benzimidazole
-
Kd: 14 microM
2-amino-5(6)-chloro-benzimidazole
-
Kd: 1.8 microM
2-amino-5(6)-fluoro-benzimidazole
-
Kd: 7.2 microM
2-aminobenzimidazole
-
Kd: 6.3 microM
2-Aminotetralin
-
most effective inhibitor
2-bromo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-chlorophenylethanolamine
-
-
2-fluorophenylethanolamine
-
-
2-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
2-thiophen-2-ylethanamine
-
-
3,4-Dichlorophenylethanolamine
3,4-dichlorophenylethylenediamine
-
substrate inhibition
3,4-dihydroxyphenylethanolamine
-
-
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
very high selectivity
3-(fluoromethyl)-7-(thiomorpholin-4-ylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-(fluoromethyl)-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-(fluoromethyl)-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
very high selectivity
3-(fluoromethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
3-(trifluoromethyl)-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
-
3-bromophenylethanolamine
-
-
3-butyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(ethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-2,2,2-trifluoroethylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-3-methoxypropylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(N-4-nitrophenylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-(propylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-difluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-ethyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-ethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-ethyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-fluoromethyl-7-(2,2,2-trifluoroethylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(3,3,3-trifluoropropylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(4,4,4-trifluorobutylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(4-chlorobenzylsulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-(N-benzylaminosulfonyl)-1,2,3,4-tetrahydrosioquinoline
-
-
3-fluoromethyl-7-(N-methylaminosulfonyl)-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-azido-1,2,3,4-tetrahydrosioquinoline
-
-
3-fluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
3-fluoromethyl-7-isothiocyanato-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-methanesulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-propylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
3-fluoromethyl-7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-[N-(4-chlorophenyl)aminosulfonyl]-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-hydroxymethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-hydroxypropyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
extension of the 3-hydroxyalkyl chain by just one carbon results in a significant loss in phenylethanolamine N-methyltransferse inhibitory potency
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-isopropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-methyl-1,2,3,4-tetrahydroisoquinoline
3-methyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-methyl-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
-
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
3-methyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-propyl-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
3-propyl-N-(2,2,2-trifluoroethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
moderate selectivity
3-thienylmethylamine
-
inhibits the enzyme and is selective toward the alpha2-adrenoceptor
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines
-
several 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines and some enantiomers of 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines. For the phenylethanolamine N-methyltransferase inhibitory potency of different 3-trifuoromethyl-1,2,3,4-tetrahydroisoquinolines, compounds bearing a lipophilic 7-substituent show higher potency than compounds bearing a hydrophilic 7-substituent. Comparison to the inhibitory activity of the entantiomers of the most potent racemates show that the R-enantiomers are approximately 4fold as potent as their corresponding S-enantiomers.
-
3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-7-cyano-1,2,3,4-tetrahydroisoquinoline
-
-
3-trifluoromethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
-
4-(benzo[d][1,3]dioxol-5-ylamino)-4-oxobutanoic acid
-
-
4-bromo-1H-imidazole
-
Kd: 170 microM
4-bromophenylethanolamine
-
-
4-fluorophenylethanolamine
-
-
4-hydroxyphenylethanolamine
-
-
4-oxo-1,4-dihydroquinoline-3,7-dicarboxylic acid
-
-
4-quinolinol
-
Kd: 690 microM
5,6-Dichloro-2-aminotetralin
-
0.00093 mM, 50% inhibition, competitive with norepinephrine as substrate
5-chlorobenzimidazole
-
Kd: 97 microM
6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-Aminoquinoline
-
Kd: 380 microM
6-Chloropurine
-
Kd: 140 microM
6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
-
6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
7-(3-methoxypropylsulfonyl)-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-(N-4-chlorophenylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-(N-butylaminosulfonyl)-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-acetamido-1,2,3,4-tetrahydroisoquinoline
-
-
7-allylsulfonyl-1,2,3,4-tetrahydrosioquinoline
-
-
7-aminocarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-aminomethyl-1,2,3,4-tetrahydroisoquinoline dihydrochloride
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-aminosulfonyl-1,2,3,4-tetrahydroisoquinoline
-
i.e. SK&F 29661
7-aminosulfonyl-3-difluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-benzoyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-benzyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenzo[h]isoquinoline
-
7-bromo-1,2,3,4-tetrahydroben[h]isoquinoline is 2fold more potent as an inhibitor of phenylethanolamine N-methyltransferase than 1,2,3,4-tetrahydroben[h]isoquinoline.
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-bromo-1,2,3,4-tetrahydroisoquinoline
7-bromo-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
7-bromo-3-butyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-ethyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-hydroxyethyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-3-hydroxypropyl-1,2,3,4-tetrahydroisoquinoline
-
little selcetivity
7-bromo-3-isopropyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
7-bromo-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-bromo-N-triphenylmethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-butylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-ethylsulfonyl-3-fluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline oxalate
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfinyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylsulfonyl-3-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-methylthio-1,2,3,4-tetrahydroisoquinoline
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
7-nitro-1,2,3,4-tetrahydroisoquinoline
7-nitro-3-pentyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-nitro-3-propyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
7-trichloromethylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
D-norepinephrine
-
substrate inhibition
dopamine
-
competitive inhibition with respect to phenylethanolamine
human cerebrospinal fluid
-
-
-
L-norepinephrine
-
substrate inhibition
methanol
-
at nonsaturating concentrations of phenylethanolamine, methanol inhibits in a competitive fashion. With respect to S-adenosyl-L-methionine inhibition by methanol is noncompetitive
N-(4-chlorophenyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
N-(4-chlorophenyl)-3-(fluoromethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
N-(4-chlorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
octopamine
-
at high concentrations
p-hydroxymercuribenzoate
-
0.00001 mM, 75% loss of activity
phenylethanolamine
-
at high concentrations
Phenylethylamine
-
competitive inhibition with respect to phenylethanolamine
R-(+)-7-bromo-3-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline
-
-
SKF 64139
1,2,3,4-tetrahydroisoquinoline derivate with two chloro substituents on the aromatic ring. Is able to cross the blood-brain barrier.
trans-(1S,2S)-2-amino-1-tetralol
-
tyramine
-
at high concentrations
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
the inhibitor forms hydrophobic interactions with Val53, Met258, Val272, and Val269 in the PNMT active site, binding site structure, overview
1,2,3,4-tetrahydrobenz[h]isoquinoline
-
the inhibitor forms hydrophobic interactions with Val53, Met258, Val272, and Val269 in the PNMT active site, binding site structure, overview
1,2,3,4-tetrahydroisoquinoline
-
a nonselective inhibitor
1,2,3,4-tetrahydroisoquinoline
-
-
1,2,3,4-tetrahydroisoquinoline
-
a nonselective inhibitor
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
high selectivity
1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
-
2,5-Dimethyl-1-aminobenzimidazole
-
-
2,5-Dimethyl-1-aminobenzimidazole
-
-
3,4-dichloroamphetamine
-
3,4-dichloroamphetamine
-
-
3,4-Dichlorophenylethanolamine
-
substrate inhibition
3,4-Dichlorophenylethanolamine
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-fluoromethyl-7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-hydroxyethyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
3-hydroxypropyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
extension of the 3-hydroxyalkyl chain by just one carbon results in a significant loss in phenylethanolamine N-methyltransferse inhibitory potency
3-methyl-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
high selectivity
3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
-
-
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
i.e. SK&F 64139
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-aminosulfonyl-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-bromo-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-1,2,3,4-tetrahydroisoquinoline
-
-
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
moderate selectivity
7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-cyano-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-hydroxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
7-iodo-1,2,3,4-tetrahydroisoquinoline
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-methoxy-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydrobenz[h]isoquinoline hydrochloride
-
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
little selectivity
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
-
7-nitro-1,2,3,4-tetrahydroisoquinoline
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
-
7-sulfonamido-1,2,3,4-tetrahydroisoquinoline
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
-
8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine
i.e. LY 134046
epinephrine
-
-
epinephrine
-
noncompetitive with normetanephrine as substrate
epinephrine
-
isoenzyme E2, noncompetitive inhibitor of S-adenosyl-L-methionine
LY134046
-
selective inhibitor, IC50: 0.0019 mM
LY134046
2,3,4,5-tetrahydro-1H-2-benzyzepine derivate with two chloro substituents on the aromatic ring. Is able to cross the blood-brain barrier.
norepinephrine
-
noncompetitive inhibition with phenylethanolamine as substrate, competitive inhibition with normetanephrine as substrate
norepinephrine
-
4 distinct substrate inhibition patterns: enzyme form E1 is not subject to substrate inhibition, isoenzyme E-2 is inhibited by S-adenosyl-L-methionine and norepinephrine, isoenzyme E-3 and E-4 are inhibited by norepinephrine only, isoenzyme E5 is inhibited only by S-adenosyl-L-methionine
norepinephrine
-
at high concentrations
PCMB
-
-
PCMB
-
0.01 mM, complete inhibition
S-adenosyl-L-methionine
-
substrate inhibition
S-adenosyl-L-methionine
-
4 distinct substrate inhibition patterns: enzyme form E1 is not subject to substrate inhibition, isoenzyme E-2 is inhibited by S-adenosyl-L-methionine and norepinephrine, isoenzyme E-3 and E-4 are inhibited by norepinephrine only, isoenzyme E5 is inhibited only by S-adenosyl-L-methionine
S-adenosylhomocysteine
-
competitive
S-adenosylhomocysteine
-
-
SKF 29661
1,2,3,4-tetrahydroisoquinoline derivate
additional information
-
7-substituted-1,2,3,4-tetrahydroisoquinolines are potent inhibitors, unfortunately, most of these compounds also exhibit a strong affinity for the alpha2-adrenoreceptor
-
additional information
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inhibitor docking studies, molecular modelling; the addition of a 7-substituent (NO2, SO2NH2, OMe, OH, or CN) to 1,2,3,4-tetrahydroben[h]isoquinoline does not lead to an increase in phenylethanolamine N-methyltransferase inhibitory potency.
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additional information
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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.
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additional information
the series of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines is more lipophilic but less potent than the correspnding sulfonamides. The interaction of the human phenylethanolamnie N-methyltransferase main chain carbonyl oxygen of Asn39 with the sulfonamide -NH- is likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfones.
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additional information
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the series of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines is more lipophilic but less potent than the correspnding sulfonamides. The interaction of the human phenylethanolamnie N-methyltransferase main chain carbonyl oxygen of Asn39 with the sulfonamide -NH- is likely responsible for much of the enhanced inhibitory potency of the sulfonamides versus the sulfones.
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additional information
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importance of protein flexibility in structure-based inhibitor design
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additional information
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inhibitor docking studies, molecular modelling
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2.1.1.28 phenylethanolamine N-methyltransferase
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