Target Validation Information
TTD ID T83011
Target Name Monoamine oxidase type B (MAO-B)
Type of Target
Successful
Drug Potency against Target Pargyline Drug Info Ki = 1800 nM [8]
Rasagiline Drug Info Ki = 700 nM [8]
Tranylcypromine Drug Info Ki = 16 uM
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholin-5-one Drug Info Ki = 74 nM [31]
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine Drug Info Ki = 130 nM [31]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one Drug Info Ki = 160 nM [31]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholine Drug Info Ki = 270 nM [31]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one Drug Info Ki = 3400 nM [31]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholine Drug Info Ki = 2170 nM [31]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one Drug Info Ki = 13600 nM [31]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholine Drug Info Ki = 3850 nM [31]
(+/-)-2-(4'-Propoxyphenyl)thiomorpholin-5-one Drug Info Ki = 1490 nM [31]
(+/-)-2-(4'-Propoxyphenyl)thiomorpholine Drug Info Ki = 980 nM [31]
(+/-)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 170 nM [28]
(+/-)-2-(4-fluorophenyl)-7-methylchroman-4-one Drug Info IC50 = 130 nM [28]
(+/-)-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 4410 nM [28]
(+/-)-2-(4-methoxyphenyl)-7-methylchroman-4-one Drug Info IC50 = 3350 nM [28]
(+/-)-2-p-tolylchroman-4-one Drug Info IC50 = 2070 nM [28]
(+/-)-2-Phenylthiomorpholin-5-one Drug Info Ki = 9580 nM [31]
(+/-)-2-Phenylthiomorpholine Drug Info Ki = 2230 nM [31]
(+/-)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 670 nM [28]
(+/-)-7-fluoro-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 170 nM [28]
(+/-)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 160 nM [28]
(+/-)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 3770 nM [28]
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 7180 nM [28]
(+/-)-7-methoxy-2-p-tolylchroman-4-one Drug Info IC50 = 550 nM [28]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info IC50 = 1470 nM [28]
(+/-)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 500 nM [28]
(+/-)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 3620 nM [28]
(6-Benzyloxy-2-naphthyl)-2-aminopropane Drug Info Ki = 2560 nM [20]
(6-Ethoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 13600 nM [20]
(6-Methoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 16300 nM [20]
(6-Propoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 13500 nM [20]
(7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile Drug Info IC50 = 230 nM [26]
(E)-5-(3-Chlorostyryl)isatin Drug Info Ki = 1400 nM [22]
(E)-5-(3-Fluorostyryl)isatin Drug Info Ki = 600 nM [22]
(E)-5-Styrylisatin Drug Info Ki = 310 nM [22]
(E)-6-Styrylisatin Drug Info Ki = 560 nM [22]
(E)-8-(3-chlorostyryl)-caffeine Drug Info Ki = 100 nM [25]
(R)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 200 nM [28]
(R)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 150 nM [28]
(R)(+)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 150 nM [28]
(R)(+)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 650 nM [28]
(R)(+)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 530 nM [28]
(R)(+)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 140 nM [28]
(R)-3-Prop-2-ynylamino-indan-5-ol Drug Info Ki = 17000 nM [8]
(R)-Indan-1-yl-methyl-prop-2-ynyl-amine Drug Info Ki = 600 nM [8]
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 800 nM [11]
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 110 nM [11]
(R)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 450 nM [11]
(R/R)BEFLOXATONE Drug Info Ki = 220 nM [1]
(S)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 160 nM [28]
(S)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 170 nM [28]
(S)(+)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 150 nM [28]
(S)(+)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 620 nM [28]
(S)(+)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 590 nM [28]
(S)(+)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 110 nM [28]
(S)-2-amino-1-(4-butylthiophenyl)-propane Drug Info Ki = 8925 nM [10]
(S)-2-amino-1-(4-propylthiophenyl)-propane Drug Info Ki = 14030 nM [10]
(S)-N2-[4-(benzyloxy)benzyl]alaninamide Drug Info IC50 = 260 nM [11]
(S)-N2-[4-(benzyloxy)benzyl]serinamide Drug Info IC50 = 410 nM [11]
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 33 nM [11]
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 43 nM [11]
(S)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 140 nM [11]
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 2200 nM [11]
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 1100 nM [11]
(S)-N2-{4-[(4-nitrobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 7010 nM [11]
1,2,3,4-Tetrahydro-naphthalen-1-ylamine Drug Info Ki = 720 nM [36]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 6.5 nM [6]
1,4-diphenyl-(1E,3E)-1,3-butadiene Drug Info Ki = 600 nM [8]
1-(4-(benzyloxy)phenyl)propan-2-amine Drug Info Ki = 710 nM [20]
1H-Indole-2,3-dione Drug Info Ki = 3000 nM [8]
2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole Drug Info Ki = 4.7 nM [5]
2-(2,4-dichlorophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 3980 nM [18]
2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 27 nM
2-(2-cyclohexylidenehydrazinyl)-4-p-tolylthiazole Drug Info IC50 = 3689 nM
2-(2-cyclohexylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 116 nM
2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 296 nM
2-(3-nitrophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 19270 nM [18]
2-(4,5-dihydro-1H-imidazol-2-yl)quinoline Drug Info IC50 = 13300 nM [18]
2-(4-chlorophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 5350 nM [18]
2-(4-fluorophenyl)-7-methoxy-4H-chromen-4-one Drug Info IC50 = 5140 nM [28]
2-(4-methoxyphenyl)-4H-chromene-4-thione Drug Info IC50 = 480 nM [28]
2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole Drug Info Ki = 1490 nM [18]
2-BFi Drug Info IC50 = 9100 nM [18]
2-Bromo-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 320 nM [30]
2-Bromo-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 1900 nM [30]
2-Chloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 1800 nM [30]
2-Chloro-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 6500 nM [30]
2-Furan-2-yl-4,5-dihydro-1H-imidazole Drug Info Ki = 2340 nM [4]
2-Hydrazino-3-methyl-4(3H)-quinazolinone Drug Info Ki = 18580 nM [19]
2-methyl-9H-indeno[2,1-d]pyrimidin-9-one Drug Info IC50 = 9400 nM [12]
2-oxo-N-m-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 600 nM [21]
2-oxo-N-p-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 710 nM [21]
2-oxo-N-phenyl-2H-chromene-3-carboxamide Drug Info IC50 = 760 nM [21]
2-p-tolyl-4,5-dihydro-1H-imidazole Drug Info Ki = 13090 nM [18]
2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 2380 nM [28]
2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 6690 nM [28]
2-Phenethyl-4,5-dihydro-1H-imidazole Drug Info Ki = 5 nM [4]
2-Phenoxymethyl-4,5-dihydro-1H-imidazole Drug Info Ki = 5 nM [4]
2-phenyl-9H-indeno[2,1-d]pyrimidine Drug Info IC50 = 13000 nM [12]
2-Phenyl-cyclopropylamine hydrochloride Drug Info IC50 = 19000 nM [7]
2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide Drug Info IC50 = 200 nM [26]
3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin Drug Info IC50 = 1.49 nM [15]
3,4-Benzo-7-acetonyloxy-8-methoxycoumarin Drug Info IC50 = 9360 nM [15]
3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 30 nM [35]
3-(2-Bromophenyl)-6-methylcoumarin Drug Info IC50 = 4300 nM [34]
3-(3-methoxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 0.8026 nM [24]
3-(4-hydroxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 155.59 nM [24]
3-(4-methoxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 13.05 nM [24]
3-(phenoxymethyl)-5H-indeno[1,2-c]pyridazin-5-one Drug Info IC50 = 2510 nM [12]
3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 330 nM [35]
3-phenyl-9H-indeno[1,2-e][1,2,4]triazin-9-one Drug Info IC50 = 6310 nM [12]
4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin Drug Info IC50 = 3870 nM [15]
4,9-Dihydro-3H-beta-carboline Drug Info Ki = 7.3 nM [6]
4-(2-oxo-2H-chromene-3-carboxamido)benzoic acid Drug Info IC50 = 1140 nM [21]
4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one Drug Info IC50 = 21 nM [26]
4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one Drug Info IC50 = 5570 nM [15]
4-oxo-4H-chromene-3-carboxylic acid Drug Info IC50 = 48 nM [32]
5-Aminomethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 4400 nM [1]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [5]
5-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 86 nM [5]
5-Hydroxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 2000 nM [1]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 300 nM [5]
5-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 84 nM [5]
5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE Drug Info IC50 = 13000 nM [33]
6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one Drug Info IC50 = 16530 nM [15]
6-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 2785 nM [5]
6-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 790 nM [5]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1640 nM [6]
6-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 480 nM [6]
7-(3-chlorobenzyloxy)-4-carboxaldehyde-coumarin Drug Info Ki = 400 nM [13]
7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin Drug Info IC50 = 17300 nM [15]
7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin Drug Info IC50 = 165 nM [15]
7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1290 nM [5]
7-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 400 nM [5]
7-fluoro-2-(4-fluorophenyl)-4H-chromene-4-thione Drug Info IC50 = 6890 nM [28]
7-fluoro-2-(4-methoxyphenyl)-4H-chromen-4-one Drug Info IC50 = 1340 nM [28]
7-fluoro-2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 4330 nM [28]
7-fluoro-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 1610 nM [28]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 12 nM [4]
7-methoxy-2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 11340 nM [28]
7-methoxy-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 7610 nM [28]
7-Methoxy-9H-beta-carboline Drug Info Ki = 87 nM [5]
7-methyl-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 6720 nM [28]
8-(3-Bromobenzyloxy)caffeine Drug Info Ki = 330 nM [29]
8-(3-Chlorobenzyloxy)caffeine Drug Info Ki = 230 nM [29]
8-(3-Fluorobenzyloxy)caffeine Drug Info Ki = 370 nM [29]
8-(3-Methoxybenzyloxy)caffeine Drug Info Ki = 1100 nM [29]
8-(3-Methylbenzyloxy)caffeine Drug Info Ki = 140 nM [29]
8-Benzyloxycaffeine Drug Info Ki = 430 nM [29]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 3.6 nM [5]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 17 nM [5]
8-Bromo-6-methyl-3-(4'-methoxyphenyl)coumarin Drug Info IC50 = 3230 nM [34]
8-Bromo-6-methyl-3-phenylcoumarin Drug Info IC50 = 11050 nM [34]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 270 nM [5]
8-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 160 nM [5]
8-[(3-Trifluoromethyl)benzyloxy]caffeine Drug Info Ki = 1300 nM [29]
9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [5]
Benzyl-methyl-[1-(1H-pyrrol-2-yl)-vinyl]-amine Drug Info Ki = 20 nM [2]
Butyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 1400 nM [3]
C-(1H-Indol-3-yl)-methylamine Drug Info Ki = 3440 nM [5]
CGS-19281A Drug Info Ki = 18 nM [6]
CHALCONE Drug Info IC50 = 1410 nM [23]
Cis-2-(4-chlorophenyl)-2-fluorocyclopropanamine Drug Info IC50 = 4800 nM [14]
Cis-2-(para-fluorophenyl)cyclopropylamine Drug Info IC50 = 10000 nM [14]
Cis-2-Fluoro-2-(4-methoxyphenyl)cyclopropylamine Drug Info IC50 = 18000 nM [14]
Cis-2-fluoro-2-phenylcyclopropanamine Drug Info IC50 = 19000 nM [14]
Cis-2-phenylcyclopropylamine Drug Info IC50 = 19000 nM [14]
CORDOIN Drug Info IC50 = 18760 nM [23]
Flavanone Drug Info IC50 = 2870 nM [28]
Heptyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 2000 nM [3]
HYDRAZINECARBOXAMIDE Drug Info IC50 = 6700 nM [7]
IPRONIAZIDE Drug Info IC50 = 7500 nM [30]
Isopropyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 19000 nM [3]
L-136662 Drug Info IC50 = 195 nM [33]
Lazabemide Drug Info Ki = 84 nM [8]
Methyl piperate Drug Info Ki = 1600 nM [27]
Methyl-(1,2,3,4-tetrahydro-naphthalen-1-yl)-amine Drug Info Ki = 1400 nM [36]
Methyl-pentyl-prop-2-ynyl-amine oxalic acid Drug Info IC50 = 370 nM [3]
MOFEGILINE Drug Info IC50 = 3.6 nM [17]
N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine Drug Info Ki = 1000 nM [16]
N-(1H-Indol-2-ylmethyl)-N-phenylamine Drug Info Ki = 320 nM [16]
N-(2-aminoethyl)-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 7680 nM [21]
N-(2-Methyl-1H-indol-5-yl)benzamide Drug Info Ki = 1650 nM [35]
N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide Drug Info Ki = 3000 nM [35]
N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 700 nM [9]
N-(2-Phenylethyl)-1H-indole-2-carboxamide Drug Info Ki = 190 nM [16]
N-(3-Phenylpropyl)-1H-indole-2-carboxamide Drug Info Ki = 800 nM [16]
N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 890 nM [21]
N-(4-Phenylbutyl)-1H-indole-2-carboxamide Drug Info Ki = 10000 nM [16]
N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 7200 nM [9]
N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 620 nM [9]
N-Benzyl,N-methyl-1H-indole-2-carboxamide Drug Info Ki = 1600 nM [16]
N-Benzyl-1H-indole-2-carboxamide Drug Info Ki = 120 nM [16]
N-benzyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 1960 nM [21]
N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine Drug Info Ki = 700 nM [16]
N-cyclohexyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 500 nM [21]
N-isobutyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 3270 nM [21]
N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 20 nM [9]
N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 20 nM [9]
N-Methyl,N-phenyl-1H-indole-2-carboxamide Drug Info Ki = 94 nM [16]
N-Methyl-N-phenyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 8890 nM [21]
N-Phenyl-1H-indole-2-carboxamide Drug Info Ki = 230 nM [16]
N2-[4-(benzyloxy)benzyl]glycinamide Drug Info IC50 = 3150 nM [11]
N2-{4-[(3-chlorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 340 nM [11]
N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 2240 nM [11]
N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 7100 nM [11]
N2-{4-[(4-nitrobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 9100 nM [11]
NSC-50187 Drug Info IC50 = 2200 nM [28]
NSC-93405 Drug Info IC50 = 12940 nM [28]
Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate Drug Info Ki = 1380 nM [18]
PIPERINE Drug Info Ki = 3190 nM [27]
PNU-22394 Drug Info Ki = 1030 nM [5]
TOLOXATONE Drug Info Ki = 15000 nM [1]
TRACIZOLINE Drug Info Ki = 2 nM [4]
Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine Drug Info IC50 = 3700 nM [14]
Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine Drug Info IC50 = 4900 nM [14]
Trans-2-fluoro-2-p-tolylcyclopropanamine Drug Info IC50 = 13000 nM [14]
Trans-2-fluoro-2-phenylcyclopropylamin Drug Info IC50 = 6400 nM [14]
TRYPTAMINE Drug Info Ki = 5400 nM [5]
TRYPTOLINE Drug Info Ki = 9.4 nM [4]
Action against Disease Model Phenelzine Drug Info In ongoing studies of the neuroprotective properties of monoamine oxidase inhibitors, we found that phenelzine provided robust neuroprotection in the gerbil model of transient forebrain ischemia, with drug administration delayed up to 3 h post reperfusion. Since ischemia-reperfusion brain injury is associated with large increases in the concentrations of reactive aldehydes in the pen uMbra area, we investigated if the hydrazine function of phenelzine was capable of sequestering reactive aldehydes. Both aminoaldehydes and acrolein are generated from the metabolism of polyamines to putrescine by polyamine oxidase. These toxic aldehydes in turn compromise mitochondrial and lysosomal integrity and initiate apoptosis and necrosis. Previous studies have demonstrated that pharmacological neutralization of reactive aldehydes via the formation of thioacetal derivatives results in significant neuroprotection in ischemia-reperfusion injury, in both focal and global ischemiamodels. In our studies of acrolein and 3-aminopropanal toxicity, using an immortalized retinal cell line, we found that aldehyde sequestration with phenelzine was neuroprotective. The neuroprotectionobserved with phenelzine is in agreement with previous studies of aldehyde sequestering agents in the treatment of ischemia-reperfusion brain injury and supports the concept that "aldehyde load" is amajor factor in the delayed cell losses of the ischemic pen uMbra. [37]
Rasagiline Drug Info It has demonstrated neuroprotective properties in laboratory studies. Current concepts of PD aetiopathogenesis include the role of alpha-synuclein, protein aggregation, free radical metabolism and mitochondrial dysfunction in contributing to cell death. We have used a combination of alpha-synuclein and free radical mediated toxicity in a dopaminergic cell line to provide a model of nigral toxicity in order to investigate the potential molecular mechanisms that mediate rasagiline protection. We demonstrate that rasagiline protects against cell death induced by the combination of free radicals generated by paraquat and either wild-type or A53T mutant alpha-synuclein over-expression. This protection was associated with a reduction in caspase 3 activation, a reduction insuperoxide generation and a trend to ameliorate the fall in mitochondrial membrane potential. Rasagiline induced an increase in cellular glutathione levels. The results support a role for rasagiline in protecting dopaminergic cells against free radical mediated damage and apoptosis in the presence of alpha-synuclein over-expression. The data are of relevance to the interpretation of the potentialmechanisms of action of rasagiline in explaining the results of disease modification trials in PD. [38]
Tranylcypromine Drug Info Glioblastoma multiforme (GBM) is a particularly aggressive brain t uMor and remains a clinically devastating disease. Pharmacologically inhibiting the lysine specific demethylase 1 with the monoamine oxidase inhibitor tranylcypromine, in combination with HDAC inhibitors, led to synergistic apoptotic cell death in GBM cells [39]
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