Table 3.

MAOB Inhibitors

Name	Chemo-Structure	IC50 for MAOB	Description	Ref.
MAO-B inhibitor 1		0.02 nM	Effective, reversible, orally active, and selective with blood-brain barrier (BBB) permeability	[79]
MAO-B inhibitor 2		1.33 nM	Effective, reversible, orally active, and selectively permeable across the BBB	[79]
MAO-B inhibitor 4		8.3 nM	Selective, anti-neuroinflammation with lower neurotoxicity. With Inhibiting the release of NO, TNF-α, and IL-1β induced by LPS and Aβ1-42 stimulation, and attenuating Aβ(1–42) induced cytotoxicity	[25]
MAO-B inhibitor 5		67.3 nM	Reversibility, permeability to the BBB	[26]
MAO-B inhibitor 6		0.11 μM	Penetrate the BBB, highly selective, reversible, and competitively antioxidant and neuroprotective effects	[27]
MAO-B-IN-1		10 μM	Effective	[28]
CA/MAO-B-IN-1		7.0 nM	Dual inhibitors of CA and MAOB	[29]
hMAO-B-IN-4		33.82 μM	Selective, reversible, able to penetrate the BBB	[30]
hMAO-B-IN-5		0.11 µM	BBB penetration, Multitarget inhibitors for acetylcholinesterase (AChE and BChE) and MAO-B	[30]
hMAO-B-IN-7		0.79±0.05 μM	Validity, ability to penetrate the BBB	[31]
hMAO-B-IN-9		1.58µM	Non-competitive inhibitor of MAOB with BBB permeability	[32]
MAO-B-IN-9		0.18 μM	Effective, selective, BBB-permeable, irreversible, time-dependent MAOB inhibitor, which prevents Aβ1-42 induced neuronal cell death and possess neuroprotective effects	[33]
MAO-B-IN-10		NA	Effective, selective, and capable of crossing the BBB	[34]
hMAO-B-IN-11		0.11 µM	Selective and reversible inhibition for MAOB, with suppressing pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia	[35]
MAO-B-IN-11		1.3 μM	Effective	[36]
MAO-B-IN-12		1.3 μM	Effective	[36]
MAO-B-IN-14		0.95 μM	Effective Selective	[37]
MAO-B-IN-16		1.55 µM	Effective Selective	[38]
MAO-B-IN-17		5.08 μM	Effective Selective	[38]
MAO-B-IN-27		NA	Effective Selective	[39]
MAO-B-IN-28		1.9±0.5 nM	An effective hMAO-B inhibitor	[40]
MAO-B-IN--31		41 nM	Effective, selective, and capable of inhibiting α-syn and tau aggregation	[41]
MAO-B-IN-33		0.021 μM	Effective Reversible Selective	[42]
MAO-B-IN-34		NA	Effective	[43]
MAO-B-IN-35		1.02 μM	Effective Reversible Selective	[44]
MAO-B-IN-37		270 nM	Selective, with good metabolic stability in mouse microsomes and demonstrated good affinity with human serum albumin	[45]
MAO-B-IN-39		3.61 μM	Effective	[46]
MAO-B-IN-42		0.184 μM	Effective Reversible Selective	[47]
MAO-B-IN-44		1.01 μM	Effective, selective	[48]
Monoamine oxidase/Aromatase-IN-1		39 nM	Efficient	[49]
Lazabemide		0.03 μM	Effective Reversible Selective	[50]
Homopterocarpin		0.72 μM	Competitive Reversible	[51]
4-Hydroxyderricin		3.43 μM	The main active ingredient of Angelica keiskei Koidzum, orally active, selectively effective, with anti-depressant, anti-allergic, anti-diabetic, antioxidant, and anti-tumor effects	[52]
Acacetin 7-O-(6-O-malonylglucoside)		1.87 μM	Effective Reversible	[53]
WAY-620147		55 μM	Effective	[54]
1,4-Naphthoquinone		NA	With broad-spectrum inhibitory activity can target DNA polymerase, NF-κB, and MAOA/B, and it possess antibacterial, biofilm formation activity, used for antibacterial, antitumor, and anti-inflammatory research	[55]
Ladostigil		37.1 μM	Oral effective, dual inhibitors of cholinesterase and MAOB, with neuroprotective, antioxidant, and anti-inflammatory effects, and can be used for research in depression and Alzheimer’s disease	[56]
1-Methyl-2-undecyl-4(1H)-quinolone		15.3 μM	Effective Irreversible Selective	[57]
RO 16−6491 free base		NA	Selective, reversible with high affinity and specificity for binding sites on human frontal cortical mitochondria and platelet membranes	[58]
Safinamide		0.098 μM	Effective, selective, reversible inhibitor of MAOB, which also blocks sodium channels and regulates the release of glutamate, exhibits neuroprotective effects	[59]
1-Methyl-2-nonyl-4(1H)-quinolone		12.1μM	A type of quinolone alkaloid, which is an effective and selective MAO-B inhibitor	[60]
J147		NA	Very effective Oral	[61]
SL-25.1188		NA	Effective	[62]
Desmethoxyyangonin		0.123 µM	A selective MAOB inhibitor that can inhibit the Jak2/STAT3 and IKK signaling pathways to exert anti-inflammatory effects	[63]
Sembragiline		NA	A potent, selective, and reversible MAOB inhibitor	[64]
NW-1689		NA	A highly selective and reversible MAOB inhibitor that also blocks sodium channels and N-type calcium channels	[65]
(E)-8-(3-Chlorostyryl)caffeine		NA	A selective adenosine A2A receptor antagonist, inhibiting MAOB. with an independent pathway of its action on A2A receptors	[66]
PSB-1434		1.59 nM	Highly selective	[44]
PSB-1491		0.386 nM	Selectivie Competitive	[44]
Methyl citrate		0.23 mM	Effective	[67]
NW-1772		NA	Effective Selective BBB permeability	[68]
(E/Z)-J147		1.88 μM	An extremely effective oral active neuroprotectant that can enhance cognitive abilities. It can easily cross the BBB, with inhibiting MAO B and dopamine transporter.	[69]
Pargyline		0.5 μM	An irreversible MAOB inhibitor with antihypertensive and anticancer activity	[70]
Norharmane		4.7 μM	A type of β-carboline alkaloid, effective, reversible MAO inhibitor	[71]
Rasagiline		4.43 nM	Efficient, irreversible selective MAO inhibitor	[72]
Rasagiline mesylate		4.43 nM	Efficient, irreversible selective MAO inhibitor	[73]
OG-L002		0.02 μM	An effective MAO inhibitor	[74]
Tranylcypromine hydrochloride		0.95 μM	Lysine-specific demethylase 1 (LSD1/BHC110), irreversible inhibitor of MAO	[75]
2,6-Dimethoxybenzylamine hydrochloride		190 μM	Effective Reversible	[76]
PSB-1410		Human MAOB IC50=0.23 nM rat MAOB, IC50=1.01 nM	Effective Selective Competitive	[76]
MAO-IN-1		20 nM	Effective	[77]