MAO-A Inhibitor

Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC₅₀s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression.

Apomorphine ((-)-Apomorphine) is a potent dopamine receptor agonist. Apomorphine also inhibit MAO-A and MAO-B. Apomorphine exerts neuroprotective effect and can relax rat corpus cavernosum. Apomorphine can inhibit ROS production, DNA fragmentation and inibit JNK and ERK1/2 phosphorylation. Apomorphine can enhance degradation of intracellular Aβ40 and Aβ42, reduces tau protein levels and inhibit MMP-9 expression. Apomorphine is a highly potent radical scavenger and iron chelator. Apomorphine can be used for the researches of dementia, parkinson's disease, alzheimer disease, breast carcinoma, and erectile dysfunction.

Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC₅₀ values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings.

Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with K_is of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities. Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 μM) over MAO-A (IC₅₀=580 μM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 μM) than at resting (IC₅₀=262 μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

Ro 41-1049 is a highly selective, reversible MAO-A inhibitor. Ro 41-1049 effectively blocks the Quinpirole (HY-B1752)-induced increase in dopamine D2-like receptor density in the nucleus accumbens and alters the pattern of behavioral sensitization, shifting animals' responses from enhanced motor activity to immobile self-directed gaping behavior. Tritium-labeled Ro 41-1049 serves as a high-affinity radioligand, enabling accurate mapping of the distribution and abundance of MAO-A in the central nervous system, peripheral organs, and human brain via quantitative enzyme autoradiography. Ro 41-1049 can be used for basic research on depression and other related diseases.

MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC₅₀ values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.

(trans)-m-Cl-PCA hydrochloride is a monoamine oxidase inhibitor, with an IC₅₀ of 0.55 μM against rat MAO-A and an IC₅₀ of 0.63 μM against MAO-B. (trans)-m-Cl-PCA hydrochloride inhibits the activities of MAO-A and MAO-B in rat brain mitochondria. (trans)-m-Cl-PCA hydrochloride can be used for the research of neurological disorders.

Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with K_is of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline hydrochloride has antihypertensive and anticancer activities. Pargyline (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC₅₀ of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.

Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 μM) over MAO-A (IC₅₀=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 μM) than at resting (IC₅₀=262 μM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.

Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC₅₀=0.74 μM, K_i=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer.

Xanthone is a monoamine oxidase A (MAO-A) inhibitor with an IC₅₀ of 0.84 µM. Xanthon inhibits Norepinephrine (HY-13715) and high-K⁺-induced vasoconstriction with IC₅₀ values of 60.26 μM and 82.9 μM, respectively. Xanthon increases intracellular cyclic adenosine 3′,5′-monophosphate (cAMP) content and blocks Ca²⁺ channels. Xanthone is the scaffold of several pharmacologically active compounds.

1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models.

Tedizolid phosphate (TR-701FA) is a MAO-A and MAO-B inhibitor with activity against Gram-positive bacteria.

Rubrofusarin gentiobioside (Rrubrofusarin-6-β-gentiobioside) is an orally active weak inhibitor of PTP1B and MAO-A (IC₅₀ >100 μM), and its glycosylation modification results in lower biological activity than its aglycone Rubrofusarin (HY-130307). Rubrofusarin gentiobioside promotes AMPK phosphorylation in an LKB1-independent manner and inhibits the mTOR signaling pathway, thereby downregulating the expressions of PPARγ, C/EBPα, as well as FAS, LPL and aP2. Rubrofusarin gentiobioside inhibits lipid accumulation, reduces body weight and epididymal white adipose tissue volume, improves fatty liver, and shows no cytotoxicity to hepatocytes. Rubrofusarin gentiobioside is widely used in obesity-related studies.

LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC₅₀ values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma.