Catechol-O-Methyltransferase (COMT)

Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.

opicapone is a novel catechol-O-methyltransferase inhibitor

Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.

3-methoxy Tyramine (HCl) is a natural metabolite of dopamine, produced by catechol-O-methyltransferase (COMT).

Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation.

Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor.

Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.

Serotonin maleate acts as a selective agonist for 5-HT receptors in the central nervous system, influencing various physiological processes, including mood regulation and cognitive function. Additionally, it serves as a catechol O-methyltransferase (COMT) inhibitor with a Ki value of 44 μM, making it valuable for research involving neurotransmitter dynamics and the modulation of serotonergic pathways. Its multiple biological activities position it as a critical reagent for studies in neuroscience and pharmacology.

Serotonin-13C,D4 (5-Hydroxytryptamine-13C,D4) is a stable isotope-labeled form of serotonin, featuring carbon-13 and deuterium isotopes. As a monoamine neurotransmitter, it serves as an endogenous agonist of 5-HT receptors in the central nervous system (CNS). Additionally, Serotonin-13C,D4 acts as a catechol O-methyltransferase (COMT) inhibitor, demonstrating a Ki value of 44 μM. This reagent is valuable for research in neurobiology, pharmacology, and metabolic studies involving serotonin signaling and metabolism.

Tolcapone-d4 is a deuterated derivative of the selective catechol-O-methyltransferase (COMT) inhibitor, Tolcapone. This compound exhibits an IC50 of 773 nM, demonstrating its potency in inhibiting COMT activity. Tolcapone-d4 is utilized in research related to neurodegenerative disorders and cancer, as it influences α-synuclein and amyloid-beta oligomerization and fibrillogenesis. Additionally, it has been shown to induce oxidative stress, promote apoptosis in cancer cells, and increase reactive oxygen species (ROS) production, making it valuable for studies in both cancer and neurological disease contexts.

3-O-Methyltolcapone is a drug metabolite derived from Tolcapone, a selective and potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 of 773 nM. This compound is known to block α-synuclein and Aβ42 oligomerization and fibrillogenesis, while also inducing oxidative stress, apoptosis in cancer cells, and reactive oxygen species (ROS) production. Research applications include studies related to cancer and neurological disorders, particularly in the context of Parkinson’s disease and neuroblastoma.

3-O-Methyltolcapone-d4 is a deuterium-labeled metabolite of Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 of 773 nM. This compound is utilized in research focused on cancer and neurological disorders, including Parkinson's disease and neuroblastoma, due to its ability to inhibit α-synuclein and Aβ42 oligomerization, promote oxidative stress, and induce apoptosis in cancer cells. 3-O-Methyltolcapone-d4 provides a valuable tool for studying the metabolic pathways of Tolcapone and its therapeutic implications.

Tolcapone 3-β-D-glucuronide is a drug metabolite derived from Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT). While Tolcapone exhibits notable pharmacological activity, Tolcapone 3-β-D-glucuronide itself is pharmacologically inactive. Research indicates that Tolcapone plays a role in inhibiting α-synuclein and Aβ42 oligomerization, contributing to oxidative stress, cancer cell apoptosis, and reactive oxygen species (ROS) production. This metabolite is valuable for investigations into cancer mechanisms and neurological disorders, including Parkinson's disease and neuroblastoma.

3-BTD (3-Benzothiazole-daphnetin) is a two-photon fluorescence probe targeting Catechol-O-methyltransferase (COMT). It exhibits key biological activity by enabling the detection of endogenous COMT in living cells and tissue sections, making it a valuable tool for biological imaging applications. This compound aids in understanding the role of COMT in various physiological and pathological processes.

3-BTMD is a fluorescent compound generated through the action of the COMT enzyme on its substrate, 3-BTD, exhibiting an excitation wavelength of 390 nm and an emission wavelength of 510 nm. This reagent is primarily utilized in fluorescent labeling and imaging applications, facilitating the study of enzymatic activity and biomolecular interactions in various biological contexts. Its distinct fluorescence properties make it a valuable tool for researchers in the fields of biochemistry and molecular biology.

Serotonin-d4 is a deuterated form of serotonin that serves as a stable isotope for research applications. As a monoamine neurotransmitter in the central nervous system, serotonin is an endogenous agonist of 5-HT receptors. It also exhibits inhibitory activity against catechol O-methyltransferase (COMT) with a Ki of 44 μM. This compound is valuable for studies in neurobiology, pharmacology, and metabolic pathway analysis.

Serotonin-d4 hydrochloride is a stable isotope of the monoamine neurotransmitter serotonin (5-Hydroxytryptamine). It acts as an endogenous agonist at 5-HT receptors, playing a crucial role in CNS signaling. Additionally, serotonin-d4 hydrochloride serves as a catechol O-methyltransferase (COMT) inhibitor, exhibiting a Ki value of 44 μM. This reagent is valuable for studies investigating neurotransmitter dynamics, receptor interactions, and metabolic pathways in pharmacological and neurobiological research.

(R)-3-O-Methyldopa-d3 is a deuterated form of the R-enantiomer of 3-O-Methyldopa, which acts as a metabolite of L-DOPA. The compound exerts its biological activity by competitively inhibiting catechol-O-methyltransferase (COMT), thus influencing the pharmacological effects of both L-DOPA and dopamine. This stable isotope is essential for research applications involving metabolic pathways and neurological studies.

Comtifator is an integrated stress response pathway modulator that influences cellular responses to various stressors. This compound is essential for studying the role of the integrated stress response in diseases such as neurodegeneration and cancer. Its ability to alter stress signaling makes it a valuable tool for research investigating therapeutic interventions and mechanisms underlying stress-related disorders.

Neluxicapone is a potent inhibitor of catechol-O-methyltransferase (COMT), primarily utilized in the research of Parkinson's disease (PD). By inhibiting COMT, this compound enhances dopamine levels in the brain, which may alleviate motor symptoms associated with PD. Researchers can use neluxicapone to investigate its pharmacological effects and potential therapeutic benefits in neurodegenerative conditions.

5-Hydroxyferulic acid is a hydroxycinnamic acid derived from the phenylpropanoid pathway. It serves as a key precursor in the biosynthesis of sinapic acid and acts as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is utilized in various research applications focused on studying phenolic compounds and their roles in plant metabolism and health benefits.

Ro 41-0960 is a selective inhibitor of catechol-O-methyltransferase (COMT), which plays a crucial role in the metabolism of catecholamines. By inhibiting COMT, this compound enhances the levels of neurotransmitters such as dopamine, norepinephrine, and epinephrine. It is widely used in research to investigate the biochemical pathways of neurotransmission and to explore potential therapeutic applications in conditions such as Parkinson's disease and other neuropsychiatric disorders.

Nitecapone is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor. It exhibits notable gastroprotective and antioxidant properties by scavenging reactive oxygen and nitrogen species, thereby preventing lipid peroxidation. Nitecapone is valuable in research applications focusing on neurodegenerative diseases and other conditions where COMT modulation may play a therapeutic role.

3-O-Methyldopa monohydrate is a notable metabolite of L-DOPA, primarily interacting with catechol O-methyltransferase (COMT). It does not function as a substrate or inhibitor of L-amino acid decarboxylase, distinguishing it from its precursor. The inhibition of COMT by this compound may enhance the therapeutic effects of L-DOPA in Parkinson's disease, making it a valuable tool in neurological research and studies on Parkinson's treatments.

hMAO-B/MB-COMT-IN-1 is a dual inhibitor of human monoamine oxidase B (hMAO-B) and membrane-bound catechol-O-methyltransferase (MB-COMT), exhibiting IC50 values of 2.5 µM and 3.84 µM, respectively. This compound is effective in protecting cells from oxidative damage, making it a valuable tool for studying neurodegenerative diseases, including Parkinson's Disease. Its dual inhibition profile provides insights into the molecular mechanisms underlying these conditions and aids in the development of potential therapeutic strategies.

S-Adenosylhomocysteine sulfoxide is a potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. This compound is utilized in research to investigate the modulation of methylation reactions, providing valuable insights into biochemical pathways involving methyltransferases. Its inhibitory properties make it a significant tool for studies related to neurotransmitter metabolism and epigenetic regulation.

Entacapone-d10 is a deuterium-labeled version of Entacapone, a potent, reversible inhibitor of catechol-O-methyltransferase (COMT). This compound selectively inhibits COMT with IC50 values of 10 nM in rat brain, 20 nM in erythrocytes, and 160 nM in liver, demonstrating minimal interaction with other catecholamine metabolizing enzymes. Entacapone-d10 is utilized primarily in research related to Parkinson's disease and metabolic disorders, serving as an FTO demethylation inhibitor with an IC50 of 3.5 μM.

U-0521 is a selective inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound exhibits significant biological activity by modulating neurotransmitter levels, which is crucial for investigations into Parkinson's disease and related disorders. U-0521 is valuable for research focused on understanding the role of COMT in neurodegenerative conditions and for exploring potential therapeutic strategies targeting this pathway.

(Z)-Entacapone is a selective inhibitor of catechol-O-methyltransferase (COMT), crucial for catecholamine metabolism. This compound serves as a valuable tool in studying COMT's role in neurological disorders and drug metabolism. Additionally, it may appear as a potential impurity in commercial Entacapone preparations or as a degradation product due to UV light exposure, providing further relevance in quality control and biological research applications.

(E)-5-Hydroxyferulic acid is an isomer of the hydroxycinnamic acid class, functioning as a key intermediate in the phenylpropanoid pathway. It plays a crucial role as a precursor in the biosynthesis of sinapic acid and serves as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is important for studying metabolic pathways and the functions of phenolic compounds in various biological systems.

hMAO-B/MB-COMT-IN-2 is a potent dual inhibitor of hMAO-B and MB-COMT, exhibiting IC50 values of 4.27 μM and 2.69 μM, respectively. This compound effectively protects cells from oxidative damage, making it valuable for studies related to neurodegenerative diseases. hMAO-B/MB-COMT-IN-2 is particularly relevant in the research of conditions such as Parkinson’s Disease, offering insights into potential therapeutic strategies.

COMT-IN-1 is a potent catechol-O-methyltransferase (COMT) inhibitor, demonstrating an IC50 of 0.37 μM for COMT activity. This nitrophenolic analogue effectively inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 95.58 μM and 58.82 μM, respectively. With good blood-brain barrier permeability, COMT-IN-1 enhances dopamine levels and alleviates symptoms associated with MPTP-induced Parkinson's disease in murine models, making it a valuable tool for research into Parkinson's disease and dopamine metabolism.

CGP 28014 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound has been shown to lower homovanillic acid (HVA) levels and increase dihydroxyphenylacetic acid (DOPAC) levels in the striatum of rat models. CGP 28014 is valuable in research focused on the pathophysiology and potential treatment strategies for Parkinson's disease, providing insights into dopaminergic signaling and neurotransmitter dynamics.

BIA 3-335 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. Its primary mechanism disrupts the methylation of catechols, leading to increased levels of dopamine, which may be beneficial in the study of Parkinson's disease and related neurological disorders. This compound is widely used in research settings to explore therapeutic strategies aimed at enhancing dopaminergic signaling.

Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT), exhibiting an IC50 of 0.8 μg/ml. Isolated from the actinobacterium Streptomyces, Methylspinazarin demonstrates selectivity for COMT compared to tyrosine hydroxylase. This compound is valuable for research applications focused on neurotransmitter metabolism and the pharmacological modulation of catecholamine pathways.

Catechol O-methyltransferase (COMT), derived from porcine liver, is a methyltransferase that facilitates the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to the hydroxyl group of dopamine, resulting in the formation of 3-methoxytyramine. This enzyme exists in two forms: a soluble form (S-COMT) and a membrane-bound form (MB-COMT). COMT plays a critical role in regulating the levels of key neurotransmitters, including epinephrine, norepinephrine, and dopamine, making it essential for research related to neuropharmacology and psychiatric disorders.

Rosmarinic acid racemate acts as a monoamine oxidase inhibitor, specifically targeting the MAO-A and MAO-B enzymes as well as catechol-O-methyltransferase (COMT). It demonstrates inhibition with IC50 values of 50.1 μM for MAO-A, 184.6 μM for MAO-B, and 26.7 μM for COMT. This compound is useful in research applications focused on neurochemical regulation, mood disorders, and the modulation of catecholamine levels.

Serotonin is a monoamine neurotransmitter that acts as an endogenous agonist at 5-HT receptors. It plays a critical role in various physiological processes, including mood regulation and cognitive function. Additionally, serotonin functions as a catechol O-methyltransferase (COMT) inhibitor, exhibiting a Ki value of 44 μM. This compound is essential for studies related to neuroscience, pharmacology, and the understanding of mood disorders.