MCAT/MDMA/MET/MOP

MTD Introduction

Methadone, an organic compound with the chemical formula C21H27NO, is a μ-opioid receptor agonist, similar in potency to morphine, with analgesic effects, and can produce respiratory depression, pupil constriction, sedation, etc. Compared with morphine, it has a longer duration of action, less likely to produce tolerance, and low drug dependence. Compared with morphine, it has a longer duration of action, is not easy to produce tolerance, low drug dependence.In the early 1960s, it was found that this drug has the pharmacodynamic effect of treating heroin dependence detoxification and alternative maintenance therapy.

As an opioid agonist, it can be used in heroin addiction detoxification, called "methadone therapy". The pharmacological effects of methadone are qualitatively the same as those of morphine. It is characterized by a strong analgesic effect, a significant effect on the treatment of physical withdrawal symptoms of opioid addicts, a long-lasting effect, and repeated application is effective. It is suitable for the drug treatment of opioid addicts. Its sedative and respiratory inhibition, as well as the effect on smooth muscle and cardiovascular system is similar to morphine, but weaker than morphine.MTD has a strong analgesic effect, its efficacy is two to three times that of morphine, and its analgesic effect is slower and lasts for a longer period of time, which is suitable for chronic pain, and is a little bit poorer in the effect of acute pain. The hypnotic effect caused by a single dose is lighter than the equivalent dose of morphine, such as repeated application can cause obvious sedative effect. Methadone induces pupil dilation, cough suppressant effect and effect on pituitary hormones, which is the same as morphine in nature. Methadone slows gastrointestinal peristalsis, prolongs gastric emptying, increases the tension of intestinal smooth muscle at rest, and significantly reduces the propulsive activity of the rectum, which can lead to constipation. This is more common in methadone detoxification. Methadone has a respiratory inhibitory effect on the fetus in pregnancy, so it is not suitable for obstetric analgesia.

Figure 1 Structural formula of MTD

Introduction of ETG

Ethyl glucuronide (EtG) is also known as ethyl β-D-glucuronide. It is a widely used biochemical marker for detecting alcohol abuse behavior and can be detected in urine, blood, or hair.EtG is produced by the reaction of Glucuronide, which is produced in the liver, with alcohol. This reaction is secondary to the metabolism of alcohol and usually occurs when acetaldehyde is oxidized to acetic acid.The presence of EtG is a strong indicator of alcohol abuse because it can remain in the body for a long period of time after alcohol is consumed until the metabolism is complete.

 EtG testing has now become one of the revolutionary breakthroughs in detecting alcohol abuse. While traditional alcohol measurement tests (such as blood alcohol concentration tests or breathalyzer tests) can usually only detect the time it takes for the alcohol to disappear, the EtG test can detect alcohol abuse within the last few days or weeks.

EtG tests typically use urine samples because they are easier to obtain and more closely match alcohol intake in daily life situations. In addition, EtG can also be performed on blood and hair samples. Although urine tests are more common, blood and hair tests are more diagnostic because they can be used to detect alcohol abuse over a longer period of time. the advantage of the EtG test is that it eliminates the means many alcohol abusers often use to avoid alcohol testing, such as drinking "substitutes" such as soda or gum, scrubbing their mouths, sniffing perfume, or using a "substitute" such as a soda or gum. scrubbing the mouth, sniffing perfume, and so on.

Figure 2 ETG structure

Introduction to FTY

Multiple sclerosis (MS) is an autoimmune demyelinating and neurodegenerative disease of the central nervous system (CNS) and a major cause of non-traumatic neurological deficits in young people. Currently, three types of drugs are used to treat MS: immunomodulators, immunosuppressants, and anti-inflammatory drugs, but these drugs are not effective in the treatment of MS and have many side effects. Fingolimod is a new type of immunosuppressant, mainly used in the treatment of autoimmune diseases, and was approved by the FDA in 2010 for the treatment of multiple sclerosis. Fingolimod is an S1P inhibitor that blocks lymphocyte efflux from secondary lymphoid organs and prevents reactive lymphocytes from entering the central nervous system.

The targets of action of fingolimod include T cells, microglia, and other cells of the central nervous system. Fingolimod neuroprotective mechanisms are numerous, one of which is the regulation of S1P1 receptor triggers lymphatic homing, promotes the retention of lymphocytes in lymph nodes, and regulates immune function; the other is the down-regulation of fingolimod in combination with the expression of S1P1 receptor activates microglial cells, which results in the production of inflammatory factors in the brain tissue, such as TNF-α, IL-1β, and IL- 6, and the concomitant up-regulation of brain-derived neurotrophic factor and glial cell-derived microglial production of neurotrophic factors. Third, to protect the blood-brain barrier, phosphorylated fingolimod can down-regulate the level of S1P receptors on the surface of endothelial cells constituting the blood-brain barrier and reduce S1P-mediated chemotaxis. Fourthly, it inhibited the aggregation of inflammatory cells in the central nervous system, and significantly reduced the infiltration of neutrophils in the ischemic center and around the infarct foci and the activation of microglia and macrophages after cerebral ischemic injury; Fifthly, fingolimod may attenuate the autophagy process of glial cells, neuronal cells, and vascular endothelial cells of the central nervous system, etc.; and it may also attenuate the cerebral ischemic injury through non-immune effects.

Figure 3 Chemical structure of FTY

Introduction of K2

Vitamin K2 is also known as tetraenylmenaquinone, vitamin K2 is a collective name for a series of terpene side-chain compounds containing 2-methyl-1, 4-naphthoquinone parent nucleus and the C3 position with a varying number of isoprenoid structural units, which can be classified into K2(10), K2(20), K2(35), K2(40), and so on, according to the number of carbons on the terpene side-chain.

As a fat-soluble vitamin, K2 has a derivative of the naphthoquinone moiety of chlorophyll quinone bioactivity, and is one of the indispensable and important vitamins in the human body, and is the only biologically active form of vitamin K. It is mostly used for accelerating coagulation, maintaining clotting time, and treating hemorrhagic disorders caused by vitamin K deficiency.

Vitamin K2 is found only in fermented foods. It is actually formed by specific bacteria during the fermentation process. Certain bacteria in the intestines also produce Vitamin K2 in the body in a natural way. interestingly, Vitamin K1 in vegetables is difficult to absorb, but virtually all of the Vitamin K2 found in fermented foods can be easily absorbed by the body. Vitamin K2 can be categorized into two types: MK-4 (Methylnaphthoquinone-4), which is a short-chain form of vitamin K2 that is found in animal foods such as meat, dairy products, and eggs. MK-7 (Methylnaphthoquinone-7), which is a long-chain form of vitamin K2 from fermented foods.There are many different long-chain forms of vitamin K, but one of the most common is MK-7.

Vitamin K2 is a calcium navigator, guiding calcium into bones and teeth and away from soft tissues such as arteries, veins and skin. Guiding Calcium into the Bone: Vitamin K2 has the ability to help carboxylate primary osteocalcin secreted by osteoblasts into active osteocalcin, thus promoting the deposition of calcium ions in the bloodstream into the bone. If there is enough vitamin K2 in the body, osteocalcin can be activated. Activated osteocalcin has a unique affinity for calcium ions, which can draw calcium into the bone and cause calcium salts to be deposited, thus promoting bone mineralization. Vitamin K2 also activates another protein, matrix GLA protein (matrix gla protein (MGP)), which clears calcium from soft tissues such as arteries and veins. When vitamin K2 is deficient, these proteins cannot be activated and do not function.

Figure 4 Chemical structure of K2

Introduction to KET

In the human brain, dysfunction of the N-methyl-D-aspartate receptor (NMDA receptor) causes a variety of neurological disorders: if this receptor is over-inhibited, cognitive dysfunction, schizophrenia, and autoimmune encephalitis are manifested; if the receptor is over-activated, Alzheimer's disease, Parkinson's disease, epilepsy, cerebral ischemic injury, chronic pain, and depression result.

Ketamine (KET), whose full name is 2-o-Chlorophenyl-2-methylaminocyclohexanone, is a derivative of phenylcyclohexylpiperidine (PCP). It is commonly known as ketamine hydrochloride. As a blocker of NMDA receptor, an important glutamate-gated ion channel in the brain, it can be involved in the regulation of synaptic transmission and synaptic plasticity signaling pathway by inhibiting NMDA receptor channel activity, and then restore the synaptic damage in the cortex and hippocampal region caused by chronic stress.

Figure 4 Structural formula of KET

KMD Bioscience is a high-tech enterprise specializing in the sales and technical consulting of in vitro diagnostic reagent raw materials - antigens, antibodies, quality control products, etc., as well as import agency services. KMD Bioscience's antibody diagnostic raw materials and antigen diagnostic raw materials are strictly monitored during the R&D and production phases, and the performance indicators (specificity, activity, stability, etc.) of antibodies/antigens are analyzed to ensure that IVD raw materials are characterized by small batch-to-batch/intra-batch variations, wide linear ranges, good stability, high sensitivity, and so on.

The inventory of reagents associated with K2 and KET that KMD Bioscience can offer: