|
Osavampator
Osavampator (developmental code names TAK-653 and NBI-1065845) is an experimental drug being investigated as a treatment for treatment-resistant depression. It is being developed by Takeda Pharmaceuticals (Millennium Pharmaceuticals, Inc.). Pharmacology Osavampator is a selective positive allosteric modulator (PAM) of the AMPA receptor. Osavampator and other AMPA PAMs potentiate the effects of agonists at the main site of the AMPA receptor by slowing the rate of desensitization and internalization of the receptor. The terminal half-life of osavampator is 33.1–47.8 hours. Research Depression There is evidence suggesting that activation of the AMPA receptor, downstream activation of mammalian target of rapamycin (mTOR), and upregulation of brain-derived neurotrophic factor (BDNF) are central to the antidepressant effects of certain NMDA receptor antagonists such as ketamine. Blockage of the AMPA receptor nullifies the antidepressant actions of ketamine in rodents. By potent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMPA Receptor
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic receptor, ionotropic glutamate receptor (iGluR) and predominantly sodium ion channel that mediates fast excitatory neurotransmission in the Central nervous system, central nervous system (CNS). Its activation by the neurotransmitter Glutamate (neurotransmitter), glutamate facilitates rapid neuronal communication, essential for various brain functions, including learning and memory. Its name is derived from the ability to be activated by the artificial glutamate analog AMPA. The receptor was initially named the "Quisqualic acid, quisqualate receptor" by Watkins and colleagues after the naturally occurring agonist quisqualic acid, quisqualate. Later, the receptor was designated as the "AMPA receptor" following the development of the selective agonist AMPA by Tage Honore and colleagues at the Royal Danish School of Pharmacy in Copenhagen. The ''GRIA2''- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drug
An experimental drug is a medicinal product (a drug or vaccine) that has not yet received drug approval, approval from governmental regulatory agency, regulatory authorities for routine use in human medicine, human or veterinary medicine. A medicinal product may be approved for use in one disease or condition but still be considered experimental for other diseases or conditions. United States In the United States, the body responsible for approval is the Food and Drug Administration (FDA), which must grant the substance Investigational New Drug (IND) status before it can be tested in human clinical trials. IND status requires the drug's sponsor to submit an IND application that includes data from laboratory and animal testing for drug safety, safety and efficacy. A drug that is made from a living organism or its products undergoes the same approval process but is called a biologics license application (BLA). Biological drugs include antibodies, interleukins, and vaccines. In 2018 f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor Antagonist
NMDA receptor antagonists are a class of drugs that work to receptor antagonist, antagonize, or inhibit the action of, the NMDA, ''N''-Methyl-D-aspartate receptor (NMDA receptor, NMDAR). They are commonly used as anesthetics for humans and animals; the state of anesthesia they induce is referred to as dissociative anesthesia. Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol, and ketobemidone. Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide (N2O), are sometimes used as recreational drugs, for their dissociative, hallucinogenic, and euphoriant properties. When used recreationally, they are classified as dissociative drugs. Uses and effects NMDA receptor antagonists induce a state called dissociative drug, dissociative anesthesia, marked by catalepsy, amnesia, and analgesia. Ketamine is a favored anesthet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocyclic Compounds With 2 Rings
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of pyridin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Antidepressants
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMPA Receptor Positive Allosteric Modulators
AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the AMPA receptor, receptor (AMPR), a type of ionotropic glutamate receptor which mediates most fast synaptic cleft, synaptic neurotransmission in the central nervous system. Medical applications AMPAR PAMs have cognition- and memory-enhancing and antidepressant-like effects in preclinical models. It has potential medical applications in the treatment of cognitive impairment (e.g., Schizophrenia#Cognitive dysfunction, cognitive symptoms in schizophrenia, mild cognitive impairment), dementia (e.g., Alzheimer's disease), depression (mood), depression, and for other indications. They can broadly be divided into low-impact and high-impact potentiators, with high-impact potentiators able to produce comparatively more robust increases in AMPAR activation. However, high-impact AMPAR PAMs can cause motor coordination motor disorder, disruptions, convulsions, and neurotoxicity at sufficiently high d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsion
A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is often used as a synonym for ''seizure''. However, not all epileptic seizures result in convulsions, and not all convulsions are caused by epileptic seizures. Non-epileptic convulsions have no relation with epilepsy, and are caused by non-epileptic seizures. Convulsions can be caused by epilepsy, infections (including a severe form of listeriosis which is caused by eating food contaminated by Listeria monocytogenes), brain trauma, or other medical conditions. They can also occur from an electric shock or improperly enriched air for scuba diving. The word ''fit'' is sometimes used to mean a convulsion or epileptic seizure. Signs and symptoms A person having a convulsion may experience several different symptoms, such as a brief blackout, confusion, drooling, l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Excitotoxicity
In excitotoxicity, neuron, nerve cells suffer damage or death when the levels of otherwise necessary and safe neurotransmitters such as glutamic acid, glutamate become pathologically high, resulting in excessive stimulation of cell surface receptor, receptors. For example, when glutamate receptors such as the NMDA receptor or AMPA receptor encounter excessive levels of the excitatory neurotransmitter, glutamate, significant neuronal damage might ensue. Different mechanisms might lead to increased extracellular glutamate concentrations, e.g. reduced uptake by glutamate transporters (EAATs), synaptic hyperactivity, or abnormal release from different neural cell types. Excess glutamate allows high levels of calcium in biology, calcium ions (Ca2+) to enter the cell (biology), cell. Ca2+ influx into cells activates a number of enzymes, including phospholipases, endonucleases, and proteases such as calpain. These enzymes go on to damage cell structures such as components of the cytoskel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Seizure
A seizure is a sudden, brief disruption of brain activity caused by abnormal, excessive, or synchronous neuronal firing. Depending on the regions of the brain involved, seizures can lead to changes in movement, sensation, behavior, awareness, or consciousness. Symptoms vary widely. Some seizures involve subtle changes, such as brief lapses in attention or awareness (as seen in absence seizures), while others cause generalized convulsions with loss of consciousness ( tonic–clonic seizures). Most seizures last less than two minutes and are followed by a postictal period of confusion, fatigue, or other symptoms. A seizure lasting longer than five minutes is a medical emergency known as status epilepticus. Seizures are classified as provoked, when triggered by a known cause such as fever, head trauma, or metabolic imbalance, or unprovoked, when no immediate trigger is identified. Recurrent unprovoked seizures define the neurological condition epilepsy. Clinical features Seizur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychostimulant
Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, mood, and physical performance. Some stimulants occur naturally, while others are exclusively synthetic. Common stimulants include caffeine, nicotine, amphetamines, cocaine, methylphenidate, and modafinil. Stimulants may be subject to varying forms of regulation, or outright prohibition, depending on jurisdiction. Stimulants increase activity in the sympathetic nervous system, either directly or indirectly. Prototypical stimulants increase synaptic concentrations of excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the receptors of excitatory neurotransmitters (e.g., nicotine) or by blocking the activity of endogenous agents that promote sleep (e.g., ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hallucinogen
Hallucinogens, also known as psychedelics, entheogens, or historically as psychotomimetics, are a large and diverse class of psychoactive drugs that can produce altered states of consciousness characterized by major alterations in thought, mood, and perception as well as other changes. Hallucinogens are often categorized as either being psychedelics, dissociatives, or deliriants, but not all hallucinogens fall into these three classes. Examples of hallucinogens include psychedelics or serotonin 5-HT2A receptor agonists like LSD, psilocybin, mescaline, and DMT; dissociatives or NMDA receptor antagonists like ketamine, PCP, DXM, and nitrous oxide; deliriants or antimuscarinics like scopolamine and diphenhydramine; cannabinoids or cannabinoid CB1 receptor agonists like THC, nabilone, and JWH-018; κ-opioid receptor agonists like salvinorin A and pentazocine; GABAA receptor agonists like muscimol and gaboxadol; and oneirogens like ibogaine and harmaline, a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketamine
Ketamine is a cyclohexanone-derived general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia, depression, and pain management. Ketamine exists as its S- (esketamine) and R- (arketamine) two enantiomers and has antidepressant action likely involving additional mechanisms than NMDA antagonism. At anesthetic doses, ketamine induces a state of dissociative anesthesia, a trance-like state providing pain relief, sedation, and amnesia. Its distinguishing features as an anesthestic are preserved breathing and airway reflexes, stimulated heart function with increased blood pressure, and moderate bronchodilation. As an anesthetic, it is used especially in trauma, Emergency medical services, emergency, and Pediatrics, pediatric cases. At lower, sub-anesthetic doses, it is used as a treatment for pain and treatment-resistant depression. Ketamine is legally used in medicine but is also tightly controlled due to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
