DA-Phen
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DA-Phen
DA-Phen, also known as dopamine–phenylalanine conjugate, is a synthetic dopamine prodrug which is under preclinical evaluation. Dopamine itself is hydrophilic and is unable to cross the blood–brain barrier, thus showing peripheral selectivity. DA-Phen was developed as a dopamine prodrug that would allow for entry into the central nervous system via passive diffusion and/or active transport. DA-Phen is a conjugate of dopamine and the amino acid phenylalanine (Phe or Phen). It is slowly cleaved by brain enzymes ( t½ = 460minutes) to yield free dopamine but is also rapidly hydrolyzed in human blood plasma (t½ = 28minutes). The drug was intended as a prodrug but may also directly interact with the dopamine D1-like and/or D2-like receptors. DA-Phen has shown centrally mediated effects in animals, including increased cognitive flexibility, improved spatial learning and memory, antidepressant- and anxiolytic-like effects, and decreased ethanol intake. Other analogues, such ...
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Neurotransmitter Prodrug
A neurotransmitter prodrug, or neurotransmitter precursor, is a drug that acts as a prodrug of a neurotransmitter. A variety of neurotransmitter prodrugs have been developed and used in medicine. They can be useful when the neurotransmitter itself is not suitable for use as a pharmaceutical drug owing to unfavorable pharmacokinetic or physicochemical properties, for instance high susceptibility to metabolism, short elimination half-life, or lack of blood–brain barrier permeability. Besides their use in medicine, neurotransmitter prodrugs have also been used as recreational drugs in some cases. Monoamine prodrugs Monoamine neurotransmitter prodrugs include the catecholamine precursors and prodrugs L-phenylalanine, L-tyrosine, L-DOPA (levodopa), L-DOPS (droxidopa), dipivefrine (''O'',''O'''-dipivalylepinephrine), and dibutepinephrine, as well as the serotonin and melatonin precursors and prodrugs L-tryptophan and L-5-hydroxytryptophan (5-HTP; oxitriptan). Other dopamin ...
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Terminal Half-life
Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration ( Cmax) to half of Cmax in the blood plasma. It is denoted by the abbreviation t_. This is used to measure the removal of things such as metabolites, drugs, and signalling molecules from the body. Typically, the biological half-life refers to the body's natural detoxification (cleansing) through liver metabolism and through the excretion of the measured substance through the kidneys and intestines. This concept is used when the rate of removal is roughly exponential. In a medical context, half-life explicitly describes the time it takes for the blood plasma concentration of a substance to halve (''plasma half-life'') its steady-state when circulating in the full blood of an organism. This measurement is useful in medicine, pharmacology and pharmacokinetics because it helps determi ...
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Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ...
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Alcohol (drug)
Alcohol, sometimes referred to by the chemical name ethanol, is the active ingredient in alcoholic drinks such as beer, wine, and distilled spirits (hard liquor). Alcohol is a central nervous system (CNS) depressant, decreasing Action potential, electrical activity of neurons in the brain, which causes the characteristic effects of alcohol intoxication ("drunkenness"). Among other effects, alcohol produces euphoria, anxiolytic, decreased anxiety, increased sociability, sedation, and impairment of cognitive, memory, motor control, motor, and sense, sensory function. Alcohol has a variety of adverse effects. Short-term effects of alcohol consumption, Short-term adverse effects include generalized impairment of neurocognitive function, dizziness, nausea, vomiting, and symptoms of hangover. Alcohol is addiction, addictive and can result in alcohol use disorder, Substance dependence, dependence, and Alcohol withdrawal syndrome, withdrawal upon cessation. The long-term effects of ...
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Anxiolytic
An anxiolytic (; also antipanic or anti-anxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and response. When anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses, such as defensive behaviors, high levels of alertness, and negative emotions. Those with anxiety disorders may have concurrent psychological disorders, such as depression. Anxiety disorders are classified using six possible clinical assessments: Different types of anxiety disorders will share some general symptoms while having their own distinctive symptoms. This explains why people with different types of anxiety disorders will respond differently to diffe ...
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Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ...
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Memory
Memory is the faculty of the mind by which data or information is encoded, stored, and retrieved when needed. It is the retention of information over time for the purpose of influencing future action. If past events could not be remembered, it would be impossible for language, relationships, or personal identity to develop. Memory loss is usually described as forgetfulness or amnesia. Memory is often understood as an informational processing system with explicit and implicit functioning that is made up of a sensory processor, short-term (or working) memory, and long-term memory. This can be related to the neuron. The sensory processor allows information from the outside world to be sensed in the form of chemical and physical stimuli and attended to various levels of focus and intent. Working memory serves as an encoding and retrieval processor. Information in the form of stimuli is encoded in accordance with explicit or implicit functions by the working memory p ...
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Spatial Learning
In cognitive psychology and neuroscience, spatial memory is a form of memory responsible for the recording and recovery of information needed to plan a course to a location and to recall the location of an object or the occurrence of an event. Spatial memory is necessary for orientation in space. Spatial memory can also be divided into egocentric and allocentric spatial memory. A person's spatial memory is required to navigate in a familiar city. A rat's spatial memory is needed to learn the location of food at the end of a maze. In both humans and animals, spatial memories are summarized as a cognitive map. Spatial memory has representations within working, short-term memory and long-term memory. Research indicates that there are specific areas of the brain associated with spatial memory. Many methods are used for measuring spatial memory in children, adults, and animals. Short-term spatial memory Short-term memory (STM) can be described as a system allowing one to temporaril ...
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Cognitive Flexibility
Cognitive flexibility is an intrinsic property of a cognitive system often associated with the mental ability to adjust its activity and content, switch between different task rules and corresponding behavioral responses, maintain multiple concepts simultaneously and shift internal attention between them. The term ''cognitive flexibility'' is traditionally used to refer to one of the executive functions. In this sense, it can be seen as neural underpinnings of adaptive and flexible behavior. Most flexibility tests were developed under this assumption several decades ago. Nowadays, cognitive flexibility can also be referred to as a set of properties of the brain that facilitate flexible yet relevant switching between functional brain states. Cognitive flexibility varies during the lifespan of an individual. In addition, certain conditions such as obsessive–compulsive disorder are associated with reduced cognitive flexibility. Since cognitive flexibility is a vital component o ...
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D2-like Receptor
The D2-like receptors are a subfamily of dopamine receptors that bind the endogenous neurotransmitter dopamine. The D2-like subfamily consists of three G-protein coupled receptors that are coupled to Gi/Go and mediate inhibitory neurotransmission Neurotransmission (Latin: ''transmissio'' "passage, crossing" from ''transmittere'' "send, let through") is the process by which signaling molecules called neurotransmitters are released by the axon terminal of a neuron (the presynaptic neuron ..., of which include D2, D3, and D4. For more information, please see the respective main articles of the individual subtypes: See also * D1-like receptor References Dopamine receptors {{transmembranereceptor-stub ...
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