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DopAmide
DopAmide, or L-DopAmide, is a synthetic levodopa (L-DOPA) analogue that can serve as a levodopa and dopamine prodrug and is of potential interest in the treatment of Parkinson's disease. DopAmide has an amide rather than the carboxyl group of L-DOPA, which imparts greater water solubility. The amide is hydrolyzed back to the acid by aminopeptidase enzymes. See also * 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 selecti ... * Foslevodopa * Melevodopa * Etilevodopa * ''O'',''O''′-Diacetyldopamine * ''O'',''O''′-Dipivaloyldopamine * Neurotransmitter prodrug References Antiparkinsonian agents Catecholamines Dopamine agonists Experimental drugs Monoamine precursors Prodrugs Amides {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, su ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 dopa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Precursor
Monoamine precursors are precursors of monoamines and monoamine neurotransmitters in the body. The amino acids L-tryptophan and L-5-hydroxytryptophan (5-HTP; oxitriptan) are precursors of serotonin and melatonin, while the amino acids L-phenylalanine, L-tyrosine, and L-DOPA (levodopa) are precursors of dopamine, epinephrine (adrenaline), and norepinephrine (noradrenaline). Administration of monoamine precursors can increase the levels of monoamine neurotransmitters in the body and brain. Monoamine precursors may be used in combination with peripherally selective aromatic L-amino acid decarboxylase inhibitors (AAAD inhibitors; also known as DOPA decarboxylase (DDC) inhibitors) such as carbidopa and benserazide. Carbidopa/levodopa is used to increase brain dopamine levels in the treatment of Parkinson's disease while carbidopa/oxitriptan (EVX-101) is under development as an antidepressant Antidepressants are a class of medication used to treat major depressive dis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Precursors
Monoamine precursors are precursors of monoamines and monoamine neurotransmitters in the body. The amino acids L-tryptophan and L-5-hydroxytryptophan (5-HTP; oxitriptan) are precursors of serotonin and melatonin, while the amino acids L-phenylalanine, L-tyrosine, and L-DOPA (levodopa) are precursors of dopamine, epinephrine (adrenaline), and norepinephrine (noradrenaline). Administration of monoamine precursors can increase the levels of monoamine neurotransmitters in the body and brain. Monoamine precursors may be used in combination with peripherally selective aromatic L-amino acid decarboxylase inhibitors (AAAD inhibitors; also known as DOPA decarboxylase (DDC) inhibitors) such as carbidopa and benserazide. Carbidopa/levodopa is used to increase brain dopamine levels in the treatment of Parkinson's disease while carbidopa/oxitriptan (EVX-101) is under development as an antidepressant Antidepressants are a class of medication used to treat major depressive disor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
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 ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Agonists
A dopamine agonist (DA) is a compound that activates dopamine receptors. There are two families of dopamine receptors, D2-like and D1-like, and they are all G protein-coupled receptors. D1- and D5-receptors belong to the D1-like family and the D2-like family includes D2, D3 and D4 receptors. Dopamine agonists are primarily used to treat Parkinson's disease. They are also used, to a far lesser extent, in treating hyperprolactinemia and restless legs syndrome. They are not intended for treatment of clinical depression, and studies have shown severe detrimental side effects resulting from off-label use of dopamine agonists in treating depression, particularly in their tendency to produce impulse control disorders and extreme cases of withdrawal syndrome. Medical uses Parkinson's disease Dopamine agonists are mainly used in the treatment of Parkinson's disease. The cause of Parkinson's is not fully known but genetic factors, for example specific genetic mutations, and envi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catecholamines
A catecholamine (; abbreviated CA) is a monoamine neurotransmitter, an organic compound that has a catechol (benzene with two hydroxyl side groups next to each other) and a side-chain amine. Catechol can be either a free molecule or a substituent of a larger molecule, where it represents a 1,2-dihydroxybenzene group. Catecholamines are derived from the amino acid tyrosine, which is derived from dietary sources as well as synthesis from phenylalanine. Catecholamines are water-soluble and are 50% bound to plasma proteins in circulation. Included among catecholamines are epinephrine (adrenaline), norepinephrine (noradrenaline), and dopamine. Release of the hormones epinephrine and norepinephrine from the adrenal medulla of the adrenal glands is part of the fight-or-flight response. Tyrosine is created from phenylalanine by hydroxylation by the enzyme phenylalanine hydroxylase. Tyrosine is also ingested directly from dietary protein. Catecholamine-secreting cells use several ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiparkinsonian Agents
In the management of Parkinson's disease, due to the chronic nature of Parkinson's disease (PD), a broad-based program is needed that includes patient and family education, support-group services, general wellness maintenance, exercise, and nutrition. At present, no cure for the disease is known, but medications or surgery can provide relief from the symptoms. While many medications treat Parkinson's, none actually reverses the effects of the disease. Furthermore, the gold-standard treatment varies with the disease state. People with Parkinson's, therefore, often must take a variety of medications to manage the disease's symptoms. Several medications currently in development seek to better address motor fluctuations and nonmotor symptoms of PD. However, none is yet on the market with specific approval to treat Parkinson's. Medication The main families of drugs useful for treating motor symptoms are levodopa, dopamine agonists, and MAO-B inhibitors. The most commonly used treatme ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O,O′-Dipivaloyldopamine
''O'','-Dipivaloyldopamine, or simply dipivaloyldopamine, also known as 3,4-dipivaloyloxyphenethylamine, is a synthetic derivative of dopamine in which both of the hydroxyl groups have been acetylated. It was developed as a lipophilic prodrug of dopamine that would allow for entry of dopamine into the central nervous system. Dopamine itself is too hydrophilic to cross the blood–brain barrier and hence is peripherally selective. This, in part, prevents dopamine itself from being employed medically for central nervous system uses. Whereas the experimental log P of dopamine is -0.98, the predicted log P ( XLogP3) of ''O'',''O'''-dipivaloyldopamine is 3.1. The optimal log P for brain permeation and central activity is at least 1.5. ''O'','-Dipivaloyldopamine produced hypothermia in animals, thought to be a centrally mediated dopaminergic effect, but failed to reverse behavioral depression induced by the monoamine depleting agent reserpine. On the other hand, another analogue, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O,O′-Diacetyldopamine
''O'',''O′''-Diacetyldopamine, or 3,4-''O''-diacetyldopamine, also known as 3,4-diacetoxyphenethylamine, is a synthetic derivative of dopamine in which both of the hydroxyl groups have been acetylated. Description The drug was an attempt at creating a more lipophilic analogue and prodrug of dopamine which could potentially be used medically for central nervous system indications like treatment of Parkinson's disease. Dopamine itself is too hydrophilic to cross the blood–brain barrier and hence is peripherally selective. This, in part, prevents dopamine itself from being employed pharmaceutically for such uses. Whereas the experimental log P of dopamine is -0.98, the predicted log P ( XLogP3) of ''O'',''O′''-diacetyldopamine is 0.3. The optimal log P for brain permeation and central activity is about 2.1 (range 1.5–2.7). ''O'',''O′''-Diacetyldopamine proved to be inactive in animal behavioral tests. This suggests that dopamine ''O''-acetylation alone is insuffi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etilevodopa
Etilevodopa (TV-1203) is a dopaminergic agent which was developed as a treatment for Parkinson's disease. It is the ethyl ester of levodopa -DOPA, also known as levodopa and -3,4-dihydroxyphenylalanine, is an amino acid that is made and used as part of the normal biology of some plants and animals, including humans. Humans, as well as a portion of the other animals that utilize -DOPA .... It was never marketed. See also * Melevodopa References Prodrugs Catecholamines Dopamine agonists Propionate esters Ethyl esters Abandoned drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melevodopa
Melevodopa (brand name Levomet) is a dopaminergic agent. It is the methyl ester of levodopa. It is used in tablet form as an effervescent prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ... with 250 times the water solubility of tablet levodopa. See also * Etilevodopa References Prodrugs Dopamine agonists Catecholamines Carboxylate esters Methyl esters Phenylpropanoids {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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