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Prodipine
Prodipine (; developmental code name BY-101) is an experimental drug, experimental antiparkinsonian agent of the phenylpiperidine, 4,4-diphenylpiperidine series related to budipine which was never marketed. It was the predecessor of budipine and was similarly found to be effective in the treatment of Parkinson's disease. However, prodipine produced side effects including gastrointestinal adverse effects, nausea and vomiting, and hypotension. Due to the nausea and vomiting with the oral administration, oral form, it could only be tolerated with intravenous administration. As a result, budipine, which had fewer side effects, was developed instead. Pharmacology The mechanism of action of these drugs is unknown. However, budipine is known to stimulate the catecholaminergic system and to increase locomotor activity, motor activity and vigilance (psychology), vigilance in animals. It also increases brain dopamine, norepinephrine, and serotonin levels in animals treated with the mo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Budipine
Budipine (brand name Parkinsan) is an antiparkinson agent marketed for the treatment of Parkinson's disease. While its exact mechanism of action is not well characterized, it is believed to be an NMDA receptor antagonist, but also promoting the synthesis of dopamine. Because it provides additional benefits relative to existing treatments, it probably does not precisely mimic the mechanism of an existing known treatment. It is an hERG blocker and can produce long QT syndrome as a side effect. Analogues include prodipine and medipine. Synthesis Budipine can be prepared from the 1-tert-butyl-4-piperidone 465-76-5directly by treatment with benzene in the presence triflic acid. This method of synthesis enables a 99% yield of product. 4-Phenyl-1-t-butyl-4-piperidinol, (1) 1-t-butyl-3-benzoyl-4-phenyl-4-piperidinol 1831-81-4(3) See also * AD-1211 * Delucemine * Diphenidine * Ephenidine * Fluorolintane * Lanicemine * Methoxphenidine (MXP) * MT-45 MT-45 (IC-6) is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Locomotor Activity
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many serotonerg ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyperactivity
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple contexts, and developmentally inappropriate. ADHD symptoms arise from executive dysfunction. Impairments resulting from deficits in self-regulation such as time management, inhibition, task initiation, and sustained attention can include poor professional performance, relationship difficulties, and numerous health risks, collectively predisposing to a diminished quality of life and a reduction in life expectancy. As a consequence, the disorder costs society hundreds of billions of US dollars each year, worldwide. It is associated with other mental disorders as well as non-psychiatric disorders, which can cause additional impairment. While ADHD involves a lack of sustained attention to tasks, inhibitory deficits also can lead to diffic ... [...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] |
D2 Receptor
Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the ''DRD2'' gene. After work from Paul Greengard's lab had suggested that dopamine receptors were the site of action of antipsychotic drugs, several groups, including those of Solomon H. Snyder and Philip Seeman used a radiolabeled antipsychotic drug to identify what is now known as the dopamine D2 receptor. The dopamine D2 receptor is the main receptor for most antipsychotic drugs. The structure of DRD2 in complex with the atypical antipsychotic risperidone has been determined. Function D2 receptors are coupled to Gi subtype of G protein. This G protein-coupled receptor inhibits adenylyl cyclase activity. In mice, regulation of D2R surface expression by the neuronal calcium sensor-1 (NCS-1) in the dentate gyrus is involved in exploration, synaptic plasticity and memory formation. Studies have shown potential roles for D2R in retrieval of fear memories in the prelimbic cortex and in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Oxidase
Monoamine oxidases (MAO) () are a family of enzymes that catalyze the oxidation of monoamines, employing oxygen to clip off their amine group. They are found bound to the outer membrane of mitochondria in most cell types of the body. The first such enzyme was discovered in 1928 by Mary Bernheim in the liver and was named tyramine oxidase. The MAOs belong to the protein family of flavin-containing amine oxidoreductases. MAOs are important in the breakdown of monoamines ingested in food, and also serve to inactivate monoamine neurotransmitters. Because of the latter, they are involved in a number of psychiatric and neurological diseases, some of which can be treated with monoamine oxidase inhibitors (MAOIs) which block the action of MAOs. Subtypes and tissue distribution In humans there are two types of MAO: MAO-A and MAO-B. * Both are found in neurons and astroglia. * Outside the central nervous system: ** MAO-A is also found in the liver, pulmonary vascular end ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reserpine
Reserpine is a drug that is used for the treatment of hypertension, high blood pressure, usually in combination with a thiazide diuretic or vasodilator. Large clinical trials have shown that combined treatment with reserpine plus a thiazide diuretic reduces mortality of people with hypertension. Although the use of reserpine as a solo drug has declined since it was first approved by the FDA in 1955, the combined use of reserpine and a thiazide diuretic or vasodilator is still recommended in patients who do not achieve adequate lowering of blood pressure with first-line drug treatment alone. The reserpine-hydrochlorothiazide combo pill was the 17th most commonly prescribed of the 43 combination antihypertensive pills available in 2012. The antihypertensive actions of reserpine are largely due to its antinoradrenergic effects, which are a result of its ability to deplete catecholamines (among other monoamine neurotransmitters) from peripheral nervous system, peripheral sympathetic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Depleting Agent
Monoamine-depleting agents are a group of drugs which reversibly deplete one or more of the monoamine neurotransmittersserotonin, dopamine, and norepinephrine. One mechanism of action, mechanism by which these agents act is by reuptake inhibitor, inhibiting reuptake by the vesicular monoamine transporters, VMAT1 and VMAT2. Examples of monoamine-depleting agents include deutetrabenazine, methyldopa, oxypertine, reserpine, tetrabenazine, and valbenazine. Tetrabenazine selectively depletes dopamine at low doses and is used as an animal model of amotivation. Monoamine synthesis inhibitors, such as the tryptophan hydroxylase enzyme inhibitor, inhibitor and serotonin synthesis inhibitor para-chlorophenylalanine, ''para''-chlorophenylalanine (PCPA or fenclonine), also act as monoamine-depleting agents, as do various other agents, for instance monoaminergic neurotoxins. See also * Monoamine reuptake inhibitor * Monoamine releasing agent * Tetrabenazine#Animal model of motivational dysfu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
