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Budipine Synthesis
Budipine (brand name Parkinsan) is an Management of Parkinson's disease#Medication, 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. Synthesis 4-Phenyl-1-t-butyl-4-piperidinol, (1) 1-t-butyl-3-benzoyl-4-phenyl-4-piperidinol [81831-81-4] (3) See also * AD-1211 * Delucemine * Diphenidine * Ephenidine * Fluorolintane * Lanicemine * Methoxphenidine (MXP) * MT-45 * Remacemide References Antiparkinsonian agents Drugs with unknown mechanisms of action 4-Phenylpiperidines Tert-butyl compounds Benzhydryl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Management Of Parkinson's Disease
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 treatm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluorolintane
Fluorolintane (also known as 2-FPPP and 2-F-DPPy) is a dissociative anesthetic drug that has been sold online as a designer drug. Fluorolintane and related diarylethylamines are antagonists of the NMDA receptor and have been studied ''in vitro'' as potential treatments for neurotoxic injury, depression and as sympathomimetic. See also * AD-1211 * Diphenidine * Ephenidine * Lanicemine * Methoxphenidine (MXP) * MT-45 * Prolintane * Remacemide Remacemide is a drug which acts as a low-affinity NMDA antagonist with sodium channel blocking properties. It has been studied for the treatment of acute ischemic stroke, epilepsy, Huntington's disease, and Parkinson's disease. Because remacem ... References Designer drugs Dissociative drugs NMDA receptor antagonists Diarylethylamines Fluoroarenes Pyrrolidines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs With Unknown Mechanisms Of Action
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Pharmaceutical drugs are often classified into drug classes—groups of related drugs ... [...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 treatm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Remacemide
Remacemide is a drug which acts as a low-affinity NMDA antagonist with sodium channel blocking properties. It has been studied for the treatment of acute ischemic stroke, epilepsy, Huntington's disease, and Parkinson's disease. Because remacemide has only a modest effect on seizure frequency and causes dizziness, it is no longer believed that remacemide will be an effective treatment for epilepsy. Although no such statement has been made about remacemide's potential for treating stroke, Huntington's, or Parkinson's, remacemide is no longer being developed for these conditions. Remacemide is also known as remacemide hydrochloride, (±)-2-amino-''N''-(1-methyl-1,2-diphenylethyl)-acetamide hydrochloride, or FPL 12924AA. Adverse effects *dizziness *nausea Lack of adverse effects Unlike many other treatments for epilepsy, remacemide does not appear to impair cognitive performance or driving performance in humans, although the evidence for effects on cognitive performance in animal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MT-45
MT-45 (IC-6) is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-(1,2-diphenylethyl)piperazine derivative, which is structurally unrelated to most other opioid drugs. Racemic MT-45 has around 80% the potency of morphine, with almost all opioid activity residing in the (S) enantiomer (the opposite stereochemistry from the related drug lefetamine). It has been used as a lead compound from which a large family of potent opioid drugs have been developed, including full agonists, partial agonists, and antagonists at the three main opioid receptor subtypes. Fluorinated derivatives of MT-45 such as 2F-MT-45 are significantly more potent as μ-opioid receptor agonists, and one of its main metabolites 1,2-diphenylethylpiperazine also blocks NMDA receptors. ] Side effects Recreational use of MT-45 has been associated with unconsciousness and overdose, as well as a range of unusual side effects not typically seen with other ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methoxphenidine
Methoxphenidine (methoxydiphenidine, 2-MeO-Diphenidine, MXP) is a dissociative of the diarylethylamine class that has been sold online as a designer drug. Methoxphenidine was first reported in a 1989 patent where it was tested as a treatment for neurotoxic injury. Shortly after the 2013 UK ban on arylcyclohexylamines methoxphenidine and the related compound diphenidine became available on the gray market, where it has been encountered as a powder and in tablet form. Though diphenidine possesses higher affinity for the NMDA receptor, anecdotal reports suggest methoxphenidine has greater oral potency. Of the three isomeric anisyl-substituents methoxphenidine has affinity for the NMDA receptor that is higher than 4-MeO-Diphenidine but lower than 3-MeO-Diphenidine, a structure–activity relationship shared by the arylcyclohexylamines. Side effects Acute methoxphenidine intoxication has been reported to produce confusion, hypertension, and tachycardia that was responsive to treat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lanicemine
Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under development by AstraZeneca for the management of severe and treatment-resistant depression. Lanicemine differs from ketamine in that it is a ''low-trapping'' NMDA receptor antagonist, showing similar rapid-acting antidepressant effects to ketamine in clinical trials but with little or no psychotomimetic side effects. However, lanicemine did not meet study endpoints, and its development was terminated by AstraZeneca in 2013. See also * 4-Chlorokynurenine * AD-1211 * Apimostinel * CERC-301 * Diphenidine * Ephenidine * Esketamine * Lefetamine * Memantine * Methoxphenidine * MT-45 * Rapastinel Rapastinel () (former developmental code name GLYX-13) is a novel antidepressant that was under development by Allergan (previously Naurex) as an adjunctive therapy for the treatment of treatment-resistant depression. It is a centrally active ... References {{Ionotropic glutamate receptor modulators ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ephenidine
Ephenidine (also known as NEDPA and EPE) is a dissociative anesthetic that has been sold online as a designer drug. It is illegal in some countries as a structural isomer of the banned opioid drug lefetamine, but has been sold in countries where it is not yet banned. Pharmacology Pharmacodynamics Ephenidine and related diarylethylamines have been studied in vitro as treatments for neurotoxic injuries, and are antagonists of the NMDA receptor (Ki = 66.4 nM for ephenidine). Ephenidine also possesses weaker affinity for dopamine and norepinephrine transporters (379 nM and 841 nM, respectively) as well as σ1R (629 nM) and σ2R (722 nM) binding sites. Pharmacokinetics Metabolism Ephenidine's metabolic pathway consists of N-oxidation, N-dealkylation, mono- and bis-hydroxylation of the benzene ring, and hydroxylation of the phenyl ring only after N-dealkylation. The dihydroxy metabolites were conjugated by methylation of one hydroxy group, and hydroxy metab ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parkinson's Disease
Parkinson's disease (PD), or simply Parkinson's, is a long-term degenerative disorder of the central nervous system that mainly affects the motor system. The symptoms usually emerge slowly, and as the disease worsens, non-motor symptoms become more common. The most obvious early symptoms are tremor, rigidity, slowness of movement, and difficulty with walking. Cognitive and behavioral problems may also occur with depression, anxiety, and apathy occurring in many people with PD. Parkinson's disease dementia becomes common in the advanced stages of the disease. Those with Parkinson's can also have problems with their sleep and sensory systems. The motor symptoms of the disease result from the death of cells in the substantia nigra, a region of the midbrain, leading to a dopamine deficit. The cause of this cell death is poorly understood, but involves the build-up of misfolded proteins into Lewy bodies in the neurons. Collectively, the main motor symptoms are also known as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diphenidine
Diphenidine (1,2-DEP, DPD, DND) is a dissociative anesthetic that has been sold as a designer drug. The synthesis of diphenidine was first reported in 1924, and employed a Bruylants reaction analogous to the one that would later be used to discover phencyclidine in 1956. Shortly after the 2013 UK ban on arylcyclohexylamines, diphenidine and the related compound methoxphenidine became available on the grey market. Anecdotal reports describe high doses of diphenidine producing "bizarre somatosensory phenomena and transient anterograde amnesia." Diphenidine and related diarylethylamines have been studied in vitro as treatments for neurotoxic injury and are antagonists of the NMDA receptor. In dogs diphenidine exhibits greater antitussive potency than codeine phosphate. Electrophysiological analysis demonstrates that the amplitude of NMDA-mediated fEPSPs are reduced by diphenidine and ketamine to a similar extent, with diphenidine displaying a slower onset of antagonism. The two en ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
