|
Diphenidine
Diphenidine (1,2-DEP, DPD, DND) is a dissociative anesthetic that has been sold as a designer drug. Diphenidine was first synthesized in 1924 using a Bruylants reaction similar to the one later employed in the discovery of phencyclidine in 1956. Following the 2013 UK ban on arylcyclohexylamines, diphenidine and the related compound methoxphenidine emerged on the grey market. Anecdotal reports indicate that high doses of diphenidine can produce "bizarre somatosensory phenomena and transient anterograde amnesia." Pharmacology Electrophysiological studies show that diphenidine reduces the amplitude of NMDA-mediated fEPSPs to a similar extent as ketamine, although its antagonistic effect has a slower onset. The drug's two enantiomers exhibit markedly different NMDA receptor affinities, with the (S)-enantiomer being approximately 40 times more potent than the (R)-enantiomer. Since diphenidine's emergence in 2013, vendors have claimed it acts on the dopamine transporter, but ... [...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 trea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lefetamine
Lefetamine (Santenol) is a drug which is a stimulant and also an analgesic with effects comparable to codeine. Discovery The parent structure of lefetamine, 1,2-diphenylethylamine was first synthesized in the 1940s and showed weak analgesic activity. Lefetamine itself was first investigated in Japan in the 1950s. The L-isomer showed weak analgesic action comparable to codeine and antitussive action far weaker than codeine. The d-isomer showed no such activity but caused seizures in rats. Society and culture It was abused in Japan during the 1950s. In a small study in 1989 it showed some effect against opioid withdrawal symptoms without causing withdrawal symptoms itself. It was concluded that it may be an opioid partial agonist. It has been abused in Europe; in 1989 a small study of 15 abusers and some volunteers found that it had some partial similarity to opioids, that it produced withdrawal symptoms, and had dependence and abuse potential to a certain degree. In a sm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lanicemine
Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under drug development, 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 References {{Ionotropic glutamate receptor modulators Abandoned drugs Phenyl compounds NMDA receptor antagonists 1,2-Diarylethylamines 2-Pyridyl compounds ... [...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 * Alpha-D2PV * Diphenidine * Ephenidine * Lanicemine Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under drug development, development by AstraZeneca for the management of severe and treatment-resistant depression. Lanicemine differs from ketamine in that it is a ''low- ... * Methoxphenidine (MXP) * MT-45 * Prolintane * Remacemide References Designer drugs Dissociative drugs NMDA receptor antagonists 1,2-Diarylethylamines 2-Fluorophenyl compounds Phenyl compounds 1-Pyrrolidinyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ephenidine
Ephenidine (also known as NEDPA and EPE) is a Dissociative drug, dissociative anesthesia, 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 Receptor antagonist, antagonists of the NMDA receptor (Ki = 66.4 nM for ephenidine). Ephenidine also possesses weaker affinity for Dopamine transporter, dopamine and norepinephrine transporters (379 nM and 841 nM, respectively) as well as Sigma-1 receptor, σ1R (629 nM) and Sigma-2 receptor, σ2R (722 nM) binding sites. Pharmacokinetics Metabolism Ephenidine's metabolic pathway consists of N-oxidation, N-dealkylation, mono- and bis-hydroxylation of the benzyl ring, and hydroxylation of the phenyl ring only after N-dea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AD-1211
AD-1211 is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4- prenyl-piperazine derivative, which is structurally unrelated to most other opioid drugs. The (''S'')-enantiomers in this series are more active as opioid agonists, but the less active (''R'')-enantiomer of this compound, AD-1211, is a mixed agonist–antagonist at opioid receptors with a similar pharmacological profile to pentazocine, and has atypical opioid effects with little development of tolerance or dependence seen after extended administration in animal studies. See also * Diphenidine * Diphenpipenol * Ephenidine * Fluorolintane * Lanicemine Lanicemine (AZD6765) is a low-trapping NMDA receptor antagonist that was under drug development, development by AstraZeneca for the management of severe and treatment-resistant depression. Lanicemine differs from ketamine in that it is a ''low- ... * Lefetamine * Methoxphenidine (MXP) * MT-45 * Rem ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5F-AMB
5F-AMB (also known as 5F-MMB-PINACA and 5F-AMB-PINACA) is an indazole-based synthetic cannabinoid from the indazole-3-carboxamide family, which has been used as an active ingredient in synthetic cannabis products. It was first identified in Japan in early 2014. Although only very little pharmacological information about 5F-AMB itself exists, its 4-cyanobutyl analogue (instead of 5-fluoropentyl) has been reported to be a potent agonist for the CB1 receptor (''K''I = 0.7 nM). Side effects 5F-AMB intoxication caused one fatality on its own, another through ketoacidosis in combination with AB-CHMINACA, AB-FUBINACA, AM-2201, 5F-APINACA, EAM-2201, JWH-018, JWH-122, MAM-2201, STS-135 and THJ-2201 and another fatality in combination with AB-CHMINACA and Diphenidine. Legality In the United States, 5F-AMB is a Schedule I controlled substance. 5F-AMB is an Anlage II controlled substance in Germany as of May 2015. Sweden's public health agency suggested classify ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NMDA Receptor
The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other two being AMPA receptor, AMPA and kainate receptors. Depending on its subunit composition, its Ligand (biochemistry), ligands are Glutamate (neurotransmitter), glutamate and glycine (or D-Serine, D-serine). However, the binding of the ligands is typically not sufficient to open the channel as it may be blocked by Magnesium, Mg2+ ions which are only removed when the neuron is sufficiently depolarized. Thus, the channel acts as a "coincidence detector" and only once both of these conditions are met, the channel opens and it allows cation, positively charged ions (cations) to flow through the cell membrane. The NMDA receptor is thought to be very important for controlling synaptic plasticity and mediating learning and memory functions. The N ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Shizuoka Prefecture
is a Prefectures of Japan, prefecture of Japan located in the Chūbu region of Honshu. Shizuoka Prefecture has a population of 3,555,818 and has a geographic area of . Shizuoka Prefecture borders Kanagawa Prefecture to the east, Yamanashi Prefecture to the northeast, Nagano Prefecture to the north, and Aichi Prefecture to the west. Shizuoka (city), Shizuoka is the capital and Hamamatsu is the largest city in Shizuoka Prefecture, with other major cities including Fuji, Shizuoka, Fuji, Numazu, and Iwata, Shizuoka, Iwata. Shizuoka Prefecture is located on Japan's Pacific Ocean coast and features Suruga Bay formed by the Izu Peninsula, and Lake Hamana which is considered to be one of Japan's largest lakes. Mount Fuji, the tallest volcano in Japan and cultural icon of the country, is partially located in Shizuoka Prefecture on the border with Yamanashi Prefecture. Shizuoka Prefecture has a significant Motor vehicle, motoring heritage as the founding location of Honda, Suzuki Motor C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NPDPA
NPDPA (also known as isopropylphenidine or isophenidine) is a dissociative anesthetic that has been sold online as a designer drug. It was first identified in Germany in 2008, and while it has never been as widely sold as related compounds such as diphenidine and ephenidine, it has continued to show up in seized drug samples occasionally, and was banned in Sweden in 2015. Metabolism Isopropylphenidine'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 metabolites by glucuronidation or sulfation. Legality Sweden's public health agency suggested that NPDPA be classified as a hazardous substance on 1 June 2015. Due to that suggestion it became a scheduled substance in Sweden, as of 18 August 2015. It has also been proposed for control in Germany under analogue provisions ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Health Canada
Health Canada (HC; )Health Canada is the applied title under the Federal Identity Program; the legal title is Department of Health (). is the Structure of the Canadian federal government#Departments, with subsidiary units, department of the Government of Canada responsible for national health policy. The department itself is also responsible for numerous federal health-related agencies, including the Canadian Food Inspection Agency (CFIA) and the Public Health Agency of Canada (PHAC), among others. These organizations help to ensure compliance with federal law in a variety of Healthcare in Canada, healthcare, Agriculture in Canada, agricultural, and Pharmaceutics, pharmaceutical activities. This responsibility also involves extensive collaboration with various other federal- and provincial-level organizations in order to ensure the safety of food, health, and Medication, pharmaceutical products—including the regulation of health research and pharmaceutical manufacturing/Clinical ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
