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HDMP-28
HDMP-28 or methylnaphthidate is a piperidine based stimulant drug, closely related to methylphenidate, but with the benzene ring replaced by naphthalene. It is a potent dopamine reuptake inhibitor, with several times the potency of methylphenidate and a short duration of action, and is a structural isomer of another potent dopamine reuptake inhibitor, N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate. Most of the TMP analogs of HDMP-28 have SERT Ki values in the range >10,000 and so are selective for dopamine and noradrenaline reuptake, with little or no effect on serotonin. HDMP-28 has high affinity to SERT, and so behaves as a triple reuptake inhibitor. D.R. = Discrimination Ratio = HA ÷ HFT. A low D.R. = addictive, whereas a high D.R. = low propensity for self-administration. Legality HDMP-28 is illegal in Switzerland as of December 2015. See also * 3-Bromomethylphenidate * 3,4-Dichloromethylphenidate * BMAPN * Ethylphenidate * HDEP-28 * Naphthylisopropyla ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Methylphenidate Analogues
This is a list of methylphenidate (MPH or MPD) Analog (chemistry), analogues, or Phenidates. The most well known compound from this family, methylphenidate, is widely prescribed around the world for the treatment of attention deficit hyperactivity disorder (ADHD) and certain other indications. Several other derivatives including rimiterol, phacetoperane and pipradrol also have more limited medical application. A rather larger number of these compounds have been sold in recent years as designer drugs, either as quasi-legal substitutes for illicit stimulants such as methamphetamine or cocaine, or as purported "study drugs" or nootropics. More structurally diverse compounds such as Desoxypipradrol (and thus Pipradrol, including such derivatives as AL-1095, Difemetorex, Diphemethoxidine, SCH-5472 and Diphenylprolinol, D2PM), and even mefloquine, 2-Benzylpiperidine, 2-benzylpiperidine, rimiterol, enpiroline and DMBMPP, can also be considered structurally related, with the former ones a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Fluoromethylphenidate
4-Fluoromethylphenidate (also known as 4-FMPH and 4F-MPH) is a stimulant drug that acts as a higher potency dopamine reuptake inhibitor than the closely related methylphenidate. 4-Fluoromethylphenidate was studied further along with other analogues of (±)-threo-methylphenidate (TMP) to assess their potential as anti-cocaine medications. 4F-MPH was reported as having an ED50 mg/kg of 0.26 (0.18–0.36), regarding its efficacy as a substitute for cocaine, and a relative potency of 3.33 compared to methylphenidate for the same purpose. This is based on its binding strength to the dopamine transporter vs. its activity as a dopamine reuptake inhibitor. In theory, this would block some of the effects of cocaine, without being as addictive. This has been misinterpreted as a dopamine vs. norepinephrine selectivity ratio. Another study found that in the threo-isomers of methylphenidate, the meta- and para-substituted compounds with electron-withdrawing substituents tended to have incre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-Methylmethylphenidate
''threo''-4-Methylmethylphenidate (4-MeTMP) is a stimulant drug related to methylphenidate. It is slightly less potent than methylphenidate and has relatively low efficacy at blocking dopamine reuptake despite its high binding affinity, which led to its investigation as a possible substitute drug for treatment of stimulant abuse (cf. nocaine). On the other hand, several other simple ring-substituted derivatives of ''threo''-methylphenidate such as the 4-fluoro and 3-chloro compounds are more potent than methylphenidate both in efficacy as dopamine reuptake inhibitors and in animal drug discrimination assays. Legality 4-Methylmethylphenidate was banned in the UK as a Temporary Class Drug from June 2015 following its unapproved sale as a designer drug. See also * 3-Bromomethylphenidate * 3,4-Dichloromethylphenidate * 4-Fluoromethylphenidate * 4-Methylphenmetrazine * Dexmethylphenidate * HDMP-28 * Isopropylphenidate * Propylphenidate Propylphenidate (also known as PPH) is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethylphenidate
Ethylphenidate (EPH), also known as Baxtercaine in the United Kingdom is a psychostimulant and a close analog of methylphenidate. Ethylphenidate acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. However, considering the close similarities between ethylphenidate and methylphenidate and the fact that methylphenidate, like cocaine, actually does not primarily act as a "classical" reuptake inhibitor, but rather as an "inverse agonist at the DAT" (also called a "negative allosteric modulator at the DAT"), it is at least very likely that ethylphenidate also primarily acts as an inverse DAT agonist instead of (or at least only secondarily) as a classical reuptake inhibitor (which could be called a "competitive antagonist at ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HDEP-28
HDEP-28 or ethylnaphthidate is a piperidine based stimulant drug, closely related to ethylphenidate, but with the benzene ring replaced by naphthalene. It is even more closely related to HDMP-28, which acts as a potent serotonin–norepinephrine–dopamine reuptake inhibitor with several times the potency of methylphenidate and a short duration of action. Legality HDEP-28 was banned in the UK as a Temporary Class Drug from June 2015 following its unapproved sale as a designer drug, alongside 4-Methylmethylphenidate. See also * 2β-Propanoyl-3β-(2-naphthyl)-tropane (WF-23) * 3,4-Dichloromethylphenidate * 4-Methylmethylphenidate * 4-Fluoromethylphenidate * Isopropylphenidate * Naphthylisopropylamine * Naphyrone * Propylphenidate Propylphenidate (also known as PPH) is a piperidine based stimulant drug, closely related to methylphenidate, but with the methyl ester replaced by a propyl ester. It was banned in the UK as a Temporary Class Drug from April 2015 following its u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphthylisopropylamine
Naphthylaminopropane (PAL-287) is an experimental drug under investigation as of 2007 for the treatment of alcohol and stimulant addiction. Naphthylisopropylamine acts as a non-neurotoxic releasing agent of serotonin, norepinephrine, and dopamine, with EC50 values of 3.4 nM, 11.1 nM, and 12.6 nM, respectively. It also has affinity for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50 values = 466 nM, 40 nM, and 2.3 nM, respectively), and acts as a full agonist at 5-HT2B and as a partial agonist at 5-HT2C, while its affinity for 5-HT2A is probably too low to be significant. In animal studies, naphthylisopropylamine was shown to reduce cocaine self-administration, yet produced relatively weak stimulant effects when administered alone, being a (much) lesser stimulant than d-amphetamine for comparison. Further research is now being conducted in primates to see if it will be a useful substitute for treating drug addiction in humans as well. An important observation is that in behav ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphyrone
Naphyrone, also known as O-2482 and naphthylpyrovalerone, is a substituted cathinone drug derived from pyrovalerone that acts as a triple reuptake inhibitor, producing stimulant effects and has been reported as a novel designer drug. No safety or toxicity data is available on the drug. The drug has been marketed under the name NRG-1, although only a minority of samples of substances sold under this name have been found to actually contain naphyrone, and even samples that proved to contain genuine β-naphyrone were in some cases also found to contain the 1-naphthyl isomer α-naphyrone in varying proportions, further confusing the reported effects profile. Use in the United Kingdom Naphyrone emerged as a new legal high in the United Kingdom only months after the ban of similar drug mephedrone (which was also a cathinone derivative). Until July 2010 the substance was not controlled by the Misuse of Drugs Act 1971 and was therefore not illegal for someone to possess. The Medi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate
''N'',''O''-Dimethyl-4β-(2-naphthyl)piperidine-3β-carboxylate (DMNPC) is a piperidine based stimulant drug which is synthesised from arecoline. It is similar to nocaine in chemical structure, and has two and a half times more activity than cocaine as a dopamine reuptake inhibitor. However it is also a potent serotonin reuptake inhibitor, with similar affinity to fluoxetine. Clearly it is not just the SS enantiomer of the title compound that is an active MAT inhibitor. Effect of ''N''-demethylation For the SR enantiomer, increased DAT affinity is seen upon demethylation. This is the same choice of isomer used in the production of Paxil. Simplification A substantially simpler method that ablates the carbomethoxy ester substituent can be found by D. Koch in Ex2: See also * 1-Methyl-3-propyl-4-(p-chlorophenyl)piperidine * Naphthylamphetamine * Naphyrone * List of cocaine analogues This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2β-Propanoyl-3β-(2-naphthyl)-tropane
2β-Propanoyl-3β-(2-naphthyl)-tropane or WF-23 (Wake Forest-23, named after the university where it was first created) is a cocaine analogue. It is several hundred times more potent than cocaine at being a serotonin-norepinephrine-dopamine reuptake inhibitor. As can be seen on PubMed, these acyl substituted phenyltropanes are highly potent MAT inhibitors and also have a very long half-life, spanning perhaps at least a few days; as the half-life of the dopamine transporter in rats was found to be 2-3 days under normal conditions (with agonists, antagonists, and transporter inhibitors altering the half-life), it may be that WF-23 largely or mostly binds to its transporters until they are degraded. See also * HDEP-28 * HDMP-28 * List of cocaine analogues This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point of natural) cocaine's molecular structure, with the result product suf ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isopropylphenidate
Isopropylphenidate (also known as IPH and IPPD) is a piperidine based stimulant drug, closely related to methylphenidate, but with the methyl ester replaced by an isopropyl ester. It has similar effects to methylphenidate but with a longer duration of action, and was banned in the UK as a Temporary Class Drug from April 2015 following its unapproved sale as a designer drug. It has been researched as potential methylphenidate replacement for ADHD and narcolepsy, because of fewer side effects. See also * 3,4-Dichloromethylphenidate * Ethylphenidate * Desoxypipradrol * HDEP-28 * HDMP-28 * Propylphenidate Propylphenidate (also known as PPH) is a piperidine based stimulant drug, closely related to methylphenidate, but with the methyl ester replaced by a propyl ester. It was banned in the UK as a Temporary Class Drug from April 2015 following its u ... References {{Stimulants 2-Benzylpiperidines Dopamine reuptake inhibitors Stimulants Designer drugs Isopropyl esters ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Propylphenidate
Propylphenidate (also known as PPH) is a piperidine based stimulant drug, closely related to methylphenidate, but with the methyl ester replaced by a propyl ester. It was banned in the UK as a Temporary Class Drug from April 2015 following its unapproved sale as a designer drug. Legal status Propylphenidate is illegal in Sweden as of 26. January 2016, and in Finland since 2017. See also * 3,4-Dichloromethylphenidate * 4-Fluoromethylphenidate * 4-Methylmethylphenidate * Dexmethylphenidate * Ethylphenidate * Isopropylphenidate * HDEP-28 * HDMP-28 HDMP-28 or methylnaphthidate is a piperidine based stimulant drug, closely related to methylphenidate, but with the benzene ring replaced by naphthalene. It is a potent dopamine reuptake inhibitor, with several times the potency of methylphenidat ... References {{psychoactive-stub 2-Benzylpiperidines Norepinephrine–dopamine reuptake inhibitors Stimulants Designer drugs 2-Piperidinyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3,4-Dichloromethylphenidate
3,4-Dichloromethylphenidate (also known as 3,4-CTMP or 3,4-DCMP) is a stimulant drug related to methylphenidate. Dichloromethylphenidate is a potent psychostimulant that acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. 3,4-DCMP, the ''threo''-diastereomer, is approximately seven times more potent than methylphenidate in animal studies, but has weaker reinforcing effects due to its slower onset of action. However, H. M. Deutsch's discrimination ratio implies it to be more reinforcing than cocaine. Legality As of October 2015 3,4-CTMP is a controlled substance in China. 3,4-CTMP was banned in the UK as a Temporary Class Drug from April 2015 following its unapproved sale as a designer drug. Sweden's public health ag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
