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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 ...
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Dopamine Reuptake Inhibitors
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been linked ...
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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 ...
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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 ...
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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 ...
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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 ...
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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 ...
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Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ...
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Stimulants
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have Sympathomimetic drug, sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or Prohibition (drugs), illicitly) as performance-enhancing substance, performance-enhancing or recreational drug use, recreational drugs. Among narcotics, stimulants produce a noticeable crash or ''Comedown (drugs), comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and p ...
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Desoxypipradrol
Desoxypipradrol, also known as 2-⁠diphenylmethylpiperidine (2-DPMP), is a drug developed by Ciba in the 1950s which acts as a norepinephrine-dopamine reuptake inhibitor (NDRI). Chemistry Desoxypipradrol is closely related on a structural level to the compounds methylphenidate and pipradrol, all three of which share a similar pharmacological action. Of these three piperidines, desoxypipradrol has the longest elimination half-life, as it is a highly lipophilic molecule lacking polar functional groups that are typically targeted by metabolic enzymes, giving it an extremely long duration of action when compared to most psychostimulants. Methylphenidate, on the other hand, is a short-acting compound, as it possesses a methyl-ester moiety that is easily cleaved, forming a highly polar acid group, while pipradrol is intermediate in duration, possessing a hydroxyl group which can be conjugated (e.g. with glucuronide) to increase its hydrophilicity and facilitate excretion, but no eas ...
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Isopropylphenidine
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 ...
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N-Isopropyl-N'-phenyl-1,4-phenylenediamine
''N''-Isopropyl-''N''′-phenyl-1,4-phenylenediamine (often abbreviated IPPD) is an organic compound commonly used as an antiozonant in rubbers, particularly those used for tires. Like other p-phenylenediamine-based antiozonants it works by virtue of its low ionization energy, which allows it to react with ozone faster than ozone will react with rubber. This reaction converts it to the corresponding aminoxyl radical (R2N–O•), with the ozone being converted to a hydroperoxyl radical (HOO•), these species can then be scavenged by other antioxidant polymer stabilizers. IPPD is prone to process called blooming, where it migrates to the surface of the rubber. This can be beneficial to the tire, as ozone attacks the tire surface and blooming therefore moves the antiozonant to where it is most needed, however this also increases the leaching of IPPD into the environment. Many tire producers have moved to using 6PPD instead, as this migrates more slowly. Oxidation of IPPD convert ...
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