Designer Drug Exposé: Amphetamines & Other Stimulants
Stimulants increase alertness, attention, & energy by boosting the activity of certain neurotransmitters in the brain. Cocaine, meth, & MDMA are the most popular, but there are hundreds more, too.
The stimulant class of drugs has carved itself a niche over the past 50 years. It all started with the discovery of a plant called Ma Huang (Ephedra sinica), which contains a series of stimulating alkaloids — most notably ephedrine — that mimic the body's stress hormones to temporarily increase heart rate, improve attention, and sharpen cognition.
The use of ma huang dates all the way back to ancient times in China, where it was used as a treatment for asthma, congestion, and low blood pressure.
Plenty of other stimulating herbs have earned themselves a reputation as important stimulants over the years, too. Plants like khat (Catha edulis), coca (Erythroxylum coca), coffee (Coffea arabica), and kratom (Mitragyna speciosa) were all used by laborers to increase their work output and delay the onset of fatigue.
Today, we have thousands of psychostimulant drugs at our disposal — many are used as prescription medications for conditions like attention deficit hyperactivity disorder (such as Adderall, Vyvanse, and Ritalin), Parkinson's disease (such as amantadine and levodopa), obesity (such as phentermine and orlistat), narcolepsy (such as modafinil), and recreational drugs like cocaine, methamphetamine, bath salts, MDMA, and countless others (which we'll explore below).
Like any other group of drugs, the prohibition of psychostimulants has only spurred faster development of new designer drug alternatives — some objectively safer, others much more dangerous.
The stimulant class is massive, but I’ll do my best to break it down by chemical family and explore the most prominent designer drugs for each group.
This is in no way a comprehensive list of designer stimulants, but it does cover all the major families.
Amphetamines
The amphetamines are a large and diverse group, mostly consisting of psychostimulants but also a few psychedelic empathogens and even a couple of nootropics (non-medical cognitive enhancers). Medications such as Adderall (amphetamine/dextroamphetamine) and Vyvanse (lisdexamfetamine) are also found in this group.
Common amphetamine street drugs include crystal meth (methamphetamine), bath salts (ex: MDPV, ɑ-PVP), MDMA, and MDA.
Some of the more psychedelic members include the DOX psychedelics (DOI, DOB, and DOM).
All of the substances mentioned above are explicitly illegal under the Controlled Substances Act (USA) and similar regulations worldwide. Many of them have already been around for more than 30 years. All of this excludes them from the “designer drug” title.
New amphetamine designer drugs are made by swapping one or more of the hydrogen atoms attached to the central amphetamine base structure with another functional group.
Chemists started playing with this molecule in the late 1980s after MDMA was initially banned. Today, the amphetamine family contains a wealth of psychoactive designer drugs.
One of the more popular emerging subgroups of designer amphetamines is the fluorinated amphetamine group — these weren’t discovered until sometime around 2010. Several boast impressive potency over older amphetamines.
Other substances, such as MMDA, MDPH, and MDPPP, were inspired by MDMA and sold as "legal ecstasy" before getting themselves banned. There are well over 50 designer drugs in the MDMA-inspired MDXX subfamily alone.
The synthetic cathinone group (AKA “Bath Salts”) first entered the market in the late 2000s with the introduction of drugs such as mephedrone and MDPV. These compounds were modeled after the naturally occurring alkaloids found in the khat plant (Catha edulis). They offer a powerful stimulant effect, most similar to cocaine. In high doses, they possess deliriant-like qualities and can lead to fatal hyperthermia.
All of these cathinones were individually banned in 2011, but a gamut of new designer drugs have since filled the void. Today, the synthetic cathinone family hosts more than 130 unique designer drugs — the majority of which have neither been officially banned nor formally tested. Some examples include ɑ-PPP, 3-MMC, and ethylone.
Basic Amphetamines
The first and most basic amphetamine is amphetamine itself. It was first synthesized back in 1887 by the Romanian chemist Lazăr Edeleanu.
However, it wasn't until nearly 5 decades later that it began working its way into clinical use — mainly as a decongestant. Today, amphetamine is a key ingredient in the ADHD medication, Adderall.
Most of the members in this group are psychoactive but not psychedelic. They offer varying levels of stimulating, entactogenic, and euphoric effects. Very high doses of drugs like methamphetamine can produce altered states of consciousness, often described as “psychotic.” Thoughts, emotions, and perceptions become frantic and chaotic. Users often experience feelings of anxiety, paranoia, and delusional thought patterns.
The most well-known members of this group are amphetamine (Adderall), lisdexamfetamine (Vyvanse), and N-Methamphetamine (crystal meth) — all of which are restricted substances in the United States (the first two as Schedule II prescription-only medicines, the third as a banned Schedule I drug).
Other Schedule I basic amphetamines include dimethylamphetamine, ethylamphetamine, PMA, and PMMA.
Examples of designer drugs in this group include 4-ETA, propylamphetamine, selegiline, and xylopropamine.
Fluorinated Amphetamines
The fluorinated amphetamines first started appearing on the market around 2010. The most common members of this group include 2-FMA, 2-FA, and 4-FA.
This sub-family is characterized by the presence of a fluoride group attached to the central ring moiety of the base amphetamine molecule. The addition of fluorine alters the bioavailability and selectivity of a substance on target receptors — often unpredictably. In several cases, this change dramatically increases the potency of the base molecule.
Unfortunately, fluorinated substances can also release radioactive fluoride atoms into the brain, which can cause long-term cognitive problems.
Most of the members of this group are believed to act as dopamine and norepinephrine-releasing agents — but very little research is available for this niche group of compounds despite their widespread popularity in the designer drug space.
At the moment, none of the fluorinated amphetamines are explicitly listed on the DEAs restricted substance list. 4-FA is considered Schedule II according to the UN Convention on Psychotropic Substances, and 3-FPM is included in the UK Schedule II standing.
Members of this group considered true “designer drugs” include 2-FA, 2-FEA, 2-FMA, 3-FA, 3-FEA, 3-FMA, and 4-FMA.
Synthetic Cathinones (AKA “Bath Salts”)
Substituted cathinones are based on the chemical structure of cathinone, which is a naturally occurring alkaloid from the khat plant (Catha edulis).
The most common members of this class are MDPV, mephedrone, methylene, and a-PVP (Flakka) — all of which are universally banned at this point, but there are hundreds of other members here too.
Cathinones are very strong stimulants — many of these compounds are similarly selective to dopaminergic neurons as cocaine. This gives them a stark, stimulating effect with few other actions. They're rarely psychedelic or dissociative and primarily affect energy and mood.
Only a small dose is needed to produce effects comparable to basic amphetamines like Adderall or methamphetamine, while higher doses often produce euphoria, psychotic delirium, negative thought loops, panic attacks, hyperthermia, and neuronal damage.
The substituted cathinone family first became popular in the 2000s when they were sold as “legal” designer drug alternatives to crystal meth, cocaine, and MDMA. The effects can vary depending on the individual compound, but most of them resemble the effects of cocaine.
Designer cathinones are popular because of their exceptional potency and low cost.
Cathinones work by altering the function of neuronal transporters, including dopamine, norepinephrine, and serotonin. Some cathinones (such as mephedrone and other ring-substituted analogs) cause a reversal of the transporter; others (such as MDPV and other pyrrolidinophenones) block reuptake and clearance of the neurotransmitter instead.
There are currently 23 synthetic cathinones included on the DEA restricted substances list (Schedule I), including 2,3-MDMC, 3-FMC, 4-MEAP, 4-MEC, 4-MePPP, Butylone, Cathinone, Ethylone, Eutylone, MDMC, MDPV, Mephedrone (4-MMC), Methcathinone, MPHP, N-ethyl-nor-hexedrone, N-Ethylpentylone, Naphyrone (O-2482), Pentedrone, Pentylone, α-Naphyrone, α-PHP, α-PHpP (PV8), and α-PVP.
The UN Convention on Psychotropic Substances only includes about 14 of these compounds.
Our analysis shows as many as 137 individual designer drugs in the cathinone family that haven’t been added to any restricted drug list around the world (yet). Many are illegal by proxy due to structural similarities to mephedrone, alpha-PVP, and MVPV.
There are too many designer cathinones to list, but some of the most popular include: 2-EEC, 2-FMC, 2-MEC, 2-MePPP, 2-Methylbutylone, 2-MMC, 3-MMC, 3-MOMC, 4-EEC, 4-EMC, 4-FC, 4-MC, 5-DBFPV, Benzylone (BMDP), Buphedrone, Bupropion, DPPE (A-D2PV), Ethcathinone (ETH-CAT), Hexedrone, MDPEP (MD-PV8), MDPHP, MDPOP (MD-PV9), MDPPP, MDPT, Mexedrone, MPBP, N-ethyl-nor-pentedrone (NEP), N-Ethylbuphedrone (NEB), α-PBT, α-PCYP, α-PPP, α-PPT, α-PVT
MDXX Class
When most people talk about “psychedelic amphetamines,” they’re usually referring to the methylenedioxyphenethylamine class (shortened to MDXX) — which contains both MDMA and MDA, along with a few others.
The base compound of the MDXX class is 3,4-methylenedioxyphenethylamine (MDPEA), which is quickly rendered inactive by monoamine oxidase. Other functional groups can be added to prevent this from happening and provide the characteristic empathogenic, psychedelic, and stimulating effects.
The most important members of this class are MDMA and MDA. There are several other psychoactive compounds in this class, too, but the majority of them are quickly disabled by an enzyme called monoamine oxidase (MAO).
Some people report success with so-called “inactive” MDXX compounds by taking them with an MAO inhibitor.
This idea follows a similar thought process used to make ayahuasca. The MAO inhibitor blocks the enzyme that prevents the drug from working. Obviously, the safety of this is unclear, and with other very good (active) alternatives — namely MDMA — most people don’t see a point in taking this sort of unnecessary risk.
There are currently 5 members of the MDXX subgroup that are explicitly mentioned on the Schedule I list: MDA, MDE, MDMA, MDOH, and MMDA.
That leaves us with about 78 designer drug analogs for this group — the vast majority of which are either non-psychoactive or have not been tested to any reasonable capacity (either anecdotally or through formal research).
Designer Benzofurans
The substituted benzofurans consist of a benzene ring fused to a furan ring. These compounds exist in nature in plants such as soursop (Annona muricata), the camphor tree (Cinnamomum camphora), nutmeg (Myristica fragrans), and African dream herb (Entada rheedii).
In the realm of designer drugs, substituted benzofurans offer effects that overlap with many categories of drugs. 5-EAPB, 5-MAPB, 5-APDB, 5-MAPDB, 5-MBPB, 6-APB, and others have empathogenic qualities similar to MDMA. These compounds are often sold as “Benzo Fury” — though in most cases, this product specifically refers to 6-APB.
Other benzofurans have more classical psychedelic effects, similar to DMT, psilocybin, or LSD. The main compounds in this group are 5-MeO-BFE (dimemebfe) and 5-MeO-DiBF.
Designer Piperazines
This group consists of a six-membered ring containing two nitrogen atoms at opposite sides. These compounds don’t exist in nature but share similarities with piperidine and piperine — both of which are present in the black pepper plant (Piper nigra).
Many piperazines are employed in medicine as anthelmintics (anti-parasitic drugs used for killing worms), as well as antihistamines, antipsychotics, and antidepressants.
Several of these compounds are sold as designer piperazines, including BZP (benzylpiperazine), DBZP (dibenzylpiperazine), MBZP (methylbenzylpiperazine), and others. The piperazines were very popular in the early 2010s as "legal MDMA," but interest has diminished since then.
While the effects of these drugs resemble the euphoric and stimulant properties of MDMA, they’re significantly weaker, and many experience strong and uncomfortable body loads.
Tropanes
The tropane alkaloids are a powerful class of alkaloids found in plants such as datura (Datura stromatum), belladonna (Atropa belladona), the boracherro tree (Brugmansia spp.), and mandrake (Mandragora officinarum).
They’re also present in the Erythroxylaceae family, which contains members such as the coca plant (Erythroxylum coca), catuaba (Erythroxylum catuaba), and Erythroxylum novogranatense — all of which have medicinal value.
The tropane alkaloids provide a wide range of effects on the human body. Some, like cocaine, are powerful stimulants; others, like scopolamine, hyoscyamine, and atropine, are powerful deliriants and poisons.
Most of the designer tropanes are modeled after cocaine. Examples include dichloropane, 4-fluorococaine, and troparil (all now listed as Schedule III). None of the cocaine analogs have ever reached mainstream popularity and are considered inferior in effects to cocaine itself.
Direct analogs of cocaine and its metabolites, including 2-acetoxycocaine, 2-hydroxycocaine, benzoylecgonine, tropacocaine, 1-methyl-cocaine, 1-ethyl-cocaine, 1-n-propyl-cocaine, 1-n-pentyl-cocaine, and 1-phenyl-cocaine are all banned under the same status as cocaine itself.
Thiophenes
The thiophenes are simple molecules with a signature planar five-membered ring. These compounds have been discovered in the soil on Mars — some samples dated to be around 3.5 billion years old.
A handful of designer drugs contain thiophene groups that make them hard to place in other categories. Substances like 5-methylmethiopropamine, cyclo-methiodrone, methiopropamine, thiopropamine, and thiothinone most closely resemble the cathinones — the difference is that the phenyl group is replaced with thiophene.
There isn’t much information available about the subjective effects of substances containing thiophene as a functional group, but they’re most often sold as MDMA or other amphetamine alternatives.
Designer Drug Series
This has been part 3 in an 8-part series on designer drugs. Read some of our past series using the link below, or subscribe to receive new posts as they’re released in upcoming weeks:
Part 5: Amphetamines & Other Stimulants
Part 8: Sedative Hypnotics & Opioids (Subscribe)
Part 9: Deliriants (Subscribe)
Part 10: Atypical Designer Drugs (Subscribe)
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