Practitioner's Guide to Designer Drugs

A. Substituted Cathinones (stims) - Amphetamines with a ketone group (βk) added to the beta position to create a cathinone version, i.e. Methamphetamine (MA) becomes Methcathinone (βk-MA).

1. Methylone (βk-MDMA, M1, methylenedioxymethcathinone) -
Methylone is an empathogen. It has similar activity to MDMA with regards to dopamine and norepinephrine release, but only a third of MDMA's power with regards to serotonin release. Placed in Schedule 1 in October of 2011, though still relatively easy to find. Active at 100mg oral. Considered to be recreationally desirable.

a) Ethylone (βk-MDEA)
b) Butylone (βk-MBDB) - Illegal as of 2014.
c) Eutylone (βk-EBDB)
d) Dibutylone (βk-DMBDB)
e) Dimethylone (βk-MDDMA)
f) Pentylone (1-(1,3-benzodioxol-5-yl)-2-(methylamino)pentan-1-
one) - Illegal as of 2014. Not considered to be recreationally
desirable.

2. Mephedrone (4-MMC, 4-methylmethcathinone, 4-
methylephedrone, (RS)-2-methylamino-1-(4- methylphenyl)propan-1-one) -

Mephedrone is one of the most popular substituted cathinones, a strong, short-acting stimulant with empathogenic qualities similar to that of MDMA. It is a potent releaser of dopamine, norepinephrine, and serotonin. It has a rather unique danger in one of its metabolites: 4-methylephedrine is a long-acting vasoconstrictor. Placed in Schedule 1 in October 2011. Active at 100mg oral, 50mg intranasal. Considered to be recreationally desirable. Activity at NAT, SERT, and DAT.

a) 3-MMC (MiMiC, 3-Mac, 3-methylmethcathinone) Active at 30mg
intranasal. Considered to be recreationally desirable.
Unscheduled but considered a positionalal isomer of
mephedrone.

b) 2-MMC (2-methylmethcathinone) - unscheduled but a positional
isomer of mephedrone.

c) 3-MEC (3-methylmethcathinone) - unscheduled, but a positional
isomer of 4-MEC.

d) 4-MEC (4-methylethcathinone) - active at 100mg intranasal.
Illegal as of 2014. Considered to be recreationally desirable.
activity at NAT, SERT, and DAT can be found at footnote.

e) 4-EMC (4-ethylmethcathinone) - active at 100mg intranasal. not
explicitly scheduled but a positional isomer of mephedrone.

f) 4-BMC (4-bromomethcathinone, brephedrone) - Illegal as of
2014. Not considered to be recreationally desirable.

g) 4-FMC (4-fluoromethcathinone, flephedrone) - Illegal as of 2014.
 Not considered to be recreationally desirable.

h) 3-FMC (3-fluoromethcathinone) - Illegal as of 2014.

i) 2-FMC (2-fluoromethcathinone)

j) 3-MeoMC (3-methoxymethcathinone)

k) Benzedrone (4-BMZ, (±)-1-(4-methylphenyl)-2-
(benzylamino)propan-1-one) - activity at NAT, SERT, and DAT.

l) Pentedrone(1-phenyl-2-methylamino-pentan-1-one)-Illegal
as of 2014. Not considered to be recreationally desirable.

(1) 4-methylpentedrone (4-MPD, 4-Me-EAPP)

m)Naphyrone (NRG-1, napthylpyrovalerone) - Illegal as of 2014.
 Not considered to be recreationally desirable. activity at
NAT, SERT, and DAT.

n) 3,4-DMMC (3,4-dimethylmethcathinone) - Not considered to be
recreationally desirable.

o) 4-MeMABP (alpha-ethylmephedrone)

p) Buphedrone (MABP, α-methylamino-butyrophenone)

q) NEB (N-Ethylbuphedrone)

r) Methedrone (bk-PMMA, 4-methoxymethcathinone, 4-
methoxyephedrone) - see PMMA.

s) N,N-DEMEC (N,N-diethyl-4-methylethcathinone) - Suspected to be a prodrug for 4-MEC, based on activity from its cousin Amfepramone.

t) 3-CMC (Clophedrone, 3-chloromethcathinone) - active at 50mg intranasal. Remains to be seen if it becomes popular recreationally.

B. Pyrrolidines/Pyrrlidinophenones

1. Methylenedioxypyrovalerone (MDPV) - a potent NDRI, active at 2mg. The most infamous ingredient in “bath salts,” it has been responsible for many news stories of psychotically-stimulated men or women. Illegal.

2. α-PVP (alpha-pyrrolidinopentiophenone) - Illegal as of 2014.

3. 4-MePPP (4-methyl-alpha-pyrrolidinopentiophenone) - Illegal.

4. MDPPP (3,4-methylenedioxy-alpha-pyrrolidinopentiophenone)

5. α-PBP (alpha-pyrrolidinobutiophenone) - Illegal as of 2014.

6. DL-4662 (1-(3,4-dimethoxyphenyl)-2-(ethylamino)pentan-1-one)

7. α-PBT (2-(pyrrolidin-1-yl)-1-(thiophen-2-yl)butan-1-one) -

8. α-PVT (2-(pyrrolidin-1-yl)-1-(thiophen-2-yl)pentan-1-one, alpha-
pyrrolidinopentiothiophenone) - Similar to the above.

9. 4-MeO-PVP (4-methoxy-α-Pyrrolidinovalerophenone)

10. 4-MeO-PBP (4-methoxy-Pyrrolidinobutrophenone)

11. 4F-PVP (4-fluoro-pyrrolidinopropylphenone)

12. 4-MeO-a-PVP (4-methoxy-α-Pyrrolidinovalerophenone)

13. 4F-PV8 (4f-α-pyrrolidinoheptiophenone, 1-(4-fluorophenyl)-2-
(pyrrolidin-1-yl)heptan-1-one)

14. 4F-PV9 (1-(4-fluorophenyl)-2-(pyrrolidin-1-
yl)octan-1-one)

15. PV-4 (4-MPHP, 4’-Methyl-α-pyrrolidinohexiophenone)

16. α-PHP ((±)-1-Phenyl-2-(1-pyrrolidinyl)-1-hexanone)

17. 4-MeO-PV9 (1-(4-methoxyphenyl)-2-(pyrrolidin-1-yl)octan-1-one) 18. MeOPPP (4’-Methoxy-α-pyrrolidinopropiophenone)

19. 4-Me-PHP (4-methyl-pyrrolidinohexylphenone)

20. PHPP (pyrrolidinoheptanophenone)

21. POP (pyrrolidinooctanophenone)

22. 3,4-Di-Meo-PVP (3,4-dimethoxy-pyrrolidinovalerophenone) 

 

23. N-ethyl-4-methyl-pentedrone (N-Et-4-MP, N-Et-4-Me-EAPP, N-ethyl-4-methyl-ethylaminopentiophenone)

C. Benzofurans - phenethylamines with modified methylenedioxy groups, removing one of the two oxygens in the methylenedioxy ring to render a benzofuran ring.

1. 5-APB (5-(2-aminopropyl)benzofuran), and 6-APB (6-(2-
aminopropyl)benzofuran) [aka “Benzo Fury”] - Close analogues of MDA (methylenedioxyamphetamine), these two benzofurans are empathogens with some hallucinogenic activity. Created as replacements for Mephedrone and Methylone after they had been scheduled in the UK. active at 50mg oral, often sold in 100mg pellets. Considered to be recreationally desirable. activity at NAT, SERT, and DAT.

Both have high affinity for 5-HT2B receptors.

2. 5-APDB (5-(2-aminopropyl)2,3-dihydrobenzofuran)

3. 6-APDB (6-(2-aminopropyl)2,3-dihydrobenzofuran)

4. 5-MAPB (5-(2-methylaminopropyl)benzofuran) - Active at 50mg
oral. Considered to be recreationally desirable.

5. 6-MAPB (6-(2-methylaminopropyl)benzofuran)

6. 5-MAPDB (5-(2-methylaminopropyl)2,3-dihydrobenzofuran)

7. 6-MAPDB (6-(2-methylaminopropyl)2,3-dihydrobenzofuran)

8. 5-EAPB (5-(2-ethylaminopropyl)benzofuran). 5-EAPB has already
been responsible for at least one death.

9. 6-EAPB (6-(2-ethylaminopropyl)benzofuran)

D. Phenpropylamines/piperidines
1. Ethylphenidate - An analogue of Methylphenidate (Ritalin). active
at 10mg intranasal, 20mg oral. created by the body when Ritalin is consumed in combination with Alcohol. It is now illegal in the island state of Jersey.Considered to be recreationally desirable.

2. 2-DPMP (desoxypipradol) - a half-life of 16-20 hours and active at 2mg. activity at NAT, SERT, and DAT

 

3. 3,4-CTMP (3,4-Dichloromethylphenidate) - Another Methylphenidate analogue, active at 5mg.

4. MTTA (Mephtetramine, (2-((methylamino)methyl)-3,4- dihydronaphthalen-1(2H)-one)) - active at 50mg intranasal, 100mg oral. Some reports of vendors selling this compound.

E. Substituted Amphetamines (stims)

1. Fluorinated amphetamines

 

a) 4-FA (4-fluoroamphetamine) - active at 50mg oral. Considered
to be recreationally desirable.

b) 3-FA (3-fluoroamphetamine) - active at 20mg. more selective for
dopamine and noradrenaline release instead of serotonin.
Considered to be recreationally desirable.

c) 2-FA (2-fluoroamphetamine) - active at 20mg intranasal, 50mg
oral. Considered to be recreationally desirable.

d) 4-FMA (4-fluoromethamphetamine) - active at 20mg.
Considered to be recreationally desirable.

e) 2-FMA (2-fluoromethamphetamine) - active at 5mg. Considered
to be recreationally desirable.

2. Fenproporex (3-(1-phenylpropan-2-ylamino)propanenitrile) -
found in tainted diet pills in 2009.

3. 4-CA (PCA, para-chloroamphetamine, 4-chloroamphetamine) -
Although this substance has no recreational potential and is in fact a potent serotonergic neurotoxin, some “legal party pill” producers called “AM-HI-CO” have put it in a series of products, with names like “E-Blast” and “Diablo XXX.” 4-CA is a potent neurotoxin, with even one dose potentially causing brain damage. Still present in Ecstasy pills (rolls) as of mid-March 2014, found in California.

4. PMA (paramethoxyamphetamine) - Recreationally worthless. Responsible for several deaths.[18] Illegal.

5. PMMA (paramethoxymethamphetamine) - See PMA.

6. 5-Me-MDA(5-methyl-methylenedioxyamphetamine)-activeat 40mg. Not considered recreationally desirable.

7. 2-MA(2-methyl-amphetamine,Ortetamine)- 1/10 the potency of dexamphetamine.

8. 4-MTA (4-methylthioamphetamine) - potent, non-neurotoxic, selective serotonin release agent. responsible for one death and several non-fatal poisonings. Inhibitor of MAO-A.

9. 4-MA (4-methylamphetamine)-inhibits MAO and is involved in several deaths in Europe.

F. Indanes/indoles
1. MDAI (methylenedioxyaminoindane) - active at 20mg. Considered to be recreationally desirable.

2. 2-AI (2-aminoindane) - active at 15mg intranasal, 20mg oral. Not considered recreationally desirable.

3. 5-IAI (5-iodo-2-aminoindane) - active at 100mg oral. Not
considered to be recreationally desirable.

4. NM-2AI (N-methyl-2-aminoindane) - active at 50mg oral.

5. 5-APDI (IAP, 2-API, indanylaminopropane) - active at 20mg.

6. 5-IT (5-API, 5(2-aminopropyl)indole) - Active at 20mg oral. 5-IT
has been responsible for the deaths of 14 people in Sweden. Not considered to be recreationally desirable. Considered a positional isomer of aMT in the USA.

G. Tropanes/*caines
1. 3b-FBT (3b-(4-Fluorobenzoyloxy)tropane, fluorotropacocaine) - active at 100mg.

2. 4’-fluorococaine (4'-FC) - active at 10mg.

3. Dimethocaine - active at 50mg.

4. Nitracaine (3-(diethylamino)-2,2-dimethylpropyl 4-nitrobenzoate)
 

5. Troparil (b-CPT, REC, WIN-35065-2, (–)-2β-Carbomethoxy-3β-
phenyltropane)

H. piperazines
1. TFMPP (trifluoromethylphenylpiperazine) - active at 30mg.

2. BZP (benzylpiperazine) - active at 50mg oral. half-life of 5.5
hours. can cause seizures and multi-organ toxicity, although no fatalities have been reported from BZP used alone. Illegal.
3. MDBZP (methylenedioxybenzylpiperazine) - can’t find any dosing info about MDBZP itself, but a drug called Fipexide (Attentil, Vigilor, 1-(1,3-benzodioxol-5-ylmethyl)-4-[(4- chlorophenoxy)acetyl]piperazine) metabolizes into MDBZP in the human body. Fipexide was used in France and Italy to treat dementia, but is no longer used due to the occurrence of adverse reactions such as fever and hepatitis.

4. 2C-B-BZP (4-bromo-2,5-dimethoxy-benzylpiperazine)

5. pFPP (para-fluorophenylpiperazine) - active at 20mg.

I. Miscellaneous stimulants
1. Methiopropamine (MPA, Methamthetamine) - Active at 5mg. Methiopropamine is a somewhat misleading name. Imagine Methamphetamine where the phenyl ring is replaced with a thiophene ring and you have Methiopropamine, the sulfur-ring analogue of Methamphetamine. User reports on Erowid claim it's a less-potent, shorter-lasting version of Methamphetamine.[4] activity at NAT, SERT, and DAT can be found at

2. 4,4’-DMAR (4,4’-dimethylaminorex, Serotoni) - Active at 30mg. This one is based on 4-methylaminorex, which was in turn based on aminorex, which is a stimulant with effects similar to Dexamphetamine. Aminorex was used medically as an appetite suppressor but was withdrawn because it caused pulmonary hypertension, resulting in a number of deaths. A study performed on rats and another on mice found that 4-MAR is “significantly less neurotoxic than methamphetamine or MDMA”, although 4-MAR seems to have inherited aminorex’s problems with causing pulmonary hypertension.It has been linked to 26 deaths in several countries, mostly taken in combination with other substances but at least 2 deaths on its own. Also, it is worth noting that only the cis isomer of 4-MAR is specifically scheduled by the DEA, while the trans isomer is not scheduled and is much more potent than the cis isomer.

3. Camfetamine (N-methyl-3-phenyl-norbornan-2-amine) - analog of fencamfamine.

4. Diclofensine (4-(3,4-Dichlorophenyl)-7-methoxy-2- methyl-1,2,3,4-tetrahydroisoquinoline)

5. 2-PTC (2-p-tolyl-cyclopropylamine) - cyclopropylamines are appearing. Their similarity to tranylcypromine, a prescription MAOI, suggests that they could have similar effects and hazards.

6. 3,4-DFPCT (3,4-difluoro-cyclopropylamine) - another cyclopropylamine. unsure about this name. Probably an analog of 2-PTC, No IUPAC name or CAS number for it at this time.