Designer drugs are structural or functional analogues of controlled substances that are designed to mimic the pharmacological effects of the parent drug while avoiding detection or classification as illegal. Many of the older designer drugs (research chemicals) are structural analogues of psychoactive tryptamines or phenethylamines but there are many other chemically unrelated new psychoactive substances that can be considered part of the designer drug group.[1][2][3][4] Designer drugs can also include substances that are not psychoactive in effect, such as analogues of controlled anabolic steroids and other performance and image enhancing drugs (PIEDs), including nootropics, weight loss drugs and erectile dysfunction medications. The pharmaceutical activities of these compounds might not be predictable based strictly upon structural examination. Many of the substances have common effects while structurally different or different effects while structurally similar due to SAR paradox. As a result of no real official naming for some of these compounds, as well as regional naming, this can all lead to potentially hazardous mix ups for users.[5] The following list is not exhaustive.
A psychedelic substance is a psychoactive drug whose primary action is to alter cognition and perception. Psychedelics tend to affect and explore the mind in ways that result in the experience being qualitatively different from those of ordinary consciousness. The psychedelic experience is often compared to non-ordinary forms of consciousness such as trance, meditation, yoga, religious ecstasy, dreaming and even near-death experiences.
Lysergamides
Lysergamides are amide derivatives of the alkaloid lysergic acid.
Drugs containing the tryptamine moiety are typically substrates for the serotonin receptors, in keeping with their close structural resemblance to serotonin, a neurotransmitter.
Drugs containing the phenethylamine moiety bear close structural resemblance to dopamine but substitution on the benzene ring gives rise to drugs with a much higher affinity for serotonin receptors.
The DOx family of psychedelics are also known as "substituted amphetamines" as they contain the amphetamine backbone but are substituted on the benzene ring. This gives rise to serotonin agonists similar to the 2C-X class but more resistant to elimination in the body.
Dissociatives are a class of hallucinogens which distort perceptions of sight and sound and produce feelings of detachment - dissociation - from the environment and self. This is done through reducing or blocking signals to the conscious mind from other parts of the brain. Although many kinds of drugs are capable of such action, dissociatives are unique in that they do so in such a way that they produce hallucinogenic effects, which may include sensory deprivation, dissociation, hallucinations, and dream-like states or trances. Some, which are nonselective in action and affect the dopamine and/or opioid systems, may be capable of inducing euphoria. Many dissociatives have general depressant effects and can produce sedation, respiratory depression, analgesia, anesthesia, and ataxia, as well as cognitive and memory impairment and amnesia.
Arylcyclohexylamines
Arylcyclohexylamines are the oldest and most widely used dissociatives. The class includes the well known anaesthetic, ketamine.
Piperazine containing designer drugs have effects similar to MDMA (ecstasy). This class of drugs are mimics of serotonin that activate 5-HT receptor subtypes that release norepinephrine and dopamine.
Empathogens are a class of psychoactive drugs that produce distinctive emotional and social effects similar to those of MDMA. Users of empathogens say the drugs often produce feelings of empathy, love, and emotional closeness to others.
MDxx
Substituted methylenedioxyphenethylamines (MDxx) are a large chemical class of derivatives of the phenethylamines, which includes many psychoactive drugs that act as entactogens, psychedelics, and/or stimulants, as well as entheogens.
Benzofurans are similar in structure to MD(M)A but differ in that the methylenedioxy groups have been modified, removing one of the two oxygens in the methylenedioxy ring to render a benzofuran ring.
Drugs containing the tryptamine moiety are typically substrates for the serotonin receptors, in keeping with their close structural resemblance to serotonin, a neurotransmitter.
Substituted amphetamines are a chemical class of stimulants, entactogens, hallucinogens, and other drugs. They feature a phenethylamine core with a methyl group attached to the alpha carbon resulting in amphetamine, along with additional substitutions.
Stimulants produce a variety of different kinds of effects by enhancing the activity of the central and peripheral nervous systems. Common effects, which vary depending on the substance and dosage in question, may include enhanced alertness, awareness, wakefulness, endurance, productivity, and motivation, increased arousal, locomotion, heart rate, and blood pressure, and the perception of a diminished requirement for food and sleep.
Amphetamines
Amphetamines are a chemical class of stimulants, entactogens, hallucinogens, and other drugs. They feature a phenethylamine core with a methyl group attached to the alpha carbon resulting in amphetamine, along with additional substitutions.
Cathinones include some stimulants and entactogens, which are derivatives of cathinone. They feature a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon, along with additional substitutions.
Tropane alkaloids occur in plants of the families erythroxylaceae (including coca). Piperidine and its derivatives are ubiquitous building blocks in the synthesis of many pharmaceuticals and fine chemicals.
Oxazolidines are a five-membered ring compounds consisting of three carbons, a nitrogen, and an oxygen. The oxygen and NH are the 1 and 3 positions, respectively. In oxazolidine derivatives, there is always a carbon between the oxygen and the nitrogen.
Sedatives are substances that induces sedation by reducing irritability or excitement. At higher doses they may result in slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. Doses of sedatives such as benzodiazepines, when used as a hypnotic to induce sleep, tend to be higher than amounts used to relieve anxiety, whereas only low doses are needed to provide a peaceful effect.
Sedatives can be misused to produce an overly-calming effect. In the event of an overdose or if combined with another sedative, many of these drugs can cause unconsciousness and even death.
Opioids
Opioids have pharmacologic actions resembling morphine and other components of opium.
Androgenic anabolic steroids have approved medical uses as well as used illicitly as performance-enhancing drugs to build muscle mass and strength. Anabolic steroids that have been designed to evade detection in sport doping tests are known as "designer steroids".[98][99]
Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor ligands. They are intended to maintain the desirable muscle building effects of anabolic steroids while reducing undesirable androgenic actions (e.g., increased risk of prostate cancer). SARMs that are more selective in their action could potentially be used for a broader range of clinical indications other than the relatively limited legitimate uses that anabolic steroids are currently approved for.[100]
↑"Combined intoxication with methylone and 5-MeO-MIPT". Progress in Neuro-Psychopharmacology & Biological Psychiatry31 (1): 288–291. January 2007. doi:10.1016/j.pnpbp.2006.06.012. PMID16876302.
↑Phenethylamine Von der Struktur zur Funktion. Nachtschatten Verlag AG. 2013. ISBN978-3-03788-700-4.
↑"Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane". Journal of Medicinal Chemistry47 (24): 6034–6041. November 2004. doi:10.1021/jm040082s. PMID15537358.
↑"From PCP to MXE: a comprehensive review of the non-medical use of dissociative drugs". Drug Testing and Analysis6 (7–8): 614–632. 2014. doi:10.1002/dta.1620. PMID24678061.
↑ 21.021.121.221.321.421.5"Three 25-NBOMe-type drugs, three other phenethylamine-type drugs (25I-NBMD, RH34, and escaline), eight cathinone derivatives, and a phencyclidine analog MMXE, newly identified in ingredients of drug products before they were sold on the drug market". Forensic Toxicology34 (1): 108–114. January 2016. doi:10.1007/s11419-015-0293-6. ISSN1860-8965.
↑ 29.029.129.229.329.4"Characterization of four new designer drugs, 5-chloro-NNEI, NNEI indazole analog, α-PHPP and α-POP, with 11 newly distributed designer drugs in illegal products". Forensic Science International243: 1–13. October 2014. doi:10.1016/j.forsciint.2014.03.013. PMID24769262.
↑"Analysis of a new drug of abuse: cathinone derivative 1-(3,4-dimethoxyphenyl)-2-(ethylamino)pentan-1-one". Journal of Separation Science38 (5): 825–828. March 2015. doi:10.1002/jssc.201401052. PMID25545103.
↑"4F-PBP (4'-fluoro-α-pyrrolidinobutyrophenone), a new substance of abuse: Structural characterization and purity NMR profiling". Forensic Science International252: 168–176. July 2015. doi:10.1016/j.forsciint.2015.05.003. PMID26005857.
↑"Identification and quantification of 4′-methoxy-α-pyrrolidinobutiophenone (4-MeOPBP) in human plasma and urine using LC–TOF-MS in an autopsy case". Forensic Toxicology33 (2): 348–354. May 2015. doi:10.1007/s11419-015-0281-x.
↑"The syntheses, characterization and in vitro metabolism of nitracaine, methoxypiperamide and mephtetramine". Drug Testing and Analysis6 (7–8): 668–675. January 2014. doi:10.1002/dta.1616. PMID24574100.
↑"Identification of a novel fentanyl analog: p-Hydroxy-butyrylfentanyl". Drug Testing and Analysis12 (1): 152–155. January 2020. doi:10.1002/dta.2695. PMID31518047.
↑"Metabolism of novel opioid agonists U-47700 and U-49900 using human liver microsomes with confirmation in authentic urine specimens from drug users". Drug Testing and Analysis10 (1): 127–136. January 2018. doi:10.1002/dta.2228. PMID28608586.
↑"The alprazolam analogue 4'-chloro deschloroalprazolam identified in seized capsules". Drug Testing and Analysis14 (9): 1672–1680. September 2022. doi:10.1002/dta.3325. PMID35666014.
↑"[Biokinetics of a new prodrug gidazepam and its metabolite]". Biulleten' Eksperimental'noi Biologii I Meditsiny113 (1): 45–47. January 1992. PMID1356504.
↑ 74.074.1"Phase I metabolism of the carbazole-derived synthetic cannabinoids EG-018, EG-2201, and MDMB-CHMCZCA and detection in human urine samples". Drug Testing and Analysis10 (9): 1417–1429. September 2018. doi:10.1002/dta.2398. PMID29726116.
↑ 76.076.176.2"Identification and analytical characterization of four synthetic cannabinoids ADB-BICA, NNL-1, NNL-2, and PPA(N)-2201". Drug Testing and Analysis9 (1): 51–60. January 2017. doi:10.1002/dta.1990. PMID27239006.
↑"4F-MDMB-BINACA: A New Synthetic Cannabinoid Widely Implicated in Forensic Casework". Journal of Forensic Sciences64 (5): 1451–1461. September 2019. doi:10.1111/1556-4029.14101. PMID31260580.
↑"Detection of the recently emerged synthetic cannabinoid 4F-MDMB-BINACA in "legal high" products and human urine specimens". Drug Testing and Analysis11 (9): 1377–1386. September 2019. doi:10.1002/dta.2666. PMID31228224.
↑"Detection and characterization of the new synthetic cannabinoid APP-BINACA in forensic casework". Drug Testing and Analysis12 (1): 136–144. January 2020. doi:10.1002/dta.2698. PMID31788963.
↑"Identification of N,N-bis(1-pentylindol-3-yl-carboxy)naphthylamine (BiPICANA) found in an herbal blend product in the Tokyo metropolitan area and its cannabimimetic effects evaluated by in vitro [35S]GTPγS binding assays". Forensic Toxicology33: 84–92. November 2014. doi:10.1007/s11419-014-0253-6.
↑"Structure elucidation of the novel synthetic cannabinoid Cumyl-Tosyl-Indazole-3-Carboxamide (Cumyl-TsINACA) found in illicit products in Germany". Drug Testing and Analysis14 (8): 1387–1406. August 2022. doi:10.1002/dta.3261. PMID35338591.
↑Pulver, Benedikt; Fischmann, Svenja; Gallegos, Ana; Christie, Rachel (March 2023). "EMCDDA framework and practical guidance for naming synthetic cannabinoids". Drug Testing and Analysis15 (3): 255–276. doi:10.1002/dta.3403.
↑"A new cannabinoid receptor 1 selective agonist evading the 2021 "China ban": ADB-FUBIATA". Drug Testing and Analysis14 (9): 1639–1644. September 2022. doi:10.1002/dta.3285. PMID35570246.
↑"Advances in the detection of designer steroids in anti-doping". Bioanalysis6 (6): 881–896. March 2014. doi:10.4155/bio.14.9. PMID24702116.
↑"Deciphering the selective androgen receptor modulators paradigm". Expert Opinion on Drug Discovery8 (2): 191–218. February 2013. doi:10.1517/17460441.2013.741582. PMID23231475.
↑"Identification of the minimum peptide from mouse myostatin prodomain for human myostatin inhibition". Journal of Medicinal Chemistry58 (3): 1544–1549. February 2015. doi:10.1021/jm501170d. PMID25569186.