Betamethadol or β-methadol is an opioid analgesic under international control according to the UN Single Convention 1961. Betamethadol is an isomer of the racemic mixture of dimepheptanol.

Racemethorphan is racemic mixture of Dextromethorphan and Levomethorphan. Racemethorphan is listed under the Single Convention on Narcotic Drugs 1961 and is therefore listed in the United States as a Controlled Substance, specifically as a Narcotic in Schedule II. Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive. Dextromethorphan is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Levomethorphan is an opioid analgesic of the morphinan family that has never been marketed.

Alphamethadol is a synthetic opioid analgesic. Alphamethadol is composed of two isomers itself, L-α-methadol, and D-α-methadol. L-α-methadol is an important active metabolite of levacetylmethadol (LAAM), a medication therapy for individuals addicted to opiates that provides an alternative to methadone. Isomers of Alphamethadol bind to and activate the μ-opioid receptor; they are active as opioid analgesics.

Norpipanone (Orfenso; Hexalgon) is an opioid analgesic. It is a controlled substance (opiate).

Rolicyclidine (PCPy) is a dissociative anesthetic agent that has hallucinergic and sedative properties. In rats, it produces stimulant effects like that of PCP (hydrochloride) and was therefore added to the Schedule I list of illegal drugs in the USA. It is thought to be much less stimulating than PCP however, and more similar to opioids, or other central nervous system depressants.

Morpheridine is a pethidine analog with strong analgesic activity. Morpheridine does not cause convulsions, although it produces the standard opioid side effects such as sedation and respiratory depression. Morpheridine is not currently used in medicine and is a Schedule I drug which is controlled under United Nations drug conventions.

Brolamfetamine (also known as DOB, bromo-DMA, and 4-bromo-2,5-dimethoxyphenylisopropylamine) is one of a vast number of compounds used recreationally to achieve hallucinogenic effects. Brolamfetamine is one of the most potent hallucinogens, with its hallucinogenic potency directly linked to its abuse potential. Brolamfetamine acts as a partial agonist of 5HT2A, 5HT2B, 5HT2C, and TAAR1 receptors, but it’s psychedelic effects are mainly mediated by its agonistic properties at the 5-HT2A receptor. Animal studies have shown physiologic effects including hypertension, tachycardia, hyperpyrexia, pupillary dilatation, and peripheral vasoconstriction. In general, Brolamfetamine having a similar effect to LSD, with slower onset (up to 3–4 h to peak intoxication) and longer duration of effect (up to 36 h). Brolamfetamine is not commonly available, through periods of higher circulation were reported in Australia in 1983, Ireland in 2003, and in Italy in 2015. Brolamphetamine, as well as many other synthetic hallucinogens, are increasingly being sold as LSD. Internationally Brolamfetamine is a Schedule I drug under the Convention on Psychotropic Substances. Due to its selectivity, Brolamfetamine is often used in scientific research when studying the 5-HT2 receptor subfamily.

Normorphine is an opiate analog, specifically the N-demethylated derivative of morphine. It was first described in the 1953 as part of an effort to characterize N-substituted morphine analogs. Normorphine has relatively little opioid activity, but it is a useful intermediate for the production of more potent morphine analogs. It is also a major metabolite of morphine.

Formebolone is an orally active anabolic-androgenic steroid that is included in the list of prohibited substances by the World Anti-Doping Agency. Formebolone was used in Italy and Spain for infants with malnutrition.

Tenocyclidine (TCP) is a dissociative anesthetic drug with psychostimulant and hallucinogenic effects. This drug shows a broad spectrum of pharmacological activity including antidotal effect in organophosphorus compounds poisoning, radioprotective and anticancer effects. It was studied that the antidotal potency could protect acetylcholinesterase (AChE) in the case of organophosphate poisoning. However, the controversial role of TCP in brain protection should be studied further. Tenocyclidine has a high affinity for the N-methyl-D-aspartate (NMDA) receptors. This property allows using of TCP binding (association rate) as a marker of channel opening and thereby permitting measurement of NMDA receptor activation and ligand binding under identical conditions.