Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
4-Methylaminorex (CAS 3568-94-3), chemically 2-amino-4-methyl-5-phenyl-2-oxazoline, is also known as McN-822, euphoria, U4Euh, ICE, d,l-cis-2-amino-4-methyl-5-phenyl-2-oxazoline, d,l-erythro-2-amino-4-methyl-5-phenyl-2-oxazoline, (±)-cis-2-amino-4-methyl-5-phenyl-2-oxazoline and (±)-erythro-2-amino-4-methyl-5-phenyl-2-oxazoline. There are two chiral carbon atoms so that four stereoisomers and two racemates are possible.
Similarity to known substances and effects on the CNS
4-Methylaminorex (cis racemate) is a potent psychomotor stimulant. Its actions are similar to those produced by amfetamine. It stimulates spontaneous activity in mice, and has sympathomimetic and central stimulating effects in dogs. In discrimination studies in rats, it generalized to d-amfetamine. Its potency is about one-half that of d-amfetamine and it produces a lower degree of stimulation.
Dependence potential
In self-administration studies in rhesus monkeys, 4-methylaminorex (cis racemate) had potent reinforcing activity. All animals self-administered the substance at rates comparable to that of cocaine. No human studies are available concerning the dependence liability of 4-methylaminorex (cis racemate).
Actual abuse and or/evidence of likelihood of abuse
No epidemiological data on actual abuse are available but there have been individual case reports. One death has been reported in which significant blood levels of 4-methylaminorex (cis racemate) and diazepam were found in the body. There is evidence of illicit traffic in the USA and clandestine production has been demonstrated.
Therapeutic usefulness
There is no known therapeutic use for 4-methylaminorex (cis racemate).
Recommendation
On the basis of available data concerning its pharmacological profile, dependence potential and actual abuse, the Committee rated the likelihood of abuse of 4-methylaminorex (cis racemate) as moderate to high. The public health and social problems associated with the substance are moderately serious and it has no therapeutic use. The Committee found that there was sufficient evidence that 4-methylaminorex is currently being, or is likely to be, abused so as to constitute a public health and social problem warranting the placing of the substance under international control. In the light of this assessment, the Committee recommended that 4-methylaminorex (cis racemate) be controlled under Schedule I of the Convention on Psychotropic Substances, 1971.
4-Methylaminorex (CAS 3568-94-3), chemically 2-amino-4-methyl-5-phenyl-2-oxazoline, is also known as McN-822, euphoria, U4Euh, ICE, d,l-cis-2-amino-4-methyl-5-phenyl-2-oxazoline, d,l-erythro-2-amino-4-methyl-5-phenyl-2-oxazoline, (±)-cis-2-amino-4-methyl-5-phenyl-2-oxazoline and (±)-erythro-2-amino-4-methyl-5-phenyl-2-oxazoline. There are two chiral carbon atoms so that four stereoisomers and two racemates are possible.
Similarity to known substances and effects on the CNS
4-Methylaminorex (cis racemate) is a potent psychomotor stimulant. Its actions are similar to those produced by amfetamine. It stimulates spontaneous activity in mice, and has sympathomimetic and central stimulating effects in dogs. In discrimination studies in rats, it generalized to d-amfetamine. Its potency is about one-half that of d-amfetamine and it produces a lower degree of stimulation.
Dependence potential
In self-administration studies in rhesus monkeys, 4-methylaminorex (cis racemate) had potent reinforcing activity. All animals self-administered the substance at rates comparable to that of cocaine. No human studies are available concerning the dependence liability of 4-methylaminorex (cis racemate).
Actual abuse and or/evidence of likelihood of abuse
No epidemiological data on actual abuse are available but there have been individual case reports. One death has been reported in which significant blood levels of 4-methylaminorex (cis racemate) and diazepam were found in the body. There is evidence of illicit traffic in the USA and clandestine production has been demonstrated.
Therapeutic usefulness
There is no known therapeutic use for 4-methylaminorex (cis racemate).
Recommendation
On the basis of available data concerning its pharmacological profile, dependence potential and actual abuse, the Committee rated the likelihood of abuse of 4-methylaminorex (cis racemate) as moderate to high. The public health and social problems associated with the substance are moderately serious and it has no therapeutic use. The Committee found that there was sufficient evidence that 4-methylaminorex is currently being, or is likely to be, abused so as to constitute a public health and social problem warranting the placing of the substance under international control. In the light of this assessment, the Committee recommended that 4-methylaminorex (cis racemate) be controlled under Schedule I of the Convention on Psychotropic Substances, 1971.
ECDD Recommendation
Inclusion in Schedule I of the 1971 Convention on Psychotropic Substances
Link to full TRS
who_trs_787.pdf1.19 MB