Arylcyclohexylamine

Substitutive structure of an arylcyclohexylamine molecule

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Arylcyclohexylamine refers to a class of compounds which typically produce dissociative anaesthesia.

Chemistry

Arylcyclohexylamines are comprised of an amine moiety and an aromatic ring attached to a cyclohexane ring.

Hydrogen atoms around the structure can be substituted for other functional groups to produce drugs of varying potency, affinity, efficacy and half-life.

Pharmacology

Arylcyclohexylamines are believed to produce their effects primarily by antagonism of NMDA receptors. Antagonism of the NMDA receptor confers anesthetic, anticonvulsant, and dissociative effects. Contrary to popular belief, most arylcyclohexylamines do not significantly inhibit re-uptake of dopamine or agonise μ-opioid receptors.

Results of Binding assays – pKi ± SE, (Ki) nM

Compound	NMDA	SERT	NET	Sigma1	Sigma2
Ketamine	6.18±0.07 (659)	-	-	-	-
Phencyclidine	7.23±0.07 (59)	5.65±0.05 (2234)	-	-	6.82±0.09 (136)
Methoxetamine	6.59±0.06 (259)	6.32±0.05 (481)	-	-	-
4-MeO-PCP	6.39±0.06 (404)	6.07±0.05 (844)	6.1±0.1 (713)	6.5±0.1 (296)	7.93±0.08 (143)
3-MeO-PCP	7.69±0.08 (20)	6.7±0.1 (216)	-	7.4±0.1 (42)	-

Examples

• 3-MeO-PCMo
• 3-Me2'-Oxo-PCE
• 3-MeO-PCP
• 4-MeO-PCP
• Ketamine
• Methoxetamine (MXE)
• Methoxyketamine
• Phencyclidine (PCP)

See also

• Responsible use
• Arylcyclohexylamine (Wikipedia)
• Dissociative
• Ketamine
• Methoxetamine
• NMDA receptor antagonist