Table 1.

Pharmacological actions of ketamine.

Molecular target	Mechanism	Potency (μM)	References
NMDA receptor (PCP site)	Antagonism	Ki 0.4–46 IC50 1.6–6.2	6,7,9,138
μ-Opioid receptors	Agonism	Ki 27	13,14,139
δ-Opioid receptor	Agonism	Ki 101	13,139
k-Opioid receptor	Agonism	Ki 85	13
Sigma receptor	Agonism	Ki 66	13
Noradrenaline transporter	Inhibition of reuptake	Ki 67	14,140
Dopamine transporter	Inhibition of reuptake	Ki 162	140
Serotonin transporter binding	Inhibition of reuptake	Ki 67	140
Muscarinic, nicotinic receptor	Antagonism	IC50: >50 or 100	16,17
Voltage-dependent Na2+, Ca2+ channels	Block	Ki 67	19,21
Dopamine D2	Partial agonism	Ki 0.5	141,142
Serotonin 5HT2	Antagonism	Ki 15	141

IC₅₀, half-maximum inhibitory concentration; K_i, inhibitory constant; NMDA, N-methyl-D-aspartate.