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group of stereoisomers

Ketamine

Ketamine be a dissociative anesthetic dem use medically for induction den maintenance of anesthesia. Dem sanso dey use am as a treatment for depression den insyd pain management. Ketamine be an NMDA receptor antagonist wich dey account for chaw of ein psychoactive effects.

Pharmacology

Molecular targets

Ketamine den biological targets (plus Ki below 100 μM)
Site Value (μM) Type Action Species Ref
NMDA (N-Methyl-D-aspartate receptor) 0.25–0.66 Ki Antagonist Human
MOR(μ-Opioid receptor) 42 Ki Antagonist Human
MOR2 (μ-Opioid receptor) 12.1 Ki Antagonist Human
KOR (κ-Opioid receptor) 28

25

Ki

Ki

Antagonist

Agonist

Human

σ2 26 Ki ND (No data) Rat
D2 receptor (D2) 0.5

>10

Ki

Ki

Agonist

ND (No data)

Human

Muscarinic acetylcholine receptor M1 (M1) 45 Ki ND (No data) Human
α2β2 (Nicotinic acetylcholine receptor) 92 IC50 Antagonist Human
α2β4 (Nicotinic acetylcholine receptor) 29 IC50 Antagonist Human
Alpha-3 beta-2 nicotinic receptor (α3β2) 50 IC50 Antagonist Human
Alpha-3 beta-4 nicotinic receptor (α3β4) 9.5 IC50 Antagonist Human
Alpha-4 beta-2 nicotinic receptor (α4β2) 72 IC50 Antagonist Human
Alpha-4 beta-4 nicotinic receptor (α4β4) 18 IC50 Antagonist Human
Alpha-7 nicotinic receptor (α7) 3.1 (Hydroxynorketamine) IC50 Negative allosteric modulation (NAM) Rat
ERα (Estrogen receptor alpha) 0.34 Ki ND (No data) Human
NET (Norepinephrine transporter) 82–291 IC50 Inhibitor Human
DAT (Dopamine transporter) 63 Ki Inhibitor Rat
HCN1 (Hyperpolarization-activated cyclic nucleotide-gated channel 1) 8–16 EC50 Inhibitor Mouse
TRPV1 1-100 Ki Agonist Rat
De smaller de value, de stronger de interaction plus de site.

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