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)SiteValue (μM)TypeActionSpeciesRefNMDA (N-Methyl-D-aspartate receptor)0.25–0.66KiAntagonistHumanMOR(μ-Opioid receptor)42KiAntagonistHumanMOR2 (μ-Opioid receptor)12.1KiAntagonistHumanKOR (κ-Opioid receptor)28
25Ki
KiAntagonist
AgonistHumanσ226KiND (No data)RatD2 receptor (D2)0.5
>10Ki
KiAgonist
ND (No data)Human Muscarinic acetylcholine receptor M1 (M1)45KiND (No data)Humanα2β2 (Nicotinic acetylcholine receptor)92IC50AntagonistHumanα2β4 (Nicotinic acetylcholine receptor)29IC50AntagonistHumanAlpha-3 beta-2 nicotinic receptor (α3β2)50IC50AntagonistHumanAlpha-3 beta-4 nicotinic receptor (α3β4)9.5IC50AntagonistHumanAlpha-4 beta-2 nicotinic receptor (α4β2)72IC50AntagonistHumanAlpha-4 beta-4 nicotinic receptor (α4β4)18IC50AntagonistHumanAlpha-7 nicotinic receptor (α7)3.1 (Hydroxynorketamine)IC50Negative allosteric modulation (NAM)RatERα (Estrogen receptor alpha)0.34KiND (No data)HumanNET (Norepinephrine transporter)82–291IC50InhibitorHumanDAT (Dopamine transporter)63KiInhibitorRatHCN1 (Hyperpolarization-activated cyclic nucleotide-gated channel 1)8–16EC50InhibitorMouseTRPV11-100KiAgonistRatDe smaller de value, de stronger de interaction plus de site.

References

 External links 




Category:Analgesics
Category:Antidepressants
Category:Arylcyclohexylamines
Category:Chemical substances for emergency medicine
Category:2-Chlorophenyl compounds
Category:D2 receptor agonists
Category:Dissociative drugs
Category:Drug-facilitated sexual assault
Category:Drugs wey Pfizer develop
Category:Drugs plus unknown mechanisms of action
Category:Equine medications
Category:Euphoriants
Category:Experimental antidepressants
Category:Experimental hallucinogens
Category:General anesthetics
Category:Ketones
Category:Muscarinic antagonists
Category:Nicotinic antagonists
Category:NMDA receptor antagonists
Category:Opioid modulators
Category:Opioid receptor positive allosteric modulators
Category:Sedatives
Category:Sigma agonists
Category:Veterinary medicine
Category:Translated from MDWiki