Repositioning Candidate Details

Candidate ID: R0452
Source ID: DB01221
Source Type: approved; vet_approved
Compound Type: small molecule
Compound Name: Ketamine
Synonyms: (+-)-Ketamine; (±)-ketamine; 2-(2-Chloro-phenyl)-2-methylamino-cyclohexanone; 2-(methylamino)-2-(2-chlorophenyl)cyclohexanone; 2-(o-chlorophenyl)-2-(methylamino)-cyclohexanone; DL-ketamine; Ketamine; NMDA; Special K
Molecular Formula: C13H16ClNO
SMILES: CNC1(CCCCC1=O)C1=CC=CC=C1Cl
Structure:
DrugBank Description: Ketamine is an NMDA receptor antagonist with a potent anesthetic effect. It was developed in 1963 as a replacement for phencyclidine (PCP) by Calvin Stevens at Parke Davis Laboratories. It started being used for veterinary purposes in Belgium and in 1964 was proven that compared to PCP, it produced minor hallucinogenic effects and shorter psychotomimetic effects. It was FDA approved in 1970, and from there, it has been used as an anesthetic for children or patients undergoing minor surgeries but mainly for veterinary purposes.
CAS Number: 6740-88-1
Molecular Weight: 237.725
DrugBank Indication: Ketamine is indicated as an anesthetic agent for recommended diagnostic and surgical procedures. If skeletal muscle relaxation is needed, it should be combined with a muscle relaxant. If the surgical procedure involves visceral pain, it should be supplemented with an agent that obtunds visceral pain. Ketamine can be used for induction of anesthesia prior other general anesthetic agents and as a supplement of low potency agents. Reports have indicated a potential use of ketamine as a therapeutic tool for the management of depression when administered in lower doses. These reports have increased the interest for ketamine in this area and several clinical trials are launched for this indication.
DrugBank Pharmacology: Ketamine is a rapid-acting general anesthetic producing an anesthetic state characterized by profound analgesia, normal pharyngeal-laryngeal reflexes, normal or slightly enhanced skeletal muscle tone, cardiovascular and respiratory stimulation, and occasionally a transient and minimal respiratory depression. The anesthetic state produced by Ketamine has been termed as "dissociative anesthesia" in that it appears to selectively interrupt association pathways of the brain before producing somesthetic sensory blockade. It may selectively depress the thalamoneocortical system before significantly obtunding the more ancient cerebral centers and pathways (reticular-activating and limbic systems). Ketamine enhances descending inhibiting serotoninergic pathways and can exert antidepressive effects. These effects are seen in concentrations ten times lower than the needed concentration for anesthetic proposes. The effect of ketamine can be described as analgesic by the prevention of central sensitization in dorsal horn neurons as well as by the inhibition on the synthesis of nitric oxide. Ketamine can present cardiovascular changes and bronchodilatation.
DrugBank MoA: Ketamine interacts with N-methyl-D-aspartate (NMDA) receptors, opioid receptors, monoaminergic receptors, muscarinic receptors and voltage sensitive Ca ion channels. Unlike other general anaesthetic agents, ketamine does not interact with GABA receptors.
Targets: Glutamate receptor ionotropic, NMDA 3A antagonist; Neurokinin 1 receptor antagonist; Dopamine D2 receptor agonist&partial agonist; Delta-type opioid receptor binder; Sodium-dependent noradrenaline transporter inhibitor; Kappa-type opioid receptor agonist; Mu-type opioid receptor binder; Muscarinic acetylcholine receptor binder; 5-hydroxytryptamine receptor 2 antagonist; 5-hydroxytryptamine receptor 1 antagonist; 5-hydroxytryptamine receptor 3A potentiator; Alpha-7 nicotinic cholinergic receptor subunit antagonist; Cholinesterase inhibitor; Nitric oxide synthase, brain inhibitor
Inclusion Criteria: Indication associated