NMDA Receptor Antagonists

DrugDrug NameDrug Indication
DB00514DextromethorphanFor treatment and relief of dry cough.
DB00915AmantadineFor the chemoprophylaxis, prophylaxis, and treatment of signs and symptoms of infection caused by various strains of influenza A virus. Also for the treatment of parkinsonism and drug-induced extrapyramidal reactions.
DB01221KetamineKetamine 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.[L1336, FDA label] Reports have indicated a potential use of ketamine as a therapeutic tool for the management of depression when administered in lower doses.[A31873] These reports have increased the interest for ketamine in this area and several clinical trials are launched for this indication.[L1337, A31874]
DB01173OrphenadrineIndicated for the treatment of Parkinson's disease.
DB00454MeperidineUsed to control moderate to severe pain.
DB08838AgmatineAgmatine is being studied experimentally for several indications such as cardioprotection, diabetes, decreased kidney function, neuroprotection (stroke, severe CNS injuries, epilepsy, glaucoma, and neuropathic pain), and psychiatric conditions (depression, anxiety, schizophrenia, and cognition). As an investigational drug, agamatine is being studied in a non-blinded prospective case study in the United States looking at patients who have been diagnosed with small fiber peripheral neuropathy.
DB08954IfenprodilNot Available
DB01520TenocyclidineBecause of its high affinity for the phencyclidine binding site on the NMDA receptor, the 3H radiolabelled form of tenocyclidine is widely used in research into NMDA receptors.
DB00502HaloperidolFor the treatment of schizophrenia [L2016] For the treatment of acute psychosis in acutely agitated schizophrenic patients with moderately severe to very severe symptoms [L2016] For the treatment of severe behavioral or psychological symptoms of dementia [L2016] For the treatment of delirium in the pediatric intensive care unit [L2016] For the treatment of agitation or delirium [L2016] For agitation† or delirium in adult patients with no underlying psychiatric illness [L2016] For use as a second-line agent for rescue treatment of chemotherapy-induced nausea/vomiting [L2016] For the treatment of irritability associated with autistic disorder [L2016] For the treatment of tics and vocal utterances associated with Tourette's syndrome [L2016] For the treatment of severe behavioral problems associated with oppositional defiant disorder or other disruptive behavioral disorders, or for the treatment of attention-deficit hyperactivity disorder (ADHD) in pediatric patients who show excessive motor activity with accompanying conduct disorders [L2016]
DB00949FelbamateFor use only in those patients who respond inadequately to alternative treatments and whose epilepsy is so severe that a substantial risk of aplastic anemia and/or liver failure is deemed acceptable in light of the benefits conferred by its use.
DB01043MemantineMemantine is used to manage moderate to severe Alzheimer's dementia [FDA label]. A more recent systemic review and meta-analysis [A177106] indicates that memantine is beneficial as a first line drug for the treatment of Alzheimer's dementia. Cholinesterase inhibitors may be added to memantine for further beneficial effects on behavioral symptoms and other symptoms of dementia [A177106].
DB01159HalothaneFor the induction and maintenance of general anesthesia
DB00333MethadoneFor the treatment of dry cough, drug withdrawal syndrome, opioid type drug dependence, and pain.
DB00392ProfenamineFor use in the treatment of Parkinson's disease and also used to control severe reactions to certain medicines such as reserpine.
DB00721ProcaineUsed as a local anesthetic primarily in oral surgery
DB00898EthanolFor therapeutic neurolysis of nerves or ganglia for the relief of intractable chronic pain in such conditions as inoperable cancer and trigeminal neuralgia (tic douloureux), in patients for whom neurosurgical procedures are contraindicated.
DB01161ChloroprocaineFor the production of local anesthesia by infiltration and peripheral nerve block. They are not to be used for lumbar or caudal epidural anesthesia.
DB03575PhencyclidineNot Available
DB00193TramadolTramadol is approved for the management of moderate to severe pain in adults.[FDA label] As an off-label indication, tramadol has been investigated to be used for the treatment of premature ejaculation.[A173986]
DrugDrug NameTargetType
DB00514DextromethorphanSigma non-opioid intracellular receptor 1target
DB00514DextromethorphanHCG20471, isoform CRA_ctarget
DB00514DextromethorphanNeuronal acetylcholine receptor subunit alpha-2target
DB00514DextromethorphanSodium-dependent serotonin transportertarget
DB00514DextromethorphanGlutamate receptor ionotropic, NMDA 3Atarget
DB00514DextromethorphanCytochrome P450 2D6enzyme
DB00514DextromethorphanCytochrome P450 3A4enzyme
DB00514DextromethorphanCytochrome P450 3A5enzyme
DB00514DextromethorphanCytochrome P450 3A7enzyme
DB00514DextromethorphanCytochrome P450 2C9enzyme
DB00514DextromethorphanCytochrome P450 2B6enzyme
DB00514DextromethorphanCytochrome P450 2C19enzyme
DB00514DextromethorphanCytochrome P450 2C8enzyme
DB00514DextromethorphanCytochrome P450 2E1enzyme
DB00514DextromethorphanMembrane-associated progesterone receptor component 1target
DB00514DextromethorphanNeuronal acetylcholine receptor subunit alpha-3target
DB00514DextromethorphanNeuronal acetylcholine receptor subunit alpha-4target
DB00514DextromethorphanNeuronal acetylcholine receptor subunit beta-4target
DB00514DextromethorphanNeuronal acetylcholine receptor subunit beta-2target
DB00514DextromethorphanNeuronal acetylcholine receptor subunit alpha-7target
DB00514DextromethorphanMu-type opioid receptortarget
DB00514DextromethorphanDelta-type opioid receptortarget
DB00514DextromethorphanKappa-type opioid receptortarget
DB00514DextromethorphanNADPH oxidasetarget
DB00514DextromethorphanSodium-dependent noradrenaline transportertarget
DB00915AmantadineD(2) dopamine receptortarget
DB00915AmantadineMatrix protein 2target
DB00915AmantadineAromatic-L-amino-acid decarboxylaseenzyme
DB00915AmantadineAmine oxidase [flavin-containing] Benzyme
DB00915AmantadineSolute carrier family 22 member 2transporter
DB00915AmantadineSolute carrier family 22 member 1transporter
DB00915AmantadineGlutamate receptor ionotropic, NMDA 3Atarget
DB00915AmantadineNeuronal acetylcholine receptor subunit alpha-7target
DB00915AmantadineNeuronal acetylcholine receptor subunit alpha-4target
DB00915AmantadineNeuronal acetylcholine receptor subunit alpha-3target
DB01221KetamineGlutamate receptor ionotropic, NMDA 3Atarget
DB01221KetamineSubstance-P receptortarget
DB01221KetamineCytochrome P450 2B6enzyme
DB01221KetamineCytochrome P450 2C9enzyme
DB01221KetamineCytochrome P450 3A4enzyme
DB01221KetamineD(2) dopamine receptortarget
DB01221KetamineProstaglandin G/H synthase 1enzyme
DB01221KetamineCytochrome P450 2C8enzyme
DB01221KetamineDelta-type opioid receptortarget
DB01221KetamineSodium-dependent noradrenaline transportertarget
DB01221KetamineKappa-type opioid receptortarget
DB01221KetamineMu-type opioid receptortarget
DB01221KetamineMuscarinic acetylcholine receptortarget
DB01221Ketamine5-hydroxytryptamine receptor 2target
DB01221Ketamine5-hydroxytryptamine receptor 1target
DB01221Ketamine5-hydroxytryptamine receptor 3Atarget
DB01221KetamineAlpha-7 nicotinic cholinergic receptor subunittarget
DB01221KetamineCholinesterasetarget
DB01221KetamineNitric oxide synthase, braintarget
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 1target
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 2Dtarget
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 3Btarget
DB01173OrphenadrineGlutamate receptor ionotropic, NMDA 3Atarget
DB01173OrphenadrineHistamine H1 receptortarget
DB01173OrphenadrineCytochrome P450 2B6enzyme
DB01173OrphenadrineCytochrome P450 2E1enzyme
DB01173OrphenadrineCytochrome P450 3A4enzyme
DB01173OrphenadrineSodium-dependent noradrenaline transportertarget
DB01173OrphenadrineSodium channel protein type 10 subunit alphatarget
DB01173OrphenadrineCytochrome P450 1A2enzyme
DB00454MeperidineKappa-type opioid receptortarget
DB00454MeperidineCytochrome P450 2D6enzyme
DB00454MeperidineCytochrome P450 2B6enzyme
DB00454MeperidineGlutamate receptor ionotropic, NMDA 1target
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Btarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Atarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Ctarget
DB00454MeperidineGlutamate receptor ionotropic, NMDA 2Dtarget
DB00454MeperidineCytochrome P450 2C19enzyme
DB00454MeperidineCytochrome P450 3A4enzyme
DB00454MeperidineSerum albumincarrier
DB00454MeperidineAlpha-1-acid glycoprotein 1carrier
DB00454MeperidineMuscarinic acetylcholine receptortarget
DB00454MeperidineMu-type opioid receptortarget
DB00454MeperidineSodium-dependent dopamine transportertarget
DB00454MeperidineSodium-dependent noradrenaline transportertarget
DB00454MeperidineSodium-dependent serotonin transportertarget
DB00454MeperidineLiver carboxylesterase 1target
DB00454MeperidineCytochrome P450 1A2enzyme
DB08838AgmatineSolute carrier family 22 member 1transporter
DB08838AgmatineSolute carrier family 22 member 2transporter
DB08838AgmatineSolute carrier family 22 member 3transporter
DB08838AgmatineAlpha-2C adrenergic receptortarget
DB08838AgmatineNischarintarget
DB08838AgmatineAcetylcholine receptor subunit alphatarget
DB08838AgmatineGlutamate receptor ionotropic, NMDA 1target
DB08838AgmatineATP-sensitive inward rectifier potassium channel 1target
DB08838AgmatineVoltage-dependent N-type calcium channel subunit alpha-1Btarget
DB08838AgmatineAcid-sensing ion channel 3target
DB08838AgmatineY+L amino acid transporter 1transporter
DB08838AgmatineCytochrome P450 3A4enzyme
DB08954IfenprodilGlutamate receptor ionotropic, NMDA 1target
DB08954IfenprodilGlutamate receptor ionotropic, NMDA 2Btarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 3Atarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 3Btarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 2Atarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 2Ctarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 2Btarget
DB01520TenocyclidineGlutamate receptor ionotropic, NMDA 2Dtarget
DB01520TenocyclidineAlpha-7 nicotinic cholinergic receptor subunittarget
DB00502HaloperidolD(2) dopamine receptortarget
DB00502HaloperidolGlutamate receptor ionotropic, NMDA 2Btarget
DB00502HaloperidolD(1A) dopamine receptortarget
DB00502HaloperidolCytochrome P450 1A2enzyme
DB00502HaloperidolCytochrome P450 2D6enzyme
DB00502Haloperidol5-hydroxytryptamine receptor 2Atarget
DB00502HaloperidolD(3) dopamine receptortarget
DB00502HaloperidolCytochrome P450 3A4enzyme
DB00502HaloperidolCytochrome P450 3A5enzyme
DB00502HaloperidolCytochrome P450 3A7enzyme
DB00502HaloperidolMultidrug resistance protein 1transporter
DB00502HaloperidolCarbonyl reductase [NADPH] 1enzyme
DB00502HaloperidolUDP-glucuronosyltransferase 1-9enzyme
DB00502HaloperidolCytochrome P450 1A1enzyme
DB00502HaloperidolCytochrome P450 2C19enzyme
DB00502HaloperidolCytochrome P450 2C9enzyme
DB00502HaloperidolMelanin-concentrating hormone receptor 1target
DB00502HaloperidolSynaptic vesicular amine transportertarget
DB00949FelbamateGlutamate receptor ionotropic, NMDA 3Atarget
DB00949FelbamateGlutamate receptor ionotropic, NMDA 2Btarget
DB00949FelbamateGlutamate receptor ionotropic, NMDA 2Atarget
DB00949FelbamateCytochrome P450 2C19enzyme
DB00949FelbamateCytochrome P450 3A4enzyme
DB00949FelbamateCytochrome P450 2E1enzyme
DB00949FelbamateCytochrome P450 2C9enzyme
DB01043MemantineCytochrome P450 2B6enzyme
DB01043MemantineSolute carrier family 22 member 2transporter
DB01043Memantine5-hydroxytryptamine receptor 3Atarget
DB01043MemantineAlpha-7 nicotinic cholinergic receptor subunittarget
DB01043MemantineCytochrome P450 2A6enzyme
DB01043MemantineCytochrome P450 2C19enzyme
DB01043MemantineD(2) dopamine receptortarget
DB01043MemantineGlutamate receptor ionotropic, NMDA 1target
DB01043MemantineSodium/hydrogen exchanger 1transporter
DB01043MemantineSolute carrier family 22 member 4transporter
DB01043MemantineMultidrug and toxin extrusion protein 1transporter
DB01043MemantineGlutamate (NMDA) receptortarget
DB01043MemantineGABA-A receptor (anion channel)target
DB01043MemantineGlycine receptorstarget
DB01159HalothaneGamma-aminobutyric acid receptor subunit alpha-1target
DB01159HalothaneGlycine receptor subunit alpha-1target
DB01159HalothaneCalcium-activated potassium channel subunit alpha-1target
DB01159HalothaneCalcium-transporting ATPase type 2C member 1target
DB01159HalothaneNADH-ubiquinone oxidoreductase chain 1target
DB01159HalothaneIntermediate conductance calcium-activated potassium channel protein 4target
DB01159HalothaneATP synthase subunit delta, mitochondrialtarget
DB01159HalothaneRhodopsintarget
DB01159HalothaneG protein-activated inward rectifier potassium channel 2target
DB01159HalothaneG protein-activated inward rectifier potassium channel 1target
DB01159HalothaneGuanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2target
DB01159HalothaneNeuropeptide S receptortarget
DB01159HalothaneCytochrome P450 2E1enzyme
DB01159HalothaneCytochrome P450 2A6enzyme
DB01159HalothaneCytochrome P450 3A4enzyme
DB01159HalothaneGlutamate receptor ionotropic, NMDA 3Atarget
DB01159HalothaneGlutamate receptor ionotropic, NMDA 3Btarget
DB01159HalothaneGlutamate receptor ionotropic, NMDA 2Atarget
DB01159HalothanePotassium channel subfamily K member 3target
DB01159HalothanePotassium channel subfamily K member 9target
DB01159HalothaneSerum albumincarrier
DB01159HalothaneCytochrome P450 2B6enzyme
DB01159HalothaneCytochrome P450 2C9enzyme
DB01159HalothaneGABA-A receptor (anion channel)target
DB00333MethadoneGlutamate receptor ionotropic, NMDA 3Atarget
DB00333MethadoneMu-type opioid receptortarget
DB00333MethadoneNeuronal acetylcholine receptor subunit alpha-10target
DB00333MethadoneCytochrome P450 2B6enzyme
DB00333MethadoneCytochrome P450 3A4enzyme
DB00333MethadoneCytochrome P450 2C19enzyme
DB00333MethadoneDelta-type opioid receptortarget
DB00333MethadoneCytochrome P450 3A5enzyme
DB00333MethadoneCytochrome P450 3A7enzyme
DB00333MethadoneCytochrome P450 2D6enzyme
DB00333MethadoneMultidrug resistance protein 1transporter
DB00333MethadoneCytochrome P450 2C8enzyme
DB00333MethadoneCytochrome P450 19A1enzyme
DB00333MethadoneCytochrome P450 1A2enzyme
DB00333MethadoneCytochrome P450 2C18enzyme
DB00333MethadoneCytochrome P450 2C9enzyme
DB00333Methadone5-hydroxytryptamine receptor 3Atarget
DB00333MethadoneLymphocyte antigen 96target
DB00333MethadoneAlpha-1-acid glycoprotein 2target
DB00333MethadoneThyroxine-binding globulincarrier
DB00392ProfenamineGlutamate receptor ionotropic, NMDA 3Atarget
DB00392ProfenamineMuscarinic acetylcholine receptor M1target
DB00392ProfenamineCholinesteraseenzyme
DB00392ProfenamineMuscarinic acetylcholine receptor M2target
DB00721ProcaineSodium channel protein type 10 subunit alphatarget
DB00721ProcaineGlutamate receptor ionotropic, NMDA 3Atarget
DB00721Procaine5-hydroxytryptamine receptor 3Atarget
DB00721ProcaineSodium-dependent dopamine transportertarget
DB00721ProcaineNeuronal acetylcholine receptor subunit alpha-2target
DB00721ProcaineCholinesteraseenzyme
DB00721ProcaineDNAtarget
DB00721ProcaineCalcium-activated potassium channeltarget
DB00721ProcainePhospholipase A2target
DB00721ProcaineLysophospholipasetarget
DB00721ProcaineMonoamine oxidasetarget
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-1target
DB00898EthanolGlutamate receptor ionotropic, NMDA 3Atarget
DB00898EthanolGlycine receptor subunit alpha-1target
DB00898EthanolGlycine receptor subunit alpha-2target
DB00898EthanolCytochrome P450 2E1enzyme
DB00898EthanolCytochrome P450 1A1enzyme
DB00898EthanolCytochrome P450 1A2enzyme
DB00898EthanolCytochrome P450 2B6enzyme
DB00898EthanolCytochrome P450 2C19enzyme
DB00898EthanolCytochrome P450 2C9enzyme
DB00898EthanolCytochrome P450 3A4enzyme
DB00898EthanolCytochrome P450 4A11enzyme
DB00898EthanolAlcohol dehydrogenase 1Aenzyme
DB00898EthanolAlcohol dehydrogenase 1Benzyme
DB00898EthanolAlcohol dehydrogenase 1Cenzyme
DB00898EthanolAlcohol dehydrogenase class-3enzyme
DB00898EthanolVoltage-dependent L-type calcium channel subunit beta-1target
DB00898Ethanol5-hydroxytryptamine receptor 3Atarget
DB00898EthanolAlcohol dehydrogenase 4enzyme
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-2target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-10target
DB00898EthanolVoltage-dependent L-type calcium channel subunit alpha-1Ctarget
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-5target
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-4target
DB00898EthanolAlcohol dehydrogenase class 4 mu/sigma chainenzyme
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-3target
DB00898EthanolGlutamate receptor 1target
DB00898EthanolVoltage-dependent calcium channel gamma-1 subunittarget
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-2target
DB00898EthanolGamma-aminobutyric acid receptor subunit alpha-6target
DB00898EthanolGlutamate receptor 2target
DB00898EthanolGlutamate receptor 4target
DB00898EthanolGlutamate receptor 3target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-4target
DB00898EthanolNeuronal acetylcholine receptor subunit beta-2target
DB00898EthanolG protein-activated inward rectifier potassium channel 1target
DB00898EthanolG protein-activated inward rectifier potassium channel 2target
DB00898EthanolVascular cell adhesion protein 1target
DB00898EthanolEquilibrative nucleoside transporter 1target
DB00898EthanolG protein-activated inward rectifier potassium channel 4target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-7target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-9target
DB00898EthanolGamma-aminobutyric acid receptor subunit beta-1target
DB00898EthanolGamma-aminobutyric acid receptor subunit beta-3target
DB00898EthanolGamma-aminobutyric acid receptor subunit beta-2target
DB00898EthanolVoltage-dependent L-type calcium channel subunit alpha-1Starget
DB00898EthanolVoltage-dependent L-type calcium channel subunit alpha-1Dtarget
DB00898EthanolAlcohol dehydrogenase 6enzyme
DB00898EthanolNeuronal acetylcholine receptor subunit beta-4target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-3target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-5target
DB00898EthanolNeuronal acetylcholine receptor subunit alpha-6target
DB00898EthanolNeuronal acetylcholine receptor subunit beta-3target
DB00898EthanolGamma-aminobutyric acid receptor subunit gamma-1target
DB00898EthanolGamma-aminobutyric acid receptor subunit gamma-3target
DB00898EthanolGamma-aminobutyric acid receptor subunit epsilontarget
DB00898EthanolGamma-aminobutyric acid receptor subunit pitarget
DB00898EthanolGamma-aminobutyric acid receptor subunit thetatarget
DB00898EthanolGamma-aminobutyric acid receptor subunit deltatarget
DB00898EthanolAlcohol dehydrogenase [NADP(+)]enzyme
DB00898EthanolEquilibrative nucleoside transporter 2target
DB00898Ethanol5-hydroxytryptamine receptor 3Etarget
DB00898Ethanol5-hydroxytryptamine receptor 3Btarget
DB00898Ethanol5-hydroxytryptamine receptor 3Dtarget
DB00898Ethanol5-hydroxytryptamine receptor 3Ctarget
DB00898EthanolVoltage-dependent calcium channel gamma-2 subunittarget
DB00898EthanolG protein-activated inward rectifier potassium channel 3target
DB00898EthanolNeural cell adhesion molecule L1target
DB01161ChloroprocaineSodium channel protein type 10 subunit alphatarget
DB01161ChloroprocaineNeuronal acetylcholine receptor subunit alpha-10target
DB01161ChloroprocaineSodium-dependent dopamine transportertarget
DB01161ChloroprocaineGlutamate receptor ionotropic, NMDA 3Atarget
DB01161Chloroprocaine5-hydroxytryptamine receptor 3Atarget
DB01161ChloroprocaineCholinesteraseenzyme
DB03575PhencyclidineGlutamate receptor ionotropic, NMDA 3Atarget
DB03575PhencyclidineSigma non-opioid intracellular receptor 1target
DB03575PhencyclidineCytochrome P450 2B6enzyme
DB00193TramadolMu-type opioid receptortarget
DB00193TramadolSodium-dependent noradrenaline transportertarget
DB00193Tramadol5-hydroxytryptamine receptor 2Ctarget
DB00193TramadolKappa-type opioid receptortarget
DB00193TramadolSodium-dependent serotonin transportertarget
DB00193TramadolCytochrome P450 2D6enzyme
DB00193TramadolDelta-type opioid receptortarget
DB00193TramadolCytochrome P450 3A4enzyme
DB00193TramadolCytochrome P450 2B6enzyme
DB00193TramadolGlutamate receptor ionotropic, NMDA 3Atarget
DB00193TramadolAlpha-7 nicotinic cholinergic receptor subunittarget
DB00193TramadolMuscarinic acetylcholine receptor M3target
DB00193TramadolMuscarinic acetylcholine receptor M1target
DB00193TramadolUDP-glucuronosyltransferase 1-1enzyme
DB00193TramadolMultidrug resistance protein 1transporter