Excitatory Amino Acid Antagonists

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
DrugDrug NameDrug Indication
DB00514DextromethorphanFor treatment and relief of dry cough.
DB00555LamotrigineIndicated as adjunctive therapy for the following seizure types in patients ≥2 years of age: partial seizures/primary generalized tonic-clonic seizures/generalized seizures of Lennox-Gastaut syndrome [FDA Label]. Indicated for conversion to monotherapy in adults (≥16 years of age) with partial seizures who are receiving treatment with carbamazepine, phenytoin, phenobarbital, primidone, or valproate as the single antiepileptic drug (AED)[FDA Label]. Indicated for the maintenance treatment of Bipolar I Disorder to delay the time to occurrence of mood episodes (depression, mania, hypomania, mixed episodes) in adults (≥18 years of age) treated for acute mood episodes with standard therapy [FDA Label].
DB00740RiluzoleFor the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)
DB00996GabapentinFor the management of postherpetic neuralgia in adults and as adjunctive therapy in the treatment of partial seizures with and without secondary generalization in patients over 12 years of age with epilepsy.
DB01043MemantineFor the treatment of moderate to severe dementia of the Alzheimer's type.
DB01174PhenobarbitalFor the treatment of all types of seizures except absence seizures.
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]
DB03575PhencyclidineNot Available
DB03759FG-9041Not Available
DB06444DexanabinolInvestigated for use/treatment in traumatic brain injuries and neurologic disorders.
DB06738KetobemidoneFor the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.
DB06741GavestinelNot Available
DB08954IfenprodilNot Available
DB11937Kynurenic AcidNot Available
DB12111MK-212Not Available
DB12869EliprodilNot Available
DB13096GacyclidineNot Available
DB13835CaroverineNot Available
DB14682DextrorphanNot Available
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
DB00555LamotrigineSodium channel protein type 2 subunit alphatarget
DB00555LamotrigineUDP-glucuronosyltransferase 1-4enzyme
DB00555LamotrigineMultidrug resistance protein 1transporter
DB00555LamotrigineUDP-glucuronosyltransferase 1-3enzyme
DB00555LamotrigineDihydrofolate reductaseenzyme
DB00555Lamotrigine5-hydroxytryptamine receptor 3Atarget
DB00555LamotrigineVoltage-dependent R-type calcium channel subunit alpha-1Etarget
DB00555LamotrigineAdenosine receptor A1target
DB00555LamotrigineAdenosine receptor A2atarget
DB00555LamotrigineAlpha-1A adrenergic receptortarget
DB00555LamotrigineAlpha-2A adrenergic receptortarget
DB00555LamotrigineBeta-1 adrenergic receptortarget
DB00555LamotrigineD(1) dopamine receptortarget
DB00555LamotrigineD(2) dopamine receptortarget
DB00555LamotrigineGABA-A receptor (anion channel)target
DB00555LamotrigineGABA-A receptor (benzodiazepine site)target
DB00555LamotrigineHistamine H1 receptortarget
DB00555LamotrigineKappa-type opioid receptortarget
DB00555LamotrigineMuscarinic acetylcholine receptortarget
DB00555Lamotrigine5-hydroxytryptamine receptor 2Atarget
DB00555LamotrigineUDP-glucuronosyltransferase 1-1enzyme
DB00555LamotrigineSolute carrier family 22 member 2transporter
DB00740RiluzoleSodium channel protein type 5 subunit alphatarget
DB00740RiluzoleCytochrome P450 1A2enzyme
DB00740RiluzoleCystine/glutamate transportertarget
DB00740RiluzoleATP-binding cassette sub-family G member 2transporter
DB00740RiluzoleCytochrome P450 1A1enzyme
DB00996GabapentinAdenosine receptor A1target
DB00996GabapentinVoltage-dependent N-type calcium channel subunit alpha-1Btarget
DB00996GabapentinVoltage-dependent calcium channel subunit alpha-2/delta-1target
DB00996GabapentinVoltage-dependent calcium channel subunit alpha-2/delta-2target
DB00996GabapentinBranched-chain-amino-acid aminotransferase, cytosolicenzyme
DB00996GabapentinNMDA receptortarget
DB00996GabapentinGamma-aminobutyric acid type B receptor subunit 1target
DB00996GabapentinGamma-aminobutyric acid type B receptor subunit 2target
DB00996GabapentinCytochrome P450 3A4enzyme
DB01043MemantineGlutamate receptor ionotropic, NMDA 3Atarget
DB01043MemantineGlutamate receptor ionotropic, NMDA 2Atarget
DB01043MemantineGlutamate receptor ionotropic, NMDA 2Btarget
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
DB01174PhenobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
DB01174PhenobarbitalCytochrome P450 2C19enzyme
DB01174PhenobarbitalCytochrome P450 2C9enzyme
DB01174PhenobarbitalCytochrome P450 2B6enzyme
DB01174PhenobarbitalCytochrome P450 2C8enzyme
DB01174PhenobarbitalCytochrome P450 1A2enzyme
DB01174PhenobarbitalCytochrome P450 3A4enzyme
DB01174PhenobarbitalCanalicular multispecific organic anion transporter 2transporter
DB01174PhenobarbitalBile salt export pumptransporter
DB01174PhenobarbitalMultidrug resistance protein 1transporter
DB01174PhenobarbitalMultidrug resistance-associated protein 1transporter
DB01174PhenobarbitalSolute carrier organic anion transporter family member 2A1transporter
DB01174PhenobarbitalCanalicular multispecific organic anion transporter 1transporter
DB01174PhenobarbitalNeuronal acetylcholine receptor subunit alpha-4target
DB01174PhenobarbitalNeuronal acetylcholine receptor subunit alpha-7target
DB01174PhenobarbitalGlutamate receptor 2target
DB01174PhenobarbitalGlutamate receptor ionotropic, kainate 2target
DB01174PhenobarbitalCytochrome P450 2A6enzyme
DB01174PhenobarbitalCytochrome P450 2E1enzyme
DB01174PhenobarbitalCytochrome P450 3A5enzyme
DB01174PhenobarbitalCytochrome P450 4A11enzyme
DB01174PhenobarbitalCytochrome P450 1A1enzyme
DB01174PhenobarbitalCytochrome P450 1B1enzyme
DB01174PhenobarbitalCytochrome P450 2C18enzyme
DB01174PhenobarbitalCytochrome P450 3A7enzyme
DB01174PhenobarbitalCytochrome P450 4B1enzyme
DB01174PhenobarbitalNMDA receptortarget
DB01174PhenobarbitalNuclear receptor subfamily 1 group I member 2target
DB01174PhenobarbitalUDP-glucuronosyltransferase 1-1enzyme
DB01174PhenobarbitalUDP-glucuronosyltransferase 2B7enzyme
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
DB03575PhencyclidineGlutamate receptor ionotropic, NMDA 3Atarget
DB03575PhencyclidineSigma non-opioid intracellular receptor 1target
DB03575PhencyclidineCytochrome P450 2B6enzyme
DB03759FG-9041Glutamate receptor 2target
DB06444DexanabinolTumor necrosis factortarget
DB06738KetobemidoneProstaglandin G/H synthase 1enzyme
DB06738KetobemidoneCytochrome P450 2C9enzyme
DB06738KetobemidoneCytochrome P450 3A4enzyme
DB06738KetobemidoneUDP-glucuronosyltransferase 1-9enzyme
DB06738KetobemidoneCytochrome P450 2B6enzyme
DB06738KetobemidoneCytochrome P450 2C19enzyme
DB06738KetobemidoneCytochrome P450 2C8enzyme
DB06738KetobemidoneMu-type opioid receptortarget
DB06738KetobemidoneKappa-type opioid receptortarget
DB06738KetobemidoneDelta-type opioid receptortarget
DB06738KetobemidoneNMDA receptortarget
DB06741GavestinelUDP-glucuronosyltransferase 1-1enzyme
DB06741GavestinelUDP-glucuronosyltransferase 1-3enzyme
DB06741GavestinelUDP-glucuronosyltransferase 1-9enzyme
DB06741GavestinelUDP-glucuronosyltransferase 2B4enzyme
DB06741GavestinelGlutamate (NMDA) receptortarget
DB08954IfenprodilGlutamate receptor ionotropic, NMDA 1target
DB08954IfenprodilGlutamate receptor ionotropic, NMDA 2Btarget
DB11937Kynurenic AcidAryl hydrocarbon receptortarget
DB11937Kynurenic AcidG-protein coupled receptor 35target
DB13835CaroverineCytochrome P450 3A4enzyme