Excitatory Amino Acid Antagonists

Name
Excitatory Amino Acid Antagonists
Accession Number
DBCAT000940
Description

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

Drugs
DrugDrug Description
DextromethorphanAn NMDA receptor antagonist used to treat cases of dry cough.
RiluzoleA glutamate antagonist used to treat amyotrophic lateral sclerosis.
MemantineAn NMDA receptor antagonist used to treat moderate to severe dementia in Alzheimer's.
PhenobarbitalA long-lasting barbiturate and anticonvulsant used in the treatment of all types of seizures, except for absent seizures.
KetamineA rapid-acting general anesthetic and NMDA receptor antagonist used for induction of anesthesia diagnostic and surgical procedures typically in combination with a muscle relaxant.
PhencyclidineA hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to ketamine in structure and in many of its effects. Like...
FG-9041Not Available
IfenprodilN-methyl-D-aspartate (NMDA) receptors (NMDARs) are members of the ionotropic glutamate receptor family, with key roles in brain development and neurological function.[A220118, A220128] NMDARs are heterotetramers that typically involve a dimer...
Kynurenic AcidKynurenic Acid is under investigation in clinical trial NCT02340325 (FS2 Safety and Tolerability Study in Healthy Volunteers).
EliprodilEliprodil has been used in trials studying the treatment of Parkinson Disease and Movement Disorders.
GacyclidineGacyclidine has been used in trials studying the treatment of Tinnitus.
DextrorphanNot Annotated
5,7-Dichlorokynurenic acidNot Available
FelbamateAn anticonvulsant used to treat severe epilepsy.
DexanabinolInvestigated for use/treatment in traumatic brain injuries and neurologic disorders.
KetobemidoneFor the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.
GavestinelHighly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (Kd = 0.8 nM). Gavestinel displays > 1000-fold selectivity over NMDA, AMPA...
CaroverineA calcium channel blocker indicated in the treatment of smooth muscle spasms, alcohol and drug withdrawal, and tinnitus.
Drugs & Drug Targets
DrugTargetType
DextromethorphanSigma non-opioid intracellular receptor 1target
DextromethorphanNeuronal acetylcholine receptor subunit alpha-2target
DextromethorphanSodium-dependent serotonin transportertarget
DextromethorphanGlutamate receptor ionotropic, NMDA 3Atarget
DextromethorphanCytochrome P450 2D6enzyme
DextromethorphanCytochrome P450 3A4enzyme
DextromethorphanCytochrome P450 3A7enzyme
DextromethorphanCytochrome P450 2C9enzyme
DextromethorphanCytochrome P450 2B6enzyme
DextromethorphanCytochrome P450 2C19enzyme
DextromethorphanMembrane-associated progesterone receptor component 1target
DextromethorphanNeuronal acetylcholine receptor subunit alpha-3target
DextromethorphanNeuronal acetylcholine receptor subunit alpha-4target
DextromethorphanNeuronal acetylcholine receptor subunit beta-4target
DextromethorphanNeuronal acetylcholine receptor subunit beta-2target
DextromethorphanNeuronal acetylcholine receptor subunit alpha-7target
DextromethorphanMu-type opioid receptortarget
DextromethorphanDelta-type opioid receptortarget
DextromethorphanKappa-type opioid receptortarget
DextromethorphanNADPH oxidasetarget
DextromethorphanSodium-dependent noradrenaline transportertarget
DextromethorphanUDP-glucuronosyltransferase 2B4enzyme
DextromethorphanUDP-glucuronosyltransferase 2B7enzyme
DextromethorphanUDP-glucuronosyltransferase 2B15enzyme
DextromethorphanUDP-glucuronosyltransferase 2B17enzyme
RiluzoleSodium channel protein type 5 subunit alphatarget
RiluzoleCytochrome P450 1A2enzyme
RiluzoleCystine/glutamate transportertarget
RiluzoleATP-binding cassette sub-family G member 2transporter
RiluzoleCytochrome P450 1A1enzyme
MemantineCytochrome P450 2B6enzyme
MemantineSolute carrier family 22 member 2transporter
Memantine5-hydroxytryptamine receptor 3Atarget
MemantineNeuronal acetylcholine receptor subunit alpha-7target
MemantineCytochrome P450 2A6enzyme
MemantineCytochrome P450 2C19enzyme
MemantineDopamine D2 receptortarget
MemantineGlutamate receptor ionotropic, NMDA 1target
MemantineSodium/hydrogen exchanger 1transporter
MemantineSolute carrier family 22 member 4transporter
MemantineMultidrug and toxin extrusion protein 1transporter
MemantineGlutamate (NMDA) receptortarget
MemantineGABA(A) Receptortarget
MemantineGlycine receptorstarget
PhenobarbitalGamma-aminobutyric acid receptor subunit alpha-1target
PhenobarbitalCytochrome P450 2C19enzyme
PhenobarbitalCytochrome P450 2C9enzyme
PhenobarbitalCytochrome P450 2B6enzyme
PhenobarbitalCytochrome P450 2C8enzyme
PhenobarbitalCytochrome P450 1A2enzyme
PhenobarbitalCytochrome P450 3A4enzyme
PhenobarbitalCanalicular multispecific organic anion transporter 2transporter
PhenobarbitalBile salt export pumptransporter
PhenobarbitalP-glycoprotein 1transporter
PhenobarbitalMultidrug resistance-associated protein 1transporter
PhenobarbitalSolute carrier organic anion transporter family member 2A1transporter
PhenobarbitalCanalicular multispecific organic anion transporter 1transporter
PhenobarbitalNeuronal acetylcholine receptor subunit alpha-4target
PhenobarbitalNeuronal acetylcholine receptor subunit alpha-7target
PhenobarbitalGlutamate receptor 2target
PhenobarbitalGlutamate receptor ionotropic, kainate 2target
PhenobarbitalCytochrome P450 2A6enzyme
PhenobarbitalCytochrome P450 2E1enzyme
PhenobarbitalCytochrome P450 3A5enzyme
PhenobarbitalCytochrome P450 1A1enzyme
PhenobarbitalCytochrome P450 2C18enzyme
PhenobarbitalCytochrome P450 3A7enzyme
PhenobarbitalCytochrome P450 4B1enzyme
PhenobarbitalNMDA receptortarget
PhenobarbitalNuclear receptor subfamily 1 group I member 2target
PhenobarbitalUDP-glucuronosyltransferase 1-1enzyme
PhenobarbitalUDP-glucuronosyltransferase 2B7enzyme
KetamineGlutamate receptor ionotropic, NMDA 3Atarget
KetamineNeurokinin 1 receptortarget
KetamineCytochrome P450 2B6enzyme
KetamineCytochrome P450 2C9enzyme
KetamineCytochrome P450 3A4enzyme
KetamineDopamine D2 receptortarget
KetamineProstaglandin G/H synthase 1enzyme
KetamineCytochrome P450 2C8enzyme
KetamineDelta-type opioid receptortarget
KetamineSodium-dependent noradrenaline transportertarget
KetamineKappa-type opioid receptortarget
KetamineMu-type opioid receptortarget
KetamineMuscarinic acetylcholine receptortarget
Ketamine5-hydroxytryptamine receptor 2target
Ketamine5-hydroxytryptamine receptor 1target
Ketamine5-hydroxytryptamine receptor 3Atarget
KetamineNeuronal acetylcholine receptor subunit alpha-7target
KetamineCholinesterasetarget
KetamineNitric oxide synthase, braintarget
PhencyclidineGlutamate receptor ionotropic, NMDA 3Atarget
PhencyclidineSigma non-opioid intracellular receptor 1target
PhencyclidineCytochrome P450 2B6enzyme
FG-9041Glutamate receptor 2target
IfenprodilGlutamate receptor ionotropic, NMDA 1target
IfenprodilGlutamate receptor ionotropic, NMDA 2Btarget
IfenprodilG protein-activated inward rectifier potassium channel 1target
IfenprodilG protein-activated inward rectifier potassium channel 2target
IfenprodilG protein-activated inward rectifier potassium channel 4target
Kynurenic AcidAryl hydrocarbon receptortarget
Kynurenic AcidG-protein coupled receptor 35target
5,7-Dichlorokynurenic acidGlutamate receptor ionotropic, NMDA 1target
FelbamateGlutamate receptor ionotropic, NMDA 2Btarget
FelbamateGlutamate receptor ionotropic, NMDA 2Atarget
FelbamateCytochrome P450 2C19enzyme
FelbamateCytochrome P450 3A4enzyme
FelbamateCytochrome P450 2E1enzyme
FelbamateCytochrome P450 2C9enzyme
DexanabinolTumor necrosis factortarget
KetobemidoneProstaglandin G/H synthase 1enzyme
KetobemidoneCytochrome P450 2C9enzyme
KetobemidoneCytochrome P450 3A4enzyme
KetobemidoneUDP-glucuronosyltransferase 1-9enzyme
KetobemidoneCytochrome P450 2B6enzyme
KetobemidoneCytochrome P450 2C19enzyme
KetobemidoneCytochrome P450 2C8enzyme
KetobemidoneMu-type opioid receptortarget
KetobemidoneKappa-type opioid receptortarget
KetobemidoneDelta-type opioid receptortarget
KetobemidoneNMDA receptortarget
GavestinelUDP-glucuronosyltransferase 1-1enzyme
GavestinelUDP-glucuronosyltransferase 1-3enzyme
GavestinelUDP-glucuronosyltransferase 1-9enzyme
GavestinelUDP-glucuronosyltransferase 2B4enzyme
GavestinelGlutamate (NMDA) receptortarget
CaroverineCytochrome P450 3A4enzyme