Ch.8 Glutamate & GABA

What is the clinical use of Riluzole?

ALS – prolongs survival

What is the mechanism or receptor for Riluzole?

Reduces glutamate release and increases reuptake (indirect glutamate effect)

What is the clinical use of Nuedexta?

ALS; Pseudobulbar Affect

What is the mechanism or receptor for Nuedexta?

NMDA antagonist

What is the clinical use of Radicava (Edaravone)?

ALS – slows decline, antioxidant

What is the mechanism or receptor for Radicava (Edaravone)?

Free radical scavenger (indirect glutamate-related action)

What is the clinical use of Phencyclidine (PCP)?

Hallucinogen

What is the mechanism or receptor for Phencyclidine (PCP)?

NMDA receptor antagonist

What is the clinical use of Ketamine?

Anesthetic / antidepressant

What is the mechanism or receptor for Ketamine?

NMDA receptor antagonist on GABA interneurons

What is the clinical use of CX-717 (Ampakine)?

ADHD / Alzheimer’s / cognitive enhancement

What is the mechanism or receptor for CX-717 (Ampakine)?

AMPA positive allosteric modulator receptor

What is the clinical use of Selfotel?

Stroke (experimental, discontinued)

What is the mechanism or receptor for Selfotel?

NMDA receptor antagonist

What is the clinical use of Domoic acid?

Excitotoxin from algae

What is the mechanism or receptor for Domoic acid?

AMPA / kainate receptor agonist

What is the clinical use of Vigabatrin?

Epilepsy

What is the mechanism or receptor for Vigabatrin?

Inhibits GABA transaminase (GABA-T)

What is the clinical use of Tiagabine?

Epilepsy

What is the mechanism or receptor for Tiagabine?

Inhibits GABA transporter (GAT-1)

What is the clinical use of Picrotoxin?

Convulsant (experimental); possibly for Down’s syndrome

What is the mechanism or receptor for Picrotoxin?

GABA_A antagonist

What is the clinical use of Pentylenetetrazol (Metrazol)?

Convulsant (experimental)

What is the mechanism or receptor for Pentylenetetrazol (Metrazol)?

GABA_A antagonist

What is the clinical use of Bicuculline?

Convulsant (experimental)

What is the mechanism or receptor for Bicuculline?

GABA_A antagonist

What is the clinical use of Muscimol?

Hallucinogen / research tool

What is the mechanism or receptor for Muscimol?

GABA_A agonist

What is the clinical use of Ethanol?

Depressant / sedative

What is the mechanism or receptor for Ethanol?

GABA_A positive allosteric modulator

What is the clinical use of Flumazenil?

Reverses benzodiazepine overdose

What is the mechanism or receptor for Flumazenil?

GABA_A antagonist

What is the clinical use of Ro15-4513?

Experimental ethanol antidote

What is the mechanism or receptor for Ro15-4513?

GABA_A modulator

What is the clinical use of Baclofen (Lioresal)?

Muscle relaxant / antispastic

What is the mechanism or receptor for Baclofen (Lioresal)?

GABA_B agonist

What is the clinical use of Propofol?

IV anesthetic

What is the mechanism or receptor for Propofol?

GABA_A positive allosteric modulator

What is the clinical use of Benzodiazepines?

Anxiolytic / sedative / anticonvulsant

What is the mechanism or receptor for Benzodiazepines?

GABA_A positive allosteric modulator