Glutamate and GABA in the CNS

Which neurotransmitter is characterized as a major inhibitory transmitter in the CNS?

Glutamate

Kainic acid

Gamma-aminobutyric acid (GABA) (correct)

Aspartate

Which type of glutamate receptor subtype is coupled to G proteins and leads to long-term changes in neuronal functions/neuronal plasticity?

NMDA receptors (correct)

AMPA receptors

Kainic acid receptors

Delta receptors

What is the effect of GABAA receptor activation?

Sodium ion efflux

Chloride ion influx and subsequent hyperpolarization (correct)

Neuronal excitation

Potassium ion influx

Which amino acid is characterized as an excitatory amino acid found in very high concentrations in the brain?

Glutamate Signup and view all the answers

What is the major role of glutamate in the CNS?

Neuronal excitation Signup and view all the answers

Which type of glutamate receptor subtype is characterized as an ionotropic receptor?

NMDA receptors Signup and view all the answers

What type of receptor is the GABAA receptor?

Ligand-gated Cl- ion channel Signup and view all the answers

Which ion enters the neuron upon activation of the GABAA receptor?

Chloride Signup and view all the answers

What are the two major excitatory amino acids found in very high concentrations in the brain?

Glutamate and aspartate Signup and view all the answers

Which type of glutamate receptor subtype is named after its most selective agonist that activates it?

AMPA receptors Signup and view all the answers

What type of receptor is the NMDA receptor?

Ionotropic receptor Signup and view all the answers

What happens when NMDA receptors are activated due to high/sustained stimulation?

Mg2+ ion block is removed; Na+ and Ca2+ enter neuron Signup and view all the answers

What is the primary mechanism of action of GABAB receptor activation?

Increases conductance of an associated K+ channel Signup and view all the answers

Which class of adjuvant analgesics acts by inhibiting norepinephrine and serotonin reuptake?

Tricyclic Antidepressants (TCAs) Signup and view all the answers

What is the major site of action for gabapentin in providing analgesia?

Presynaptic nerve terminals Signup and view all the answers

What is the primary action of NMDA receptor antagonists in the context of pain management?

Inhibit central sensitization Signup and view all the answers

Which class of drugs is primarily used to counter the effects of peripheral sensitization?

Antiepileptic Drugs (AEDs) Signup and view all the answers

What is the mechanism of action underlying the use of capsaicin as an analgesic?

Activates TRPV1 receptors Signup and view all the answers

What is the purported effect of rubefacients upon application?

Induce analgesia Signup and view all the answers

What is the major site of action for TCA-associated analgesia?

Presynaptic reuptake receptors Signup and view all the answers

Which neurotransmitter is primarily affected by the mechanism of action of GABAB receptor activation?

GABA Signup and view all the answers

What is the primary pharmacokinetic characteristic of gabapentin?

Renal elimination Signup and view all the answers

What is the mechanism of action underlying the use of menthol as an analgesic?

Desensitizes nociceptors Signup and view all the answers

What is the primary site of action for NMDA receptor antagonists in pain management?

Postsynaptic nerve terminals Signup and view all the answers