CNS Neuropharmacology

Question 1

The main excitatory neurotransmitter in the CNS is ________, while the main inhibitory neurotransmitter is __________.

Answer 1

glutamate; GABA

Question 2

5HT and indoleamines are other names for __________.

Answer 2

serotonin

Question 3

GABA is formed from glutamate via ____________.

Answer 3

GAD (glutamic acid decarboxylase)

Question 4

How is GABA signalling primarily terminated?

Answer 4

By reuptake into the presynaptic terminal

Question 5

Describe two drugs that prolong/strengthen the GABA signal.

Answer 5

Tiagabine (by inhibiting the reuptake of GABA) and vigabactrin (by inhibiting the degradation)

Question 6

Describe how GABA(A) and GABA(B) work.

Answer 6

They are both inhibitory, but GABA(A) is ionotropic and exerts its effect by opening a chloride channel – which hyperpolarizes the cell. GABA(B) is metabotropic and works by inhibiting adenylyl cyclase – which then decreases calcium conductance and opens potassium channels (both of which hyperpolarize the membrane).

Question 7

Acetylcholine is synthesized by ____________ and degraded by _____________.

Answer 7

choline acetyl transferase (CAT); choline esterase

Question 8

Acetylcholine is pumped into vesicles by the protein ______________.

Answer 8

vesicle-associated transporter (VAT)

Question 9

There are five subtypes of muscarinic acetylcholine channels (M1 - M5). List the mechanisms of each.

Answer 9

M1, M3, M5: Gq stimulation of PLC (GQ is a magazine for men… “the odd man out)
M2, M4: inhibit adenylyl cyclase

Question 10

The rate-limiting enzyme for both dopamine and the catecholamines is ____________.

Answer 10

tyrosine hydroxylase

Question 11

The adrenergic system has four receptors: alpha-1, alpha-2, beta-1, and beta-2. List the mechanism by which each works.

Answer 11

Alpha-1: Gq stimulates PLC
Alpha-2: Gi/o inhibits adenylyl cyclase and opens K channels
Beta-1 and beta-2: stimulates adenylyl cyclase

Question 12

Hierarchical neuron systems are found in delineated pathways such as ____________.

Answer 12

motor and sensory tracts

Question 13

Baclofen is a _________ agonist.

Answer 13

GABA(B)

Question 14

What drug is a GABA(A) antagonist?

Answer 14

Flumazenil

Question 15

Seizures can result from depressed activity of which receptor?

Answer 15

GABA(A) –this is why benzodiazepines are given to those having seizures!

Question 16

What two receptors does lamotrigine block?

Answer 16

Voltage-gated sodium channels and voltage-gated calcium channels

Question 17

Ketamine is an antagonist of the __________ channels.

Answer 17

NMDA

Question 18

Lamotrigine is used to treat __________.

Answer 18

seizures

Question 19

What kind of receptors are NMDA and AMPA?

Answer 19

Ionotropic glutamate receptors

Question 20

Dopamine and norepinephrine only bind to _____________ receptors.

Answer 20

metabotropic

Question 21

Black widow venom works by _____________.

Answer 21

increasing acetylcholine release

Question 22

What is the generic name for Chantix?

Answer 22

Varenicline

Question 23

__________ is an indirect alpha-1 adrenergic agonist.

Answer 23

Pseudophedrine

Question 24

___________ is an alpha-2 adrenergic agonist.

Answer 24

Clonidine

Question 25

Parkinson’s results from decreased __________ activity in the nigostriatal pathway.

Answer 25

dopamine