Lecture 5

Question 1

Targets of psychiatric drugs

Answer 1

G-protein coupled receptors
Ligand-gated ion channels
Voltage gated ion channels
Enzymes
12-transmembrane domain transporteers

Question 2

Reuptake Pumps

Answer 2

Plasma membrane transporters; transport neurotransmitters from the extracellular space into the cytoplasm of the presynaptic terminals

i.e. SERT, NET, DAT

Question 3

Vesicular Transporters

Answer 3

Transport neurotransmitters from the cytoplasm to the vesicles.

i.e. Vesicular monoamine transmitter VMAT

Question 4

Cofactor for reuptake pumps?

Answer 4

Sodium

Question 5

Fluoxetine

Answer 5

Acts at the SERT

Are not carried into the presynaptic terminal they remain bound to SERT

Question 6

AChE

Answer 6

Acetylcholinesterase; rapidly breaks fown ACh into choline and acetate . Choline transporter then pumps choline in to the terminal and converted to AChE.

Question 7

VAChT

Answer 7

Vesicular ACh transporter

Question 8

GAT

Answer 8

GABA transporter

Question 9

EAAT

Answer 9

Excitatory amino acid transporter

Question 10

VGlu

Answer 10

vesicular glutamate transporter

Question 11

VIAAT

Answer 11

Vesicular inhibitory amino acid transporter

Question 12

Full Agonist

Answer 12

Completely activate i.e. morphine is a full agonist at mu opioid receptors

Question 13

Partial agonist

Answer 13

Partial agonists activate signaling to limiting degree

i.e. chantix at nicotinic ACh receptors

Question 14

Antagonists

Answer 14

Block the ability of neurotransmitters or other agonists to activate but constitutive activity is still present

i.e. naltrexone is a opioid receptor antagonist

Question 15

Inverse agonist

Answer 15

Stops all GPCR activity

i.e. cetrizine at H1 histamine receptors

Question 16

Kd

Answer 16

Dissociation constant

the concentration of a drug at which 50% of receptors are occupied

represents affinity of drug for the receptor

Question 17

Occupancy theory

Answer 17

Effectiveness of a drug is proportional to the duration the receptor is occupied

Question 18

Rate Theory

Answer 18

Effectiveness of a drug is proportional to the rate of drug receptor interactions