Lecture 5 Flashcards

1
Q

Targets of psychiatric drugs

A
G-protein coupled receptors
Ligand-gated ion channels
Voltage gated ion channels
Enzymes
12-transmembrane domain transporteers
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2
Q

Reuptake Pumps

A

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

i.e. SERT, NET, DAT

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3
Q

Vesicular Transporters

A

Transport neurotransmitters from the cytoplasm to the vesicles.

i.e. Vesicular monoamine transmitter VMAT

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4
Q

Cofactor for reuptake pumps?

A

Sodium

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5
Q

Fluoxetine

A

Acts at the SERT

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

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6
Q

AChE

A

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

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7
Q

VAChT

A

Vesicular ACh transporter

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8
Q

GAT

A

GABA transporter

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9
Q

EAAT

A

Excitatory amino acid transporter

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10
Q

VGlu

A

vesicular glutamate transporter

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11
Q

VIAAT

A

Vesicular inhibitory amino acid transporter

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12
Q

Full Agonist

A

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

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13
Q

Partial agonist

A

Partial agonists activate signaling to limiting degree

i.e. chantix at nicotinic ACh receptors

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14
Q

Antagonists

A

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

i.e. naltrexone is a opioid receptor antagonist

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15
Q

Inverse agonist

A

Stops all GPCR activity

i.e. cetrizine at H1 histamine receptors

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16
Q

Kd

A

Dissociation constant

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

represents affinity of drug for the receptor

17
Q

Occupancy theory

A

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

18
Q

Rate Theory

A

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