Receptors Occupancy + Effect

Question 1

What are non specific binding sites

Answer 1

Sites in the body that bind drugs but do not lead to a physiological effect

Question 2

what are the 3 sites of drug action

Answer 2

1. Pro receptor
2. Drugs that inhibit enzymes
3. Drugs that interact with non pro targets(bilateral)

Question 3

What is considered a first messenger

Answer 3

The ligand (ach, other neurotransmitters)

Question 4

What are examples of 2nd messengers

Answer 4

Calcium
Adenyly Cyclase
Cyclic amp
Cyclic Gmp
Insulin

Question 5

What do ligand channels do and what are 2 examples of them

Answer 5

Allows rapid movenert or ions down conc gradient

Nicotinic, muscarinicw

Question 6

Where are ligand gated channels found

Answer 6

• Synaptic membranes

Question 7

What does stimulation of the GABA receptor cause - what can bind to them (4)

Answer 7

Opening of. chloride channel - leads to hyper polarization and decreased neuronal excitability

Benzo, ethanol, borbituites, GABA

Question 8

How many protein subunits is the g pro coupled membrane receptor made of and how is it structured

Answer 8

• Seven stretches of hydrophobic aa that are embeded in membrane
• carboxyl terminus of receptor is intracellular and amino terminus is extracellular

Question 9

How does the g coupled receptor work (steps)

Answer 9

1. Unocupied receptor does not interact w g pro
2. occupied receptor changes shape and interacts with g pro and binds GTP
3. Alpha subunit of g pro dissociates and actibates adenylyl cyclase

Question 10

How does the insulin (enzyme linked) receptor work

Answer 10

• Inactive insulin receptor binds insulin
• Activates tyrosine kinase
• tyrosine kinase phosphorylates insulin receptor substrate (IRS)
• IRS promotes phosphorylation of proteins

Question 11

What type of drug can the intracellular recptor work on

Answer 11

Only lipid soluble drugs

Question 12

How does nuclear horomone receptors work

Answer 12

• lipophilic ligand difuses through cell membrane and binds/activates nuclear horomone receptor family
• leads to change in rate of transmission of target genes (growth, metabolism, differentiation)

Question 13

What is the structure of the nuclear horomone receptor and where is the binding domain

Answer 13

• single polypeptide that is divided into 3 domains

- ligand binding domain is in regon in the carboxyl terminus

Question 14

What are examples of ligands for nuclear horomone receptors

Answer 14

• glucocorticoids
• mineralocorticoids
• sex sterioids

Question 15

What are examples of drugs that work on the voltage gated channel

Answer 15

lidocaain- blocks Na channel

Phenytoin- Binds to and inhibits Na channel reducing the excessive neuronal activity that causes seizures