Receptors Occupancy + Effect Flashcards Preview

PA 2306- MOD 7 > Receptors Occupancy + Effect > Flashcards

Flashcards in Receptors Occupancy + Effect Deck (15)
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1
Q

What are non specific binding sites

A

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

2
Q

what are the 3 sites of drug action

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

What is considered a first messenger

A

The ligand (ach, other neurotransmitters)

4
Q

What are examples of 2nd messengers

A
Calcium
Adenyly Cyclase
Cyclic amp
Cyclic Gmp
Insulin
5
Q

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

A

Allows rapid movenert or ions down conc gradient

Nicotinic, muscarinicw

6
Q

Where are ligand gated channels found

A
  • Synaptic membranes
7
Q

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

A

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

Benzo, ethanol, borbituites, GABA

8
Q

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

A
  • Seven stretches of hydrophobic aa that are embeded in membrane
  • carboxyl terminus of receptor is intracellular and amino terminus is extracellular
9
Q

How does the g coupled receptor work (steps)

A
  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
10
Q

How does the insulin (enzyme linked) receptor work

A
  • Inactive insulin receptor binds insulin
  • Activates tyrosine kinase
  • tyrosine kinase phosphorylates insulin receptor substrate (IRS)
  • IRS promotes phosphorylation of proteins
11
Q

What type of drug can the intracellular recptor work on

A

Only lipid soluble drugs

12
Q

How does nuclear horomone receptors work

A
  • 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)
13
Q

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

A
  • single polypeptide that is divided into 3 domains

- ligand binding domain is in regon in the carboxyl terminus

14
Q

What are examples of ligands for nuclear horomone receptors

A
  • glucocorticoids
  • mineralocorticoids
  • sex sterioids
15
Q

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

A

lidocaain- blocks Na channel

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