L1-2 PHRM20001 Receptor families

Question 1

A)Pharmocodynamics

B) Pharmacokinetics

Answer 1

A) How drug is affecting body

B) Way body deals with the drug (absorption and excretion)

Question 2

Hippocrates

Answer 2

Do no harm

Question 3

Paracelsus

Answer 3

Does determines effect

Question 4

Erlich

Answer 4

Drugs bind molecular targets

Question 5

Corpora non agunt nisi fixata

Answer 5

A drug won’t work unless bound

Question 6

Ionotropic receptors have __ subunits that are ___, receptor is located __

Answer 6

5>, a2BGammaDelta, outside

Question 7

Aspirin compared to gluococorticoids and how they affect COX

Answer 7

Aspirin - Inhibits COX (Enzyme), binds irreversibly, as COX produces mediators of pain/fever/inflammation

Gluco - activates glucocorticoid receptor to inhibit synthesis of COX

Hence aspirin used to treat acute pain where else glucocorticoids are used for chronic pain

Question 8

Cytoplasmic/Nuclear receptors, are found ___, ____ response time, how does it work?

Answer 8

Inside the membrane, slowest, ligand binds & activates intracell receptor which may regulate gene transcription through entering nucleus and binding to DNA to induce or repress genes (protein synthesis)

Question 9

Kinase-linked receptors, agonist binds to ___, and activates __

Answer 9

Extracellular domain of a transmembrane protein and activates enzymatic activity of the protein’s cytoplasmic domain

Question 10

GPCR
Receptor location
_ Transmembrane segments
_____ signalling

Answer 10

• Cell-surface receptor
• 7 transmembrane alpha helical segments aka serpentine receptor
• Metabotropic, Activates G protein that is linked -> if bound to ion channel (affects it) but if bound to enzyme (enzyme releases 2nd messenger)

Question 11

Difference between ionotropic and metabotropic

Answer 11

Ion- agonist regulates opening of ion channel

Meta - agonist binding triggers a series of intracell events that produce second messengers to indirectly produce cellular effects

Question 12

In nicotinic receptors, where do ACh bind?

Answer 12

Alpha subunits

Question 13

Example of Kinase-linked receptors

Answer 13

Growth factor receptors - agonist binding causes receptor dimerisation activation of tyrosine kinase (cytoplasmic domain). Phosphorylates substrates that regulate cell growth through gene transcription.

Question 14

Gs, Gi, Gq

Answer 14

Gs - stimulatory, increase cAMP

• > B1: increase in heart rate
• > B2: dilation of bronchi

Gi - inhibitory, decrease cAMP

Gq - Coupled to PLC which converts PIP2 -> IP3 & DAG

Question 15

Signal amplification

Answer 15

Single agonist-receptor complex can activate multiple G-protein molecules and post second messenger generation can also be amplified