1.3

Question 1

describe what full agonist is?

Answer 1

has 100% efficacy

provokes biological response

Question 2

describe what partial agonist is?

Answer 2

less than 100% efficacy

Question 3

describe what natural antagonist is?

Answer 3

has 0% efficacy but occupies a receptor site

blocks

Question 4

describe what inverse agonist is?

Answer 4

binds to receptor and produces opposite effect of an agonist

Question 5

which molecules act as molecular switch?

Answer 5

ATP

GTP

Question 6

what removes the GDP from inactive G-proteins?

Answer 6

GEF (Guanine Exchange Factor)

Question 7

what stimulated the G protein intrinsic GTPase activity?

Answer 7

GAP (GTPase Activating Protein

Question 8

example for first massenger?

Answer 8

NE

NeuroTransmitters

Question 9

5 Receptor types:

Answer 9

1. GPCR
2. Ion channels
3. Receptor with enzyme activity
4. Enzyme Activity- Linked Receptor
5. Intracellular Receptors

Question 10

GPCR structure

Answer 10

7TM domains

heterotrimeric (a,b,gamma)

Question 11

a subunit of GPCR binds

Answer 11

GDP or GTP

Question 12

what happens when the a subunit binds GTP?

Answer 12

a subunit dissociates from the beta-gamma complex

Question 13

what breaks down cAMP?

Answer 13

phosphodiesterase

caffeine blocks it

Question 14

Gi GPCR effects

Answer 14

inhibitory- opposing Gs activity

Phospholipase A2 active -> arachidonic acid release -> COX -> bla bla bla

Question 15

Gq GPCR effects

Answer 15

stimulates Phospholipase C -> converts PIP2 to IP3 and DAG

Question 16

DAG activates:

Answer 16

PKC -> phosphorylation of stuff

Question 17

IP3 will cause:

Answer 17

sarcoplasmic reticulum and ER to release Ca++

Question 18

what will happend once Ca++ binds Calmodulin

Answer 18

they can bind CaM dependent kinase which will phosphorylates Myosin Light Chain Kinase, which initates smooth muscle contraction

Question 19

effects of G12/13 GPCR

Answer 19

regulates GEF
activates Rho small G proteins
activates Rho Kinase

Question 20

Excitatory Ion channel Receptor and their ligands

Answer 20

1. Nicotinic (ACh)
2. NMDA (Glu)
3. AMPA (Glu)
4. 5HT3 (Serotonin)

Question 21

Nicotinoc ACh Receptor is

Answer 21

ionotropic

Question 22

what is the inhibitor for nicotinic ACh R in the muscle?

Answer 22

curare

Question 23

muscarinic ACh R are inhibited by

Answer 23

Atropin

Question 24

examples for receptor tyrosine kinase?

Answer 24

GF

Insulin

Question 25

steps in receptor tyrosine kinase activation?

Answer 25

``` ligand binding receptor dimerize autophosphorylation SH2 domain GRB2 -> SOS Ras-GDP -> Ras-GTP MAPK (mitogen activated protein kinase) **also inhibirion of apoptosis ```

Question 26

anouther example for receptor with enzyme activity?

Answer 26

Guanylyl cyclase receptor

Question 27

example for Guanylyl cyclase receptor lignad

Answer 27

ANP

Question 28

action of Guanylyl cyclase receptor

Answer 28

ANP binds receptor GTP -> cGMP cGMP activated PKG -> vasodilation

Question 29

action of enzyme activity linked receptors?

Answer 29

JAK -> STAT