1.3 Flashcards

1
Q

describe what full agonist is?

A

has 100% efficacy

provokes biological response

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2
Q

describe what partial agonist is?

A

less than 100% efficacy

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3
Q

describe what natural antagonist is?

A

has 0% efficacy but occupies a receptor site

blocks

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4
Q

describe what inverse agonist is?

A

binds to receptor and produces opposite effect of an agonist

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5
Q

which molecules act as molecular switch?

A

ATP

GTP

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6
Q

what removes the GDP from inactive G-proteins?

A

GEF (Guanine Exchange Factor)

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7
Q

what stimulated the G protein intrinsic GTPase activity?

A

GAP (GTPase Activating Protein

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8
Q

example for first massenger?

A

NE

NeuroTransmitters

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9
Q

5 Receptor types:

A
  1. GPCR
  2. Ion channels
  3. Receptor with enzyme activity
  4. Enzyme Activity- Linked Receptor
  5. Intracellular Receptors
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10
Q

GPCR structure

A

7TM domains

heterotrimeric (a,b,gamma)

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11
Q

a subunit of GPCR binds

A

GDP or GTP

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12
Q

what happens when the a subunit binds GTP?

A

a subunit dissociates from the beta-gamma complex

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13
Q

what breaks down cAMP?

A

phosphodiesterase

caffeine blocks it

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14
Q

Gi GPCR effects

A

inhibitory- opposing Gs activity

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

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15
Q

Gq GPCR effects

A

stimulates Phospholipase C -> converts PIP2 to IP3 and DAG

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16
Q

DAG activates:

A

PKC -> phosphorylation of stuff

17
Q

IP3 will cause:

A

sarcoplasmic reticulum and ER to release Ca++

18
Q

what will happend once Ca++ binds Calmodulin

A

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

19
Q

effects of G12/13 GPCR

A

regulates GEF
activates Rho small G proteins
activates Rho Kinase

20
Q

Excitatory Ion channel Receptor and their ligands

A
  1. Nicotinic (ACh)
  2. NMDA (Glu)
  3. AMPA (Glu)
  4. 5HT3 (Serotonin)
21
Q

Nicotinoc ACh Receptor is

A

ionotropic

22
Q

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

A

curare

23
Q

muscarinic ACh R are inhibited by

A

Atropin

24
Q

examples for receptor tyrosine kinase?

A

GF

Insulin

25
Q

steps in receptor tyrosine kinase activation?

A
ligand binding
receptor dimerize
autophosphorylation
SH2 domain
GRB2 -> SOS
Ras-GDP -> Ras-GTP
MAPK (mitogen activated protein kinase)
**also inhibirion of apoptosis
26
Q

anouther example for receptor with enzyme activity?

A

Guanylyl cyclase receptor

27
Q

example for Guanylyl cyclase receptor lignad

A

ANP

28
Q

action of Guanylyl cyclase receptor

A

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

29
Q

action of enzyme activity linked receptors?

A

JAK -> STAT