Corso - Metabotropic Receptors

what neurotransmitter activates the D1 receptor?

a. dopamine

b. norepinephrine & epinephrine

c. histamine

a.

what neurotransmitter activates the beta-1 receptor?

a. dopamine

b. norepinephrine & epinephrine

c. histamine

b.

what neurotransmitter activates the H2 receptor?

a. dopamine

b. norepinephrine & epinephrine

c. histamine

c.

G-alpha-s cascade:

after the transmitter binds to heptahelical receptors, this activates the _______

which then kicks out _____ and binds ______

causing the G-alpha-s subunit with the GTP bound to ________

this activates ________

which converts _____ —> ______

which activates _______

transmitter binds —> activates the trimeric G-protein

kicks out GDP and binds GTP

G-alpha-s subunit with GTP bound separates

activates adenylyl cyclase

converts AMP —> cAMP

activates protein kinase A

why are G-proteins called GTPases?

turn on when they bind GTP

turn off when they hydrolyse GTP to GDP

how do phosphodiesterases control the concentration of cAMP?

decrease the levels of cAMP

hydrolyze it to AMP

how does PKA control metabolism and gene expression?

phosphorylates enzymes, turning catabolic enzymes ON and anabolic enzymes OFF

enters the nucleus and phosphorylates CREB, turning ON gene expression of catabolic enzymes

phosphorylates serines and threonines

list the receptors that activate G alpha s

D1

beta 1, 2, 3

glucagon receptor

H2

list the receptors that activate G alpha i

m2

D2

alpha 2

5HT1

mGluR2

CB1 and CB2 (cannabinoid receptors)

list the receptors that activate G alpha q

G alpha q activates PLC —> DAG + IP3

m1

alpha 1

5HT2

mGluR1

H1

what neurotransmitter activates NMDA?

glutamate

what neurotransmitter activates the m2 receptor?

acetyl choline

what neurotransmitter activates the beta 1, 2, and 3 receptors?

norepinephrine

epinephrine

what happens when glycine receptors are activated?

chloride ions go inward

what happens when beta-2 receptors are activated?

activation of G-alpha-s

increased cAMP and PKA

what happens when GABA-B receptors are activated?

potassium ions go outward

what happens when m2 receptors are activated?

G-alpha-i is activated

decreased cAMP and decreased PKA activity

what happens when 5HT3 receptors are activated?

sodium ions go inward

what happens when 5HT-2 receptors are activated?

G-alpha-q is activated

increased DAG, IP3, and calcium

PKC activated

what receptor does ATP activate?

P2X

what receptors does glutamate activate?

AMPA

kainate

NMDA

mGluR1/2

what receptors does histamine activate?

H 1/2

what receptors does GABA activate?

GABA-A, B, C

what receptors do enkephalins and endorphins activate?

mu

delta

what receptors does acetylcholine activate?

m 1/2

N 1/2

what receptors does serotonin activate?

5HT 1/2/3

what receptors does epinephrine and norepinephrine activate?

alpha 1/2

beta 1/2/3

what receptors does dopamine activate?

D 1/2

____ activates PKA

cAMP

why is the half-life of cAMP limited?

cAMP phosphodiesterases converts it to AMP

cAMP activates PKA which is a Ser/Thr kinase that phosphorylates _____

numerous target enzymes

-CREB (transcription activator)

what is a kinase?

enzyme that phosphorylates other proteins on Tyr, Ser, Thr, or His

PKA, PKB, PKC, and PKG are _______ kinases

insulin-like receptors are ______ kinases

PKA, PKB, PKC, and PKG are serine/threonine kinases

insulin-like receptors are tyrosine kinases

which are excitatory G proteins?

a. G-alpha-s

b. G-alpha-i

c. G-alpha-q

a.

c.

which are inhibitory G proteins?

a. G-alpha-s

b. G-alpha-i

c. G-alpha-q

b.

nerve growth factor (NGF) is a ___________ growth factor

insulin-like

describe the signaling cascade when G-alpha-q is activated

G-alpha-q activates PLC

PLC cleaves PIP2 —> DAG + IP3

IP3 opens calcium channel

DAG + Calcium activates PKC

PIP2 is phosphorylated —> PIP3

PIP3 activates PKB

______ activates PKG

cGMP

nitric oxide (NO) is made from ______ and causes ______

made from arginine

causes vasodilation

classify the acetylcholine receptor classes

which receptors are fast?

a. nicotinic

b. muscarinic

a.

classify the acetylcholine receptor classes

which receptors are slower?

a. nicotinic

b. muscarinic

b.

classify the acetylcholine receptor classes

which receptors are excitatory? (SATA)

a. N1

b. N2

c. m1

d. m2

e. m3

f. m4

g. m5

a.

b.

c.

e.

g.

all nicotinic

odd numbered muscarinic

classify the acetylcholine receptor classes

which receptors are inhibitory?

a. N1

b. N2

c. m1

d. m2

e. m3

f. m4

g. m5

d.

f.

even numbered muscarinics

where are N1 (nicotinic) receptors found?

N2?

N1: muscles

N2: neurons

_____ activates N1 and N2, which are _____ and activate ________

acetylcholine

excitatory

activates ligand gated sodium channels

m1, m3, and m5 receptors are ______ via _____

excitatory

via G-alpha-q

-increases IP3 and DAG

m2 and m4 are _______ via ________

inhibitory

via G-alpha-i

-decreases cAMP

what dopamine receptors are excitatory (increase cAMP)? (SATA)

a. D1

b. D2

c. D3

d. D4

e. D5

a.

e.

first and last

what dopamine receptors are inhibitory (decrease cAMP)? (SATA)

a. D1

b. D2

c. D3

d. D4

e. D5

b.

c.

d.

middle

which adrenergic receptors (activated by norepinephrine and epinephrine) are excitatory, increasing IP3 and DAG? (SATA)

a. alpha 1

b. alpha 2

c. beta 1

d. beta 2

e. beta 3

a.

which adrenergic receptors (activated by norepinephrine and epinephrine) are excitatory, increasing cAMP? (SATA)

a. alpha 1

b. alpha 2

c. beta 1

d. beta 2

e. beta 3

c.

d.

e,

which adrenergic receptors (activated by norepinephrine and epinephrine) are inhibitory, decreasing cAMP? (SATA)

a. alpha 1

b. alpha 2

c. beta 1

d. beta 2

e. beta 3

b.

what serotonin receptor is excitatory, increasing IP3 and DAG?

a. 5-HT 1

b. 5-HT 2

c. 5-HT 3

d. 5-HT 4, 6, & 7

e. 5-HT 5

b.

what serotonin receptor is excitatory, activating ligand gated sodium channels?

a. 5-HT 1

b. 5-HT 2

c. 5-HT 3

d. 5-HT 4, 6, & 7

e. 5-HT 5

c.

what serotonin receptor is excitatory, increasing cAMP?

a. 5-HT 1

b. 5-HT 2

c. 5-HT 3

d. 5-HT 4, 6, & 7

e. 5-HT 5

d.

what serotonin receptors are inhibitory (decreasing cAMP)? (SATA)

a. 5-HT 1

b. 5-HT 2

c. 5-HT 3

d. 5-HT 4, 6, & 7

e. 5-HT 5

a.

e.

what glutamate receptors are ionotropic? (SATA)

a. NMDA

b. AMPA

c. Kainate

d. mGluR1-8

a.

b.

c.

what glutamate receptors are metabotropic? (SATA)

a. NMDA

b. AMPA

c. Kainate

d. mGluR1-8

d.

what metabotropic glutamate receptor is inhibitory?

a. mGluR1

b. mGluR2

b.

what metabotropic glutamate receptor is excitatory?

a. mGluR1

b. mGluR2

a.

P2X receptors are activated by ATP, they are ________ and activate __________

a. excitatory, activate inward chloride channels

b. inhibitory, inhibit inward sodium channels

c. excitatory, activate inward sodium channels

d. inhibitory, inhibit inward chloride channels

c.

what histamine receptor is excitatory and increases IP3 and DAG?

a. H1

b. H2

c. H3

d. H4

a.

what histamine receptor is excitatory and increases cAMP?

a. H1

b. H2

c. H3

d. H4

b.

what histamine receptors are inhibitory and decreases cAMP? (SATA)

a. H1

b. H2

c. H3

d. H4

c.

d.