Eicosanoids Flashcards
PROSTAGLANDINS
-C____ fatty acids are the precursors for prostaglandins
20
prostaglandins were thought to originate in the ____
prostate
in mid 50s it was isolated from body fluids In ether extract (PGE)
T/F
T
Eicosanoids are Made by all cells except _____
RBC
EICOSANOIDS
-are ___ hormones , ___ated from _____ acid
local
oxygen
arachidonic
Arachidonic acid is a 20C with ______ bonds
4 double
prostaglandin ___ is the most potent ___genous ______ substance (sleep wake cycle)
D2
Endo
sleep-promoting
Eicosanoids have profound physiological effects at very ____ concentration
low
Eicosanoids are hormone-like
T/F
T
Eicosanoids are paracrine
T/F
T
Eicosanoids bind to ______ receptors and affect _____
G-coupled
cAMP
ASPIRIN
- aspirin inhibits ____
- ___mg% of aspirin daily is usually prescribed for hypertensive patient
Eicosanoids
75
FUNCTIONS Eicosanoids mediate: -\_\_\_\_\_\_\_\_ -production of \_\_\_ and \_\_\_\_ -regulate blood \_\_\_\_ -induction of blood \_\_\_ -\_\_\_\_\_ functions -\_\_\_\_\_\_ cycle -egress of \_\_\_\_\_\_\_
inflammation
pain and fever
pressure
clotting
reproductive
sleep/wake
T lymphocytes
arachidonic acid is synthesized from the essential ____ acid (C__:—), 692, by _____ and _____
linoleic
18:2
elongation and desaturation
arachidonic acid is phospholipid bound(___,__)
Sn2,PI
Arachidonic acid is released upon stimuli by :
1) phospholipase ___
2) phospholipase ___
3) ______ by DAG ____
A2
C
DAG hydrolysis
lipase
phospholipase C breaks down phosphatidylinositol into ______ and ____ leaves as a by product
DAG
Phosphoinositol
corticosteroids (directly or indirectly?) inhibit PH signaling
Indirectly
DAG is converted to ____ acid by ______
Phosphatidic
P+ins -> PA(DAG kinase ) -> AA(PLA2)
Phosphatidic acid is converted to _____ acid and _____ acid by _____
lysophosphatidic
arachidonic
phospholipase A2
THE REACTIONS CATALYZED BY PGH SYNTHASE
- PGHS catalyzes ___ step in __ pathway
- ________+________ activity
- heme activates _____
- target of ____
- _____ membrane protein
first; cyclic
cyclooxygenase (COX) + peroxidase
tyr radical
aspirin
monotopic
ASPIRIN
- aka _____ acid
- (inhibits or aids ?) cyclooxygenase activity of PGHS
- acetylates ___ ——
acetylsalicylic
inhibits
Ser 530
flubriprofen ____ aspirin channel and acetylates ___ protein
blocks
Ser
low dose of aspirin (reduces or increases?) heart attack risk, (inhibits or stimulates?) platelet aggregation by causing enucleated cells, __ days lifetime ,(can or cannot?) resynthesize enzyme
reduces
inhibits
10
Cannot
Some NSAIDs
- ____
- _____
- ____
- ____
- _____
- ______
aspirin
acetaminophen
indomethacin
naproxen
phenylbutazobone
flubriprofen
VIOXX
-2 PHGS isoforms (____,____)
COX1,COX 2
ASPIRIN can’t induce GIT ulceration
T/F
F
It can
ESKIMOS
- ____ results of CVS disease despite the fat that they eat a lot of ___
- they are healthy because they eat —-
- reduce cholesterol , leukotriene and PG levels
Low
fat
fish
Effect of cortisol on eicosanoids
Inhibits it
Eicosanoids regulate blood ______ and induct blood ___
Pressure
Clotting
Eicosanoids mediate production of ____ and ____
Pain and fever
Eicosanoids has no reproductive function
T/F
F
Eicosanoids play no role in the sleep wake cycle
T/F
F
Eicosanoids causes egress of T lymphocytes
T/F
T
The prostaglandin parent compound is the _____
Prostanoic acid
First 3 prostaglandins to be identified
E1
E2
F2a
Aspirin inhibits ____ enzyme
PGH synthase
COX 1 is constitutively expressed in ___ tissue include the _____
-COX2 is only seen in ____ tissues and expressed in response to ____
most; GIT mucosa
certain; thyroid
COX__ is expressed in response to inflammatory stimuli
2
COX __ is the target for acetaminophen
3
2 examples of COX2 inhibitors
Vioxx (Rofecoxib)
Celecoxib (Celebrex)
Prostaglandin ___ is the most potent endogenous sleep promoting substance
D2
For arachidonic acid to be converted to prostaglandin, it needs to undergo _____
Cyclization
