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PHCY 503- MOFO EXAM LATEST UPDATE
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PHCY 503- MOFO EXAM LATESTUPDATE
Potency
Efficacy - Answer Potency- dose range which produces a response
Efficacy- strength of response
Emax - Answer maximum response an agonist can cause in tissue
- measure of efficacy
Competitive inhibitors
Non-competitive inhibitors - Answer Competitive: reversible; shifts dose-response curve
right (no effect on Vmax, increase Km)
Non-competitive: irreversible; shifts dose-response curve down and right (no effect on
Km, decrease Vmax)
General features of hydrolase inhibitors - Answer 1) serine residue as Nu-
2) Tetrahedral intermediate (TS mimickery)
3) Binding pockets in substrate (PDE inhibitors)
Neuraminidase - Answer glycosidase that allows the budding of virion to escape cell +
infect new ones
Neuraminidase inhibitors
- structure
- examples - Answer Planar at C1; partial positive
- Zanamivir (polar)- inhaled, more potent
- Oseltamivir (non-polar)- ingested, less potent
PDE enzymes - Answer cleave cAMP to AMP and cGMP to GMP
- serve as molecular "off switches" (active in cyclic form)
PDE inhibitors
- effect(s) - Answer prevent hydrolysis of cAMP, cGMP
, - cAMP = inhibition of aggregation
- cGMP = vasodilation = erection
- Structure: mimics binding pockets in nucleobase purine (substrate)
Sildenaphil - Answer PDE5 inhibitor
- increases cGMP via inhibition of hydrolysis
- response: vasodilation + sustained erection
Why might a PDE inhibitor not have any effect? - Answer There needs to be a stimulus
for the cGMP/cAMP pathway; if not, then there is none present to begin with
Other PDE inhibitors - Answer -afils
Sildenafil
Vardenafil
Tadalafil
Effects of increasing:
cAMP
cGMP - Answer - increasing cAMP: decreases THX-2 / platelet aggregation
- increasing cGMP: vasodilation
PGH2 - Answer Prostaglandin- pain, fever, swelling (inflammation)
Prostaglandin biosynthesis - Answer 1) PLA-2 hydrolyzes membranes, releasing
arachidonic acid
2) COX converts aracidonic acid to PGH2
*place in body dictates function
COXI
- types
- mechanism
- effects - Answer COX inhibitors; prevent conversion of arachidonic acid to PGH2
- NSAIDS, aspirin, acetaminophen
Purposes
1) anti-inflammation (NSAIDS only)
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