Peptide Pharmacology

Terms

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ACE what kind of enzyme? where is it made/bound? what does it do?: dipeptidyl carboxypeptidase
made in EC's membrane-bound on luminal side
*can be cleaved and circulate
activates A1 -> A2 (active angiotensin)
C-term is more selective for A1
Aminopeptidase A what does it do?: cleaves A2->A3 and A3->A4 (both active metabolites)
captopril enalopril* ramipril* what do they treat? what are their s/e's?: ACE inhibitors
*enal, ram are prodrugs (turned into -prilats)
tx HTN, heart failure, MI, renal disease
s/e: cough, angioedema, hypotension, hyperkalemia
teratogenic
des-Arg9-BK des-Arg10-KD: active metabolites of BK, KD
produced by carboxypeptidase N
can bind B1 receptors in inflammation
Endothelin how made? how inactivated: preproendothelin
↓ metalloprotease
proendothelin
↓ ECE
endothelin
inactivated by Neutral endopeptidase
Kallikrein 2 types? What does each type act on and produce?: 1) Tissue
        RLS is secretion
        Converts LMWK -> Kallidin
        Kallidin can be converted to BK
2) Plasma
  &
Renin where released? what triggers its release? what does it do?: released from JG cells
released by 1) beta 1 stim (inc. cAMP)
2) baro-R (stretch->Ca->dec renin)
&nb
Aprotonin: Inhibits Plasma Kallikrein
tx post-op inflammation in CABG

Number of cards 8

Created By kmcelroy