Perindopril
From Proteopedia
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| - | < | + | <StructureSection load='' size='340' side='right' caption='Perindoprilat, the metabolite of Perindopril, also known as Aceon' scene='Perindopril/Perindoprilat/2'> |
===Better Known as: Aceon=== | ===Better Known as: Aceon=== | ||
* Marketed By: Abbott Labs & Servier<br /> | * Marketed By: Abbott Labs & Servier<br /> | ||
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===Mechanism of Action=== | ===Mechanism of Action=== | ||
Angiotensin II has been implicated in cardiac, renal and vascular diseases. Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for [[Hypertension]].<ref>PMID:17083068</ref> Perindopril is rapidly metabolized into its highly active metabolite Perindoprilat by hepatic enzymes. Perindoprilat binds to the active site of <scene name='Perindopril/Perindoprilat_ace/1'>Angiotensin-Converting Enzyme</scene>, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 <scene name='Perindopril/Perindoprilat_binding/1'>binds Perindoprilat</scene> using residues Gln 265, Lys 495, Tyr 504, His 497, His 337, Tyr 496, Ala 338, Glu 368, His 367, HIs 371, Glu 395 and Asp 399 to tightly affix the inhibitor to the active site of ACE-1. | Angiotensin II has been implicated in cardiac, renal and vascular diseases. Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for [[Hypertension]].<ref>PMID:17083068</ref> Perindopril is rapidly metabolized into its highly active metabolite Perindoprilat by hepatic enzymes. Perindoprilat binds to the active site of <scene name='Perindopril/Perindoprilat_ace/1'>Angiotensin-Converting Enzyme</scene>, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1 <scene name='Perindopril/Perindoprilat_binding/1'>binds Perindoprilat</scene> using residues Gln 265, Lys 495, Tyr 504, His 497, His 337, Tyr 496, Ala 338, Glu 368, His 367, HIs 371, Glu 395 and Asp 399 to tightly affix the inhibitor to the active site of ACE-1. | ||
| - | + | </StructureSection> | |
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | ||
Current revision
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Pharmacokinetics
For Pharmacokinetic Data References, See: References |
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References
- ↑ Ferrario CM. Role of angiotensin II in cardiovascular disease therapeutic implications of more than a century of research. J Renin Angiotensin Aldosterone Syst. 2006 Mar;7(1):3-14. PMID:17083068
