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I need some assistance with these assignment. modern concept of mechanism of pharma dynamic action ace inhibitor Thank you in advance for the help!
I need some assistance with these assignment. modern concept of mechanism of pharma dynamic action ace inhibitor Thank you in advance for the help! ii) Dicarboxylate-containing inhibitors. these have the largest number of inhibitors which include enalapril, ramipril, quinapril, Perindopril, lisinopril, benazepril, imidapril, trandolapril, and cilazapril.
The enzyme in question is a zinc-containing enzyme which substitutes dipeptide units from the peptide substrate and is usually the one responsible for converting the decapeptide prohormone angiotensin I to angiotensin II. This enzyme belongs to the class of zinc proteases which require zinc and chloride to be activated and results in an increase in blood pressure through this conversion and by degrading bradykinin (Thomson 24).
These drugs have been discovered to cause a relaxation in blood vessels and a reduction in blood volume which normally leads to lower blood pressure and a decrease in oxygen demand by the heart. They often react to inhibit the angiotensin-converting enzyme. Angiotensin is an important component of the rennin-angiotensin aldosterone system.
The initial stage of the development of these drugs was the discovery of an angiotensin-converting enzyme in plasma by a scientist Leonard T. Skeggs in 1956. Then in 1965, a scientist by the name, Sergio Henrique Ferreira discovered a bradykinin-potentiating factor (BPF) existing in the venom of Bothrops jararaca, a pit viper in South America. He reported that the viper’s venom had in it factors that potentiated the activity of bradykinin. With the isolated BPF, he then went to JohnVane’s laboratory to conduct further researches. During this period, there was a general belief that the conversion of the inactive angiotensin I in the human system to the active angiotensin II took place in the plasma. However, it was later shown by Kevin K. F. and John R. Vane in 1967, that this conversion in the plasma was too slow to account for the conversion of the angiotensin I to angiotensin II in the human .system. Further revelations indicated that the rapid conversion occurred through the passage of the angiotensin I through the pulmonary circulation.
Both bradykinin and angiotensin disappear in the pulmonary circulation. Bradykinin, in particular, is inactivated and completely disappears in a solo pass through the pulmonary circulation. Angiotensin I also disappears as it is converted to angiotensin II, which passes through the lungs without a loss. In 1970, using the BPF brought by Ferreira, the original thought that the inactivation of the bradykinin and the subsequent conversion of the Angiotensin I was dissipated. It was shown that this conversion was inhibited as it passed through the pulmonary circulation using the BPF by Vane and Ng. BPF became the lead compound for the further developments of new antihypertensive agents. It represented a member of the peptides family, and its potent action was linked to the inhibition of bradykinin by ACE. .
