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Teprotide
Teprotide is nonapeptide which has been isolated from the snake ''Bothrops jararaca''. It is an angiotensin converting enzyme inhibitor (ACE inhibitor) which inhibits the conversion of angiotensin I to angiotensin II and may potentiate some of the pharmacological actions of bradykinin. It has a molecular formula of C53H76N14O12 and has been investigated as an antihypertension agent. Isolation and synthesis The antihypertensive effects of teprotide were first observed by Sergio Ferreira in 1965 and it was first isolated by Ferreira ''et al.'' along with eight other peptides in 1970. Teprotide was synthesized in 1970 by Ondetti ''et al.'' and from there its antihypertensive properties were studied more closely. Medical use Teprotide was chosen as a lead because of its long-lasting ''in vivo'' activity. This was demonstrated by Bianchi ''et al''. by administering teprotide to dogs and rats and observing that it inhibited the vasopressor response induced by angiotensin I. Tepro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACE Inhibitor
Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of hypertension, high blood pressure and heart failure. They work by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart. ACE inhibitors Enzyme inhibitor, inhibit the activity of angiotensin-converting enzyme, an important component of the renin–angiotensin system which converts angiotensin I to angiotensin II, and hydrolyses bradykinin. Therefore, ACE inhibitors decrease the formation of angiotensin II, a vasoconstrictor, and increase the level of bradykinin, a peptide vasodilator. This combination is synergistic in lowering blood pressure. As a result of inhibiting the ACE enzyme in the bradykinin system, the ACE inhibitor drugs allow for increased levels of bradykinin which would normally be degraded. Bradykinin produces prostaglandin. This mechanism can expl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bothrops Jararaca
''Bothrops jararaca'' — known as the ''jararaca'' or ''yarara'' — is a highly venomous pit viper species endemic to South America in southern Brazil, Paraguay, and northern Argentina. The specific name, ''jararaca'', is derived from the Tupi words and , which mean "large snake". Within its geographic range, it is often abundant and is an important cause of snakebite. No subspecies are currently recognized. The drugs known as angiotensin converting enzyme (ACE) inhibitors, used for the treatment of hypertension and some types of congestive heart failure, were developed from a peptide found in the venom of this species. Description This is a slender and terrestrial species that grows to a maximum total length of 160 cm (63 in), although the average total length is much less. The head scalation includes 5-12 intersupraoculars that are weakly keeled, 7-9 supralabials (usually 8) of which the second is fused with the prelacunal to form a lacunolabial, and 9-13 sub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradykinin
Bradykinin (BK) (Greek brady-, slow; -kinin, kīn(eîn) to move) is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor and makes veins constrict, via prostaglandin F2, thereby leading to leakage into capillary beds, due to the increased pressure in the capillaries. Bradykinin is a physiologically and pharmacologically active peptide of the kinin group of proteins, consisting of nine amino acids. A class of drugs called angiotensin converting enzyme inhibitors (ACE inhibitors) increase bradykinin levels by inhibiting its degradation, thereby increasing its blood pressure lowering effect. ACE inhibitors are FDA approved for the treatment of hypertension and heart failure. Structure Bradykinin, sometimes referred to as BK, is a 9-amino acid peptide chain. The amino acid sequence of bradykinin is: Arg-Pro-Pro-Gly- Phe-Ser-Pro- Phe- Arg (RPPGFSPFR). Its empi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Captopril
Captopril, sold under the brand name Capoten among others, is an ACE inhibitor, angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first oral ACE inhibitor found for the treatment of hypertension. It does not cause fatigue as associated with beta-blockers. Due to the adverse drug event of causing hyperkalemia, as seen with most ACE Inhibitors, the medication is usually paired with a diuretic. Captopril was patented in 1976 and approved for medical use in 1980. Structure–activity relationship Captopril has an L-proline group which allows for it to be more bioavailable within oral formulations. The thiol moiety within the molecule has been associated with two significance adverse effects: the hapten or immune response. This immune response, also known as agranulocytosis, can explain the adverse drug events which may be seen in captopril with the allergic response, which would be: hi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
