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Bradykinin Potentiating Factor
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 been investigated as an antihypertension agent. __TOC__ 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. Teprotide was shown to be an effective an ... [...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 Old Tupi '' îararaka''. 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 sublabials (usually 10–12 ... [...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 high blood pressure and heart failure. This class of medicine works 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 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 explain t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradykinin
Bradykinin (BK) (from 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 consists of nine amino acids, and is a physiologically and pharmacologically active peptide of the kinin group of proteins. 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 Translation (genetics), peptide chain. The amino acid sequence of bradykinin is: arginine, Arg-pr ... [...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. Captopril was patented in 1976 and approved for medical use in 1980. Structure–activity relationship Captopril has an L-proline group which allows it to be more bioavailable in oral formulations. The thiol moiety within the molecule has been associated with two significant 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 includes hives, severe stomach pain, difficulty breathing, and swelling of the face, lips, tongue or throat. In terms of interaction with the enzyme, the molec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
