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Endopeptidase Inhibitor
An endopeptidase inhibitor is a drug that inhibits one or more endopeptidase enzymes. Endopeptidases are one of two types of proteases (enzymes that break down proteins and peptides), the other being exopeptidases. Endopeptidases cleave peptide bonds of non-terminal amino acids (that is, they cut proteins/peptides into two chains), whereas exopeptidases break terminal bonds, resulting in the release of a single amino acid or dipeptide from the peptide chain. Examples of endopeptidase inhibitors Some examples of endopeptidase inhibitors include the following: * Neprilysin inhibitors ** Selective neprilysin inhibitors *** Candoxatril - prodrug to candoxatrilat *** Candoxatrilat - active metabolite of candoxatril *** Dexecadotril (retorphan) - (''R'')-enantiomer of racecadotril; prodrug to (''R'')-thiorphan *** Ecadotril (sinorphan) - (''S'')-enantiomer of racecadotril; prodrug to (''S'')-thiorphan *** Racecadotril (acetorphan) - racemic form of dexecadotril and ecadotril; prodr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Reve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Angiotensin Converting Enzyme
Angiotensin-converting enzyme (), or ACE, is a central component of the renin–angiotensin system (RAS), which controls blood pressure by regulating the volume of fluids in the body. It converts the hormone angiotensin I to the active vasoconstrictor angiotensin II. Therefore, ACE indirectly increases blood pressure by causing blood vessels to constrict. ACE inhibitors are widely used as pharmaceutical drugs for treatment of cardiovascular diseases. Other lesser known functions of ACE are degradation of bradykinin, substance P and amyloid beta-protein. Nomenclature ACE is also known by the following names: * dipeptidyl carboxypeptidase I * peptidase P * dipeptide hydrolase * peptidyl dipeptidase * angiotensin converting enzyme * kininase II * angiotensin I-converting enzyme * carboxycathepsin * dipeptidyl carboxypeptidase * "hypertensin converting enzyme" peptidyl dipeptidase I * peptidyl-dipeptide hydrolase * peptidyldipeptide hydrolase * endothelial cell peptidyl dipeptidas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
UK-414,495
UK-414,495 is a drug developed by Pfizer for the treatment of female sexual arousal disorder. UK-414,495 acts as a potent, selective inhibitor of the enzyme neutral endopeptidase, which normally serves to break down the neuropeptide VIP. The consequent increase in VIP activity alters blood flow to the genital region leading to increased lubrication and muscle relaxation. See also * ABT-670 * ABT-724 * Bremelanotide * Cabergoline * Flibanserin * Testosterone (patch) * Melanotan II * Pramipexole * PF-219,061 * S-17092 * Tibolone Tibolone, sold under the brand name Livial among others, is a medication which is used in menopausal hormone therapy and in the treatment of postmenopausal osteoporosis and endometriosis. The medication is available alone and is not formulated ... References Hydrolase inhibitors Female sexual dysfunction drugs Thiadiazoles Carboxamides Carboxylic acids Aphrodisiacs Cyclopentanes Pfizer brands {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thiorphan
Thiorphan is the active metabolite of the antidiarrheal racecadotril (acetorphan). It prevents the degradation of endogenous enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephali ...s by acting as an enkephalinase inhibitor. References Enkephalinase inhibitors Antidiarrhoeals Amino acid derivatives Thiols Carboxamides Propionamides {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitrilat
Sacubitrilat (INN; or LBQ657) is the active metabolite of the antihypertensive drug sacubitril, which is used in the treatment of heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, a .... References Antihypertensive agents Biphenyls Carboxylic acids Amides {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitrilat
Sacubitrilat (INN; or LBQ657) is the active metabolite of the antihypertensive drug sacubitril, which is used in the treatment of heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, a .... References Antihypertensive agents Biphenyls Carboxylic acids Amides {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sacubitril
Sacubitril (; INN) is an antihypertensive drug used in combination with valsartan. The combination drug sacubitril/valsartan, known during trials as ''LCZ696'' and marketed under the brand name ''Entresto'', is a treatment for heart failure. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Side effects Sacubitril increases levels of bradykinin, which is responsible for the edema seen sometimes in patients with the medication. This is why the medication is not recommended for patients with a history of pulmonary edema with the usage of ACE inhibitors. Mechanism of action Sacubitril is a prodrug that is activated to sacubitrilat (LBQ657) by de- ethylation via esterases. Sacubitrilat inhibits the enzyme neprilysin, which is responsible for the degradation of atrial and brain natriuretic peptide, two blood pressure–lowering peptides that work mainly by reducing blood volume. In addition, neprilysin degrades a variety of peptides i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thiorphan
Thiorphan is the active metabolite of the antidiarrheal racecadotril (acetorphan). It prevents the degradation of endogenous enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephali ...s by acting as an enkephalinase inhibitor. References Enkephalinase inhibitors Antidiarrhoeals Amino acid derivatives Thiols Carboxamides Propionamides {{gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Racecadotril
Racecadotril, also known as acetorphan, is an antidiarrheal medication which acts as a peripheral enkephalinase inhibitor. Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect — it reduces the secretion of water and electrolytes into the intestine. It is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the United Kingdom, Spain, Portugal, Poland, Finland, Russia and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States. It is sold under the tradename Hidrasec, among others. Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinases. Medical uses Racecadotril is used for the treatment of acute diarrhea in children and adults and has better tolerability than loperamide, as i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
