|
PDE5
Cyclic guanosine monophosphate-specific phosphodiesterase type 5 is an enzyme () from the phosphodiesterase class. It is found in various tissues, most prominently the corpus cavernosum and the retina. It has also been recently discovered to play a vital role in the cardiovascular system. The phosphodiesterase (PDE) isozymes, found in several tissues including the rod and cone photoreceptor cells of the retina, belong to a large family of cyclic nucleotide PDEs that catalyze cAMP and cGMP hydrolysis. The interest in PDEs as molecular targets of drug action has grown with the development of isozyme-selective PDE inhibitors that offer potent inhibition of selected isozymes without the side-effects attributed to nonselective inhibitors such as theophylline. Sildenafil, vardenafil, tadalafil, and avanafil are PDE5 inhibitors that are significantly more potent and selective than zaprinast and other early PDE5 inhibitors. Action of PDE5 PDE5 is an enzyme that accepts cGMP and b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tadalafil
Tadalafil, sold under the brand name Cialis among others, is a medication used to treat erectile dysfunction (ED), benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension. It is taken by mouth. Onset is typically within half an hour and the duration is up to 36 hours. Common side effects include headache, muscle pain, flushed skin, and nausea. Caution is advised in those with cardiovascular disease. Rare but serious side effects include a prolonged erection that can lead to damage to the penis, vision problems, and hearing loss. Tadalafil is not recommended in people taking nitrovasodilators such as nitroglycerin, as this may result in a serious drop in blood pressure. Tadalafil is a PDE5 inhibitor which increases blood flow to the penis. It also dilates blood vessels in the lungs, which lowers the pulmonary artery pressure. Tadalafil was approved for medical use in the United States in 2003. It is available as a generic medication. In 2020, it was the 261s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sildenafil
Sildenafil, sold under the brand name Viagra, among others, is a medication used to treat erectile dysfunction and pulmonary arterial hypertension. It is unclear if it is effective for treating sexual dysfunction in women. It is taken by mouth or by injection into a vein. Onset is typically within twenty minutes and lasts for about two hours. Common side effects include headaches, heartburn, and flushed skin. Caution is advised in those with cardiovascular disease. Rare but serious side effects include a prolonged erection (priapism) that can lead to damage to the penis, vision problems, and hearing loss. Sildenafil should not be taken by people on nitrates such as nitroglycerin (glycerin trinitrate), as this may result in a serious drop in blood pressure. Sildenafil should not be taken within four hours of taking an alpha blocker. Sildenafil acts by blocking phosphodiesterase 5 (PDE5), an enzyme that promotes breakdown of cGMP, which regulates blood flow in the pe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sildenafil
Sildenafil, sold under the brand name Viagra, among others, is a medication used to treat erectile dysfunction and pulmonary arterial hypertension. It is unclear if it is effective for treating sexual dysfunction in women. It is taken by mouth or by injection into a vein. Onset is typically within twenty minutes and lasts for about two hours. Common side effects include headaches, heartburn, and flushed skin. Caution is advised in those with cardiovascular disease. Rare but serious side effects include a prolonged erection (priapism) that can lead to damage to the penis, vision problems, and hearing loss. Sildenafil should not be taken by people on nitrates such as nitroglycerin (glycerin trinitrate), as this may result in a serious drop in blood pressure. Sildenafil should not be taken within four hours of taking an alpha blocker. Sildenafil acts by blocking phosphodiesterase 5 (PDE5), an enzyme that promotes breakdown of cGMP, which regulates blood flow in the pe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ICOS
Icos Corporation (trademark ICOS) was an American biotechnology company and the largest biotechnology company in the U.S. state of Washington, before it was sold to Eli Lilly and Company in 2007. It was founded in 1989 by David Blech, Isaac Blech, Robert Nowinski, and George Rathmann, a pioneer in the industry and chief executive officer (CEO) and co-founder of Amgen, Icos focused on the development of drugs to treat inflammatory disorders. During its 17-year history, the company conducted clinical trials of twelve drugs, three of which reached the last phase of clinical trials. Icos also manufactured antibodies for other biotechnology companies. Icos is famous for tadalafil (Cialis), a drug used to treat erectile dysfunction. This drug was discovered by GlaxoSmithKline, developed by Icos, and manufactured and marketed in partnership with Eli Lilly. Boosted by a unique advertising campaign led by the Grey Worldwide Agency, sales from Cialis allowed Icos to become profitable i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vardenafil
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction that is sold under the brand name Levitra among others. Medical use Vardenafil's indications and contraindications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. Vardenafil's relatively short effective time is comparable to but somewhat longer than sildenafil's. Vardenafil also does not have an effect on PDE6, which means that it does not have vision adverse effects. Beyond its indications for erectile dysfunction, vardenafil may be effective in the treatment of premature ejaculation, where it may significantly increase the time from penetration to ejaculation. Adverse react ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Avanafil
Avanafil is a PDE5 inhibitor approved for erectile dysfunction by the FDA on April 27, 2012 and by EMA on June 21, 2013. Avanafil is sold under the brand names Stendra and Spedra. It was invented at Mitsubishi Tanabe Pharma, formerly known as Tanabe Seiyaku Co., and licensed to Vivus Inc., which partnered with Menarini Group to commercialise Spedra in over forty European countries, Australia, and New Zealand. Metuchen Pharmaceuticals obtained exclusive rights within the United States. Avanafil acts by inhibiting a specific phosphodiesterase type 5 enzyme found in various body tissues, primarily in the corpus cavernosum penis. Other similar drugs are sildenafil, tadalafil and vardenafil. The advantage of avanafil is that it has very fast onset of action compared with other PDE5 inhibitors. It is absorbed quickly, reaching a maximum serum concentration in about thirty to forty-five minutes. About two-thirds of the participants were able to engage in sexual activity within fifteen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaprinast
Zaprinast was an unsuccessful clinical drug candidate that was a precursor to the chemically related PDE5 inhibitors, such as sildenafil (Viagra), which successfully reached the market. It is a phosphodiesterase inhibitor, selective for the subtypes PDE5, PDE6, PDE9 and PDE11. IC50 values are 0.76, 0.15, 29.0, and 12.0 ''μ''M, respectively. Zaprinast inhibits the growth of asexual blood-stage malaria parasites ( ''P. falciparum'') ''in vitro'' with an ED50 value of 35 ''μ''M, and inhibits PfPDE1, a '' P. falciparum'' cGMP-specific phosphodiesterase, with an IC50 value of 3.8 ''μ''M. Zaprinast has also been shown to activate the orphan G-protein coupled receptor known as GPR35, both in rats and humans, and to inhibit the mitochondrial pyruvate Pyruvic acid (CH3COCOOH) is the simplest of the alpha-keto acids, with a carboxylic acid and a ketone functional group. Pyruvate, the conjugate base, CH3COCOO−, is an intermediate in several metabolic pathways throughout the cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phosphodiesterase
A phosphodiesterase (PDE) is an enzyme that breaks a phosphodiester bond. Usually, ''phosphodiesterase'' refers to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases (which all break the phosphodiester backbone of DNA or RNA), as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators of signal transduction mediated by these second messenger molecules. History These multiple forms (isoforms or subtypes) of phosphodies ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclic Guanosine Monophosphate
Cyclic guanosine monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate (GTP). cGMP acts as a second messenger much like cyclic AMP. Its most likely mechanism of action is activation of intracellular protein kinases in response to the binding of membrane-impermeable peptide hormones to the external cell surface. Synthesis Guanylate cyclase (GC) catalyzes cGMP synthesis. This enzyme converts GTP to cGMP. Peptide hormones such as the atrial natriuretic factor activate membrane-bound GC, while soluble GC (sGC) is typically activated by nitric oxide to stimulate cGMP synthesis. sGC can be inhibited by ODQ (1H-,2,4xadiazolo ,3-auinoxalin-1-one). Functions cGMP is a common regulator of ion channel conductance, glycogenolysis, and cellular apoptosis. It also relaxes smooth muscle tissues. In blood vessels, relaxation of vascular smooth muscles leads to vasodilation and increased blood flow. At presynaptic terminals in the striatum, cGMP controls the e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bayer
Bayer AG (, commonly pronounced ; ) is a German multinational corporation, multinational pharmaceutical and biotechnology company and one of the largest pharmaceutical companies in the world. Headquartered in Leverkusen, Bayer's areas of business include pharmaceuticals; consumer healthcare products, agricultural chemicals, seeds and biotechnology products. The company is a component of the Euro Stoxx 50 stock market index. Bayer was founded in 1863 in Barmen as a partnership between dye salesman Friedrich Bayer and dyer Friedrich Weskott. As was common in this era, the company was established as a dyestuffs producer. The versatility of aniline chemistry led Bayer to expand their business into other areas, and in 1899 Bayer launched the compound acetylsalicylic acid under the trademarked name Aspirin. In 1904 Bayer received a trademark for the "Bayer Cross" logo, which was subsequently stamped onto each aspirin tablet, creating an iconic product that is still sold by Bayer. Ot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GlaxoSmithKline
GSK plc, formerly GlaxoSmithKline plc, is a British multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a merger of Glaxo Wellcome and SmithKline Beecham. GSK is the tenth largest pharmaceutical company and #294 on the 2022 ''Fortune'' Global 500, ranked behind other pharmaceutical companies China Resources, Sinopharm, Johnson & Johnson, Pfizer, Roche, AbbVie, Novartis, Bayer, and Merck. The company has a primary listing on the London Stock Exchange and is a constituent of the FTSE 100 Index. , it had a market capitalisation of £70 billion, the eighth largest on the London Stock Exchange. It has a secondary listing on the New York Stock Exchange. The company developed the first malaria vaccine, RTS,S, which it said in 2014 it would make available for five percent above cost. Legacy products developed at GSK include several listed in the World Health Organization's List of Essential Medicines, such ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Schering Plough
Schering-Plough Corporation was an American pharmaceutical company. It was originally the U.S. subsidiary of the German company Schering AG, which was founded in 1851 by Ernst Christian Friedrich Schering. As a result of nationalization, it became an independent company. In 1971, the Schering Corporation merged with Plough (founded by Memphis area entrepreneur Abe Plough in 1908)"Abe Plough (1892-1984) ," ''Tennessee Encyclopedia of History and Culture,'' online. to form Schering-Plough. On November 4, 2009 Merck & Co. merged with Schering-Plough with the new company taking the name of Merck & Co. Schering-Plough manufactured several pharmaceutical Medication, drugs, the most well-known of which were the allergy drugs Claritin and Clarinex, an anti-cholesterol drug Vytorin, and a brain tumor drug Temodar. These are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
