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14-September-2008 18:02:40 - Phosphodiesterase inhibitor A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase PDE, therefore preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate cAMP and cyclic guanosine monophosphate cGMP, by the respective PDE subtypes. Contents 1 History 2 Classification 2.1 Non-selective phosphodiesterase inhibitors 2.2 PDE1 selective inhibitors 2.3 PDE2 selective inhibitors 2.4 PDE3 selective inhibitors 2.5 PDE4 selective inhibitors 2.6 PDE5 selective inhibitors 3 References History The different forms or subtypes of phosphodiesterase were initially isolated from rat brains by Uzunov and Weiss in 19721 and were soon afterwards shown to be selectively inhibited in the brain and in other tissues by a variety of drugs.23 The potential for selective phosphodisterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait.4 This prediction meanwhile has proved to be true in a variety of fields. Classification Non-selective phosphodiesterase inhibitors caffeine, a minor stimulant theophylline, a bronchodilator IBMX 3-isobutyl-1-methylxanthine, used as investigative tool in pharmacological research PDE1 selective inhibitors Vinpocetine PDE2 selective inhibitors EHNA erythro-9-2-hydroxy-3-nonyladenine PDE3 selective inhibitors Main article: PDE3 inhibitor Enoximone and milrinone, used clinically for short-term treatment of cardiac failure. These drugs mimic sympathetic stimulation and increase cardiac output. PDE3 is sometimes referred to as cGMP-inhibited phosphodiesterase. PDE4 selective inhibitors Mesembrine, an alkaloid from the herb Sceletium tortuosum Rolipram, used as investigative tool in pharmacological research Ibudilast, a neuroprotective and bronchodilator drug used mainly in the treatment of asthma and stroke. It inhibits PDE4 to the greatest extent, but also shows significant inhibition of other PDE subtypes, and so acts as a selective PDE4 inhibitor or a non-selective phosphodiesterase inhibitor depending on the dose. PDE4 is the major cAMP-metabolizing enzyme found in inflammatory and immune cells. PDE4 inhibitors have proven potential as anti-inflammatory drugs, especially in inflammatory pulmonary diseases such as asthma, COPD and rhinitis. They suppress the release of cytokines and other inflammatory signals and inhibit the production of reactive oxygen species. PDE4 inhibitors may have antidepressive effects5 and have also recently been proposed for use as antipsychotics.67 PDE5 selective inhibitors Main article: PDE5 inhibitor Sildenafil, tadalafil and vardenafil, and the newer udenafil and avanafil selectively inhibit PDE5, which is cGMP-specific and responsible for the degradation of cGMP in the corpus cavernosum. These phosphodiesterase inhibitors are used primarily as remedies for erectile dysfunction, as well as having some other medical applications such as treatment of pulmonary hypertension. Dipyridamole also inhibits PDE5. This results in added benefit when given together with NO or statins. References ^ Uzunov, P. and Weiss, B.: Separation of multiple molecular forms of cyclic adenosine 3',5'-monophosphate phosphodiesterase in rat cerebellum by polyacrylamide gel electrophoresis. Biochim. Biophys. Acta 284:220-226, 1972. ^ Weiss, B.: Differential activation and inhibition of the multiple forms of cyclic nucleotide phosphodiesterase. Adv. Cycl. Nucl. Res. 5:195-211, 1975. ^ Fertel, R. and Weiss, B.: Properties and drug responsiveness of cyclic nucleotide phosphodiesterases of rat lung. Mol. Pharmacol. 12:678-687, 1976. ^ Weiss, B. and Hait, W.N.: Selective cyclic nucleotide phosphodiesterase inhibitors as potential therapeutic agents. Ann. Rev. Pharmacol. Toxicol. 17:441-477, 1977. ^ Bobon D, Breulet M, Gerard-Vandenhove MA, Guiot-Goffioul F, Plomteux G, Sastre-y-Hernandez M, Schratzer M, Troisfontaines B, von Frenckell R, Wachtel H. 1988. Is phosphodiesterase inhibition a new mechanism of antidepressant action? A double blind double-dummy study between rolipram and desipramine in hospitalized major and/or endogenous depressives.. Eur Arch Psychiatry Neurol Sci. 238 1: 2-6. PMID 3063534. ^ Maxwell CR, Kanes SJ, Abel T, Siegel SJ. 2004. Phosphodiesterase inhibitors: a novel mechanism for receptor-independent antipsychotic medications.. Neuroscience. 129 1: 101-7. doi:10.1016/j.neuroscience.2004.07.038. PMID 15489033. ^ Kanes SJ, Tokarczyk J, Siegel SJ, Bilker W, Abel T, Kelly MP. 2006. Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity.. Neuroscience. ? ?: ?. PMID 17081698. v d e Selective Phosphodiesterase inhibitors C01CE, G04BE PDE1 Vinpocetine PDE2 EHNA PDE3 Amrinone Bucladesine Enoximone Milrinone RPL-554 PDE4 Cilomilast Drotaverine Etazolate Glaucine HT-0712 Ibudilast Mesembrine Roflumilast Rolipram RPL-554 PDE5 Acetildenafil Avanafil Sildenafil Tadalafil Thiomethisosildenafil Udenafil Vardenafil v d e Cardiac stimulants excluding cardiac glycosides C01C Adrenergic and dopaminergic agents Adrenergic agonists primarily β1 and mixed EPINEPHRINE Etilefrine Isoprenaline Norepinephrine Norfenefrine Phenylephrine Dobutamine Oxedrine Metaraminol Methoxamine Mephentermine Prenalterol Midodrine Arbutamine Dopamine agonists DOPAMINE Fenoldopam Both Dopexamine Ibopamine Octopamine Unknown/ungrouped Dimetofrine Gepefrine Cafedrine Theodrenaline Phosphodiesterase inhibitors PDE3I Amrinone Milrinone Enoximone Bucladesine Other cardiac stimulants Angiotensinamide Xamoterol Levosimendan v d e Pharmacology: enzyme inhibition Class Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition Substrate Oxidoreductase EC 1: Aromatase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors - COX-2 inhibitor Transferase EC 2: Integrase inhibitor - Protein kinase inhibitors - Reverse transcriptase inhibitors - COMT inhibitors Hydrolase EC 3: Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors ACE inhibitor, Trypsin inhibitor - Histone deacetylase inhibitor Lyase EC 4: Carbonic anhydrase inhibitors Retrieved from http://en..org/wiki/Phosphodiesterase_inhibitor Categories: Phosphodiesterase inhibitors Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Français 日本語 中文 This page was last modified on 11 September 2008, at 17:37
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