| 词条 | Homosildenafil |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 5-[2-Ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[4,3-d]pyrimidin-7-one | image = Homosildenafil.svg | width = 250 | tradename = | Drugs.com = | MedlinePlus = | licence_EU = | licence_US = | pregnancy_US = | legal_status = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 642928-07-2 | ATC_prefix = None | ATC_suffix = | ChEBI_Ref = | ChEBI = | PubChem = 24756844 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 0Z3JH0S0QK | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 22547032 | C=23 | H=32 | N=6 | O=4 | S=1 | molecular_weight = 488.6 g/mol | smiles = CCCC1=NN(C)C2=C1N=C(NC2=O)C1=CC(=CC=C1OCC)S(=O)(=O)N1CCN(CC)CC1 | StdInChI_Ref = | StdInChI = 1S/C23H32N6O4S/c1-5-8-18-20-21(27(4)26-18)23(30)25-22(24-20)17-15-16(9-10-19(17)33-7-3)34(31,32)29-13-11-28(6-2)12-14-29/h9-10,15H,5-8,11-14H2,1-4H3,(H,24,25,30) | StdInChIKey_Ref = | StdInChIKey = MJEXYQIZUOHDGY-UHFFFAOYSA-N }}Homosildenafil (also known as methyl-sildenafil) is a synthetic drug which acts as a phosphodiesterase inhibitor.[1] It is an analog of sildenafil and vardenafil. Homosildenafil was first identified as an adulterant in sex enhancement products in 2003 and was more recently detected in dietary supplements.[2][3][4][5] Homosildenafil has 35% the PDE5 inhibition activity of sildenafil itself with similar selectivity.[1] Sildenafil is mainly metabolized by the microsomal isozymes CYP3A4 with secondary metabolism by CYP2C9. The major active metabolite is N-desmethylsildenafil. The plasma level of the equivalent homosildenafil metabolite reaches 40% of sildenafil's bioavailability. The N-desmethyl metabolite is further metabolized, with a half-life of 4 hours.[6][7][8][9] See also
References1. ^1 {{cite journal | title=Vardenafil: structural basis for higher potency over sildenafil in inhibiting cGMP-specific phosphodiesterase-5 (PDE5) |author1=Jackie D Corbin |author2=Alfreda Beasley |author3=Mitsi A Blount |author4=Sharron H Francis | journal=Neurochemistry International |date=November 2004 | volume=45 | issue=6 | pages=859–863 | doi=10.1016/j.neuint.2004.03.016 | pmid=15312980}} {{Sexual dysfunction pharmacotherapies}}{{Phosphodiesterase inhibitors}}2. ^{{cite journal | title=Identification of a new analogue of sildenafil added illegally to a functional food marketed for penile erectile dysfunction |author1=M.H. Shin |author2=M.K. Hong |author3=W.S. Kim |author4=Y.J. Lee |author5=Y.C. Jeoung | journal=Food Additives & Contaminants |date=November 2003 | volume=20 | issue=9 | pages=793–796 | pmid=13129773 | doi=10.1080/0265203031000121455}} 3. ^{{cite journal | title=Detection of undeclared erectile dysfunction drugs and analogues in dietary supplements by ion mobility spectrometry |author1=Connie M. Gryniewicz |author2=John C. Reepmeyer |author3=John F. Kauffman |author4=Lucinda F. Buhse | journal=Journal of Pharmaceutical and Biomedical Analysis |date=April 2009 | volume=49 | issue=5 | pages=601–606 | doi=10.1016/j.jpba.2008.12.002 | pmid=19150190}} 4. ^{{cite web | url=http://www.prnewswire.com/news-releases/advisory---forta-for-men-sex-enhancement-product-recalled-contains-undeclared-drug-287148791.html | title=Advisory - "Forta for Men" sex enhancement product recalled; contains undeclared drug | publisher=PR Newswire | date=2014 | accessdate=28 April 2015}} 5. ^{{cite journal | title=Simultaneous determination of synthetic phosphodiesterase-5 inhibitors found in a dietary supplement and pre-mixed bulk powders for dietary supplements using high-performance liquid chromatography with diode array detection and liquid chromatography–electrospray ionization tandem mass spectrometry |author1=Peng Zoua |author2=Sharon Sze-Yin Ohb |author3=Peiling Houa |author4=Min-Yong Lowb |author5=Hwee-Ling Koh | journal=Journal of Chromatography A |date=February 2006 | volume=1104 | issue=1–2 | pages=113–122 | doi=10.1016/j.chroma.2005.11.103 | pmid=16364350}} 6. ^{{cite web | url=http://www.google.com/patents/WO2001080860A3 | title=Daily treatment for erectile dysfunction using a pde5 inhibitor | date=2002 | accessdate=27 April 2015 |author1=Tejada Inigo Saenz De |author2=Kenneth M Ferguson |author3=John S Whitaker }} 7. ^{{cite web | url=http://www.google.com/patents/US20090074796 | title=Pde5 inhibitor compositions and methods for immunotherapy | date=2009 | accessdate=27 April 2015 |author1=Ivan M. Borrello |author2=Paolo Serafini |author3=Kimberly A. Noonan |author4=Vincenzo Bronte }} 8. ^{{cite web | url=https://www.google.com/patents/US8497370 | title=Processes for preparing amine salts of sildenafil-analogues and use thereof | date=2013 | accessdate=27 April 2015 | author=Ing-Jun Chen}} 9. ^{{cite web | url=https://www.google.com/patents/CN101555512A | title=Preparation method for monoclonal antibody specifically binding vardenafil and analog thereof | date=2009 | accessdate=27 April 2015 | author=杨 许 |author2=郭杰标 |author3=黄志兵}} 2 : Designer drugs|PDE5 inhibitors |
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