Homosildenafil

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Homosildenafil
File:Homosildenafil.svg
Clinical data
ATC code
  • None
Identifiers
  • 5-[2-Ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[4,3-d]pyrimidin-7-one
CAS Number
PubChem CID
ChemSpider
UNII
E number{{#property:P628}}
CompTox Dashboard (EPA)
  • {{#property:P3117}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value).
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Chemical and physical data
FormulaC23H32N6O4S
Molar mass488.61 g·mol−1
3D model (JSmol)
  • CCCC1=NN(C)C2=C1N=C(NC2=O)C1=CC(=CC=C1OCC)S(=O)(=O)N1CCN(CC)CC1
  • InChI=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)
  • Key: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

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References

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  1. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
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  6. ^ WO 2001080860, De Tejada IS, Ferguson KM, Whitaker JS, "Daily treatment for erectile dysfunction using a pde5 inhibitor", published Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value)., assigned to Lilly ICOS LLC. 
  7. ^ US 20090074796, Borrello IM, Serafini P, Noonan KA, Bronte V, "Pde5 inhibitor compositions and methods for immunotherapy", published Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value)., assigned to ohns Hopkins University. 
  8. ^ US 8497370, Chen IJ, "Processes for preparing amine salts of sildenafil-analogues and use thereof", issued Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value)., assigned to Kaohsiung Medical University. 
  9. ^ CN 101555512, Yang X, Guo J, Huang Z, "Preparation method for monoclonal antibody specifically binding vardenafil and analog thereof", issued Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value)., assigned to Kaohsiung Medical University. 
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