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Drug-Target Interaction

Drug

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PubChem ID:5318997
Structure:
Synonyms:
3-((6-Deoxymannopyranosyl)oxy)-7-(glucopyranosyloxy)-5-hydroxy-2-(4-methox
3-((6-Deoxymannopyranosyl)oxy)-7-(glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-4H-1-benzopyran-4-one
489-32-7
4H-1-Benzopyran-4-one, 3-((6-deoxy-alpha-L-mannopyranosyl)oxy)-7-(beta-D-glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-
Anhydroicaritin-3-O-alpha-rhamnoside
BB_NC-0999
BSPBio_002599
CPD000466309
Icariin
KBio3_002099
KBioGR_002475
LS-185785
MLS000759413
MLS001424083
NCGC00178583-01
SAM001246560
SDCCGMLS-0066754.P001
SMR000466309
SPBio_001650
SPECTRUM1505257
Spectrum2_001695
Spectrum3_001130
Spectrum4_001975
Spectrum5_000933
ZINC03960893

Target

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Uniprot ID:PDE10_RAT
Synonyms:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
EC-Numbers:3.1.4.17
3.1.4.35
Organism:Rat
Rattus norvegicus
PDB IDs:2O8H 2OVV 2OVY 3HQW 3HQY 3HQZ 3HR1
Structure:
3HR1

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

17169663
Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells.. Hongxiu Ning; Zhong-Cheng Xin; Guiting Lin; Lia Banie; Tom F Lue; Ching-Shwun Lin (2006) Urology display abstract
OBJECTIVES: To investigate the effect of icariin on the cyclic guanosine monophosphate (cGMP)-hydrolytic activity of phosphodiesterase-5 (PDE5) isoforms and the cGMP levels in cavernous smooth muscle cells treated with sodium nitroprusside (SNP). METHODS: PDE5 isoforms (PDE5A1, A2, and A3) were isolated from sf9 insect cells infected with baculoviruses carrying PDE5 isoform cDNA. Icariin was isolated from Epimedii herba. Varying amounts (10(-6) to 10(-11) M) of icariin or zaprinast were added to reaction mixtures containing PDE5 isoforms and cGMP. The inhibitory effects of icariin and zaprinast were analyzed by GraphPad Software and are expressed as concentration that inhibits 50% (IC50) values. Cavernous smooth muscle cells were isolated from 3-month-old rats, treated with icariin (100 and 200 microM) or zaprinast (200 microM) for 15 minutes, and then with 10 microM SNP for 30, 60, 120, 240, and 360 minutes. The cells were then analyzed for the cGMP concentration using an enzyme immunoassay system. RESULTS: Icariin inhibited PDE5A1, A2, and A3 with an IC50 value of 1.0, 0.75, and 1.1 microM, respectively. The corresponding IC50 values for zaprinast were 0.33, 0.23, and 0.32 microM. Icariin consistently outperformed the control (SNP-only treatment) in maintaining greater cGMP levels, particularly at the greater concentration of 200 microM. In contrast, zaprinast at 200 microM did better than the control only at 60 and 360 minutes. CONCLUSIONS: Icariin was inhibitory to all three PDE5 isoforms with similar IC50 values, which were approximately three times greater than those for zaprinast. Icariin was able to enhance cGMP levels in SNP-treated cavernous smooth muscle cells.