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Drug-Target Interaction

Drug

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PubChem ID:1125
Structure:
Synonyms:
(1R,2S)-(2-Amino-3,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)-1,2-propandiol
(6R)-2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-1H-pteridin-4-one
(6R)-2-amino-6-[(1S,2R)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-1H-pteridin-4-one
(6r,1'r,2's)-5,6,7,8 Tetrahydrobiopterin
17528-72-2
2-Amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydoro-4(1H)-pteridinone
2-amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-1H-pteridin-4-one
2-amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydropteridin-4(3H)-one
4(1H)-Pteridinone, 5,6,7,8-tetrahydro-2-amino-6-(1,2-dihydroxypropyl)-
5,6,7,8 Tetrahydrobiopterin
5,6,7,8-erythro-tetrahydrobiopterin
5,6,7,8-tetra-H-biopterin
5,6,7,8-Tetrahydro-2-amino-6-(1,2-dihydroxypropyl)-4(1H)-pteridinone
5,6,7,8-tetrahydro-L-erythrobiopterin
5,6,7,8-tetrahydrobiopterin
5,6,7,8-tetrahydrodictyopterin
5-26-18-00418 (Beilstein Handbook Reference)
6R-BH4
6R-L-erythro-5,6,7,8-tetrahydrobiopterin
6s-5,6,7,8-Tetrahydrobiopterin
7-tetrahydrobiopterin
BH4
BPH4
BRN 0544742
C00272
C9H15N5O3
CHEBI:15372
DB00360
DB02692
DB03918
Kuvan
L-erythro-2-Amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-4(3H)-pteridi
L-erythro-2-Amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-4(3H)-pteridinon
LS-126327
Phenoptin
phenylalanine hydroxylase cofactor
TETRA-H-BIOPTERIN
tetra-hydro-biopterin
tetrahydro-6-biopterin
tetrahydrobiopterin
THBP
Side-Effects:
Side-EffectFrequency
convulsions0.0010
testicular carcinoma0
rhinorrhea0
diarrhea0
vomiting0
peripheral edema0
gastrointestinal hemorrhage0
pain0
nausea0
arthralgia0
upper respiratory tract infection0
streptococcal infections0
headache0
abdominal pain0
dizziness0
gastritis0
rash0
agitation0
respiratory failure0
fever0
nasal congestion0
myocardial infarction0
cough0
hemorrhage0
urinary tract infection0
neutropenia0
polyuria0
irritability0

Target

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Uniprot ID:NOS3_HUMAN
Synonyms:
cNOS
Constitutive NOS
EC-NOS
Endothelial NOS
eNOS
Nitric oxide synthase, endothelial
NOS type III
NOSIII
EC-Numbers:1.14.13.39
Organism:Homo sapiens
Human
PDB IDs:1M9J 1M9K 1M9M 1M9Q 1M9R 3EAH 3NOS
Structure:
3NOS

Binding Affinities:

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

References:

11053217
Tetrahydrobiopterin impairs the action of endothelial nitric oxide via superoxide derived from platelets.. M Tajima; H Sakagami (2000) British journal of pharmacology display abstract
The mechanism by which exogenous tetrahydrobiopterin (BH(4)) impairs the action of endothelial nitric oxide (NO) in the presence of platelets was investigated. The endothelial NO generated by shear stress was determined by the anti-aggregating activity of indomethacin-treated endothelial cells and the cyclic GMP concentration in platelets. The inhibitory effect of exogenous BH(4) was suppressed by superoxide dismutase (SOD), or diclofenac sodium at concentrations inhibiting O(2)(-) generation, but not by allopurinol, a xanthine oxidase inhibitor. BH(4) similarly inhibited the anti-aggregatory effect of sodium nitroprusside (SNP), a NO donor. The inhibitory effect was suppressed by diphenyleneiodonium, a specific inhibitor of NADPH oxidase. Six(S)-BH(4), an inactive diastereoisomer of 6(R)-BH(4), and the 5,6,7,8-tetrahydropterin compounds inhibited the endothelial NO action, whereas sepiapterin and 7,8-dihydrobiopterin (BH(2)), 5,6-double bond pterins, were inactive. These tetrahydropterins, but not sepiapterin and BH(2), scavenged superoxide (O(2)(-)) generated by the hypoxanthine-xanthine oxidase reaction, possibly due to electron transfer during oxidation to its quinonoid-form. BH(4) markedly stimulated the O(2)(-) generation from platelets, in the presence of NADH, rather than that of NADPH. These findings suggest that BH(4) stimulates platelet NAD(P)H oxidase to generate O(2)(-), and inhibits the anti-aggregating effect of NO. SOD activity in the local environment may modify the effect of BH(4) on the endothelial NO activity.
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