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Drug-Target Interaction

Drug

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PubChem ID:44257
Structure:
Synonyms:
(-)-(6R)-2-Amino-6-((1R,2S)-1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-4(3H)-
(-)-(6R)-2-Amino-6-((1R,2S)-1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-4(3H)-pteridinone
(6R)-2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydropteridin-4(1H)-one
(6R,1'R,2'S)-5,6,7,8 TETRAHYDROBIOPTERIN
17528-72-2
27070-47-9
5,6,7,8-TETRAHYDROBIOPTERIN
62989-33-7
6R-5,6,7,8-Tetrahydrobiopterin
6R-BH4
6R-L-5,6,7,8-Tetrahydrobiopterin
BCBcMAP01_000204
BH4
CHEBI:59560
H4B
Kuvan
R-THBP
Sapropterin
Sapropterin (INN)
SAPROPTERIN HYDROCHLORIDE
Sapropterin [INN]
Sapropterina
Sapropterina [INN-Spanish]
Sapropterinum
Sapropterinum [INN-Latin]
SMP1_000285
TETRAHYDROBIOPTERIN
THB
ZINC13585233
ATC-Codes:
Side-Effects:
Side-EffectFrequency
convulsions0.0010
abdominal pain0
neutropenia0
pain0
polyuria0
streptococcal infections0
upper respiratory tract infection0
urinary tract infection0
vomiting0
agitation0
peripheral edema0
testicular carcinoma0
respiratory failure0
nausea0
nasal congestion0
myocardial infarction0
arthralgia0
cough0
diarrhea0
dizziness0
rash0
fever0
gastritis0
gastrointestinal hemorrhage0
headache0
hemorrhage0
irritability0
rhinorrhea0

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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