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sapropterin

Structure via PubChem · Public domain (PubChem)

EntityQ419808· pop 22· linked from 581 articles

sapropterin

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Also known as 5,6,7,8-Tetrahydrobiopterin, 5,6,7,8 Tetrahydrobiopterin, BH4, (6R)-2-Amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydropteridin-4(1H)-one, 2-Amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydoro-4(1H)-pteridinone, 2-amino-6-(1,2-dihydroxypropyl)-3,4,5,6,7,8-hexahydropteridin-4-one, L-Erythro-2-Amino-6-(1,2-dihydroxypropyl)-5,6,7,8-tetrahydro-4(3H)-pteridinon, 5,6,7,8-Erythro-tetrahydrobiopterin

Tetrahydrobiopterin (BH4, THB), also known as sapropterin (INN), is a cofactor of the three aromatic amino acid hydroxylase enzymes, used in the metabolism of amino acid phenylalanine and in the biosynthesis of the neurotransmitters serotonin (5-hydroxytryptamine, 5-HT), melatonin, dopamine, norepinephrine (noradrenaline), epinephrine (adrenaline), and is a cofactor for the production of nitric oxide (NO) by the nitric oxide synthases. Chemically, its structure is that of a (dihydropteridine reductase) reduced pteridine derivative (quinonoid dihydrobiopterin).

Key facts

Drug.ChemSpiderID
40270
Drug.ChemSpiderID2
552166
Drug.Verifiedfields
changed
Drug.verifiedrevid
470604083
Drug.INN
Sapropterin
Drug.image
(6R)-Tetrahydrobiopterin structure.svg
Drug.image_class
skin-invert-image
Drug.JAN
Sapropterin hydrochloride
Drug.USAN
Sapropterin dihydrochloride
Drug.tradename
Kuvan, Biopten
Drug.MedlinePlus
a608020
Drug.licence_EU
yes
Drug.DailyMedID
Sapropterin
Drug.licence_US
Sapropterin
Drug.pregnancy_AU
B1
Drug.routes_of_administration
By mouth
Drug.ATC_prefix
A16
Drug.ATC_suffix
AX07

via Wikipedia infobox

Chemical data

Formula
C9H15N5O3
Molecular weight
241.25 g/mol
IUPAC name
(6R)-2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-5,6,7,8-tetrahydro-1H-pteridin-4-one
SMILES
C[C@@H]([C@@H]([C@H]1CNC2=C(N1)C(=O)N=C(N2)N)O)O
InChIKey
FNKQXYHWGSIFBK-RPDRRWSUSA-N
XLogP
-1.9
Polar surface area
132 Ų
H-bond donors
6
H-bond acceptors
5
Formal charge
0

via PubChem

Wikidata facts

Mass
241.117489
Show 4 more facts
chemical formula
C₉H₁₅N₅O₃
isomeric SMILES
C[C@H](O)[C@H](O)[C@H]1CNc2[nH]c(=N)nc(O)c2N1
canonical SMILES
N=C1N=C(O)C=2NC(CNC2N1)C(O)C(O)C
Commons category
Tetrahydrobiopterin
Sources (3)

via Wikidata · CC0

~9 min read

Article

20 sections
Contents
  • Medical uses
  • Adverse effects
  • Interactions
  • Functions
  • Cofactor for tryptophan hydroxylases
  • Cofactor for phenylalanine hydroxylase
  • Cofactor for tyrosine hydroxylase
  • Cofactor for nitric oxide synthase
  • Cofactor for ether lipid oxidase
  • History
  • Biosynthesis and recycling
  • Research
  • Depression
  • Autism
  • Cardiovascular disease
  • Neuroprotection in prenatal hypoxia
  • Programmed cell death
  • References
  • Further reading
  • External links

Tetrahydrobiopterin (BH4, THB), also known as sapropterin (INN), is a cofactor of the three aromatic amino acid hydroxylase enzymes, used in the metabolism of amino acid phenylalanine and in the biosynthesis of the neurotransmitters serotonin (5-hydroxytryptamine, 5-HT), melatonin, dopamine, norepinephrine (noradrenaline), epinephrine (adrenaline), and is a cofactor for the production of nitric oxide (NO) by the nitric oxide synthases. Chemically, its structure is that of a (dihydropteridine reductase) reduced pteridine derivative (quinonoid dihydrobiopterin).

Tetrahydrobiopterin is available as a tablet for oral administration in the form of sapropterin dihydrochloride (BH4*2HCL). It was approved for use in the United States as a tablet in December 2007 and as a powder in December 2013. It was approved for use in the European Union in December 2008, Canada in April 2010, and Japan in July 2008. It is sold under the brand names Kuvan and Biopten. The typical cost of treating a patient with Kuvan is per year. BioMarin holds the patent for Kuvan until at least 2024, but Par Pharmaceutical has a right to produce a generic version by 2020.

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