Neuronal NOS | Nitric oxide synthases | IUPHAR/BPS Guide to PHARMACOLOGY

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Neuronal NOS

Target not currently curated in GtoImmuPdb

Target id: 1251

Nomenclature: Neuronal NOS

Abbreviated Name: nNOS

Family: Nitric oxide synthases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - NOS1 nitric oxide synthase 1
Mouse - - Nos1 nitric oxide synthase 1
Rat - - Nos1 nitric oxide synthase 1
Previous and Unofficial Names
brain NOS | NOS1 | constitutive NOS | NC-NOS | neuronal NOS | nitric oxide synthase 1 | Nitric oxide synthase 1 (neuronal) | Nitric oxide synthase 1 / NOSI | nitric oxide synthase 1 (neuronal)
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of rat neuronal nitric oxide synthase heme domain in complex with 4-methyl-6-(2-(5-(3-(methylamino)propyl)pyridin-3-yl) ethyl)pyridin-2-amine
PDB Id:  5FVS
Ligand:  compound 14j [PMID: 27050842]
Resolution:  1.95Å
Species:  Rat
References:  3
Enzyme Reaction
EC Number: 1.14.13.39
Products
Product Species Reference
NO Human
L-citrulline Human
Cofactors
Cofactor Species Comments Reference
Zn2+ Human
NADPH Human
heme Human
flavin adenine dinucleotide Human
flavin mononucleotide Human
BH4 Human
oxygen Human
Endogenous Substrate (Human)
L-arginine

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 14j [PMID: 27050842] Hs Inhibition 7.9 pKi 3
pKi 7.9 (Ki 1.3x10-8 M) [3]
L-NNA Hs Inhibition 7.8 pKi 1
pKi 7.8 (Ki 1.5x10-8 M) [1]
compound 14j [PMID: 27050842] Rn Inhibition 7.8 pKi 3
pKi 7.8 (Ki 1.6x10-8 M) [3]
Nωpropyl-L-arginine Rn Inhibition 7.2 pKi 4
pKi 7.2 [4]
GW274150 Hs Inhibition 4.7 pIC50 2
pIC50 4.7 (IC50 1.8x10-5 M) [2]
NANT N/A Inhibition - -
View species-specific inhibitor tables

References

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1. Collins JL, Shearer BG, Oplinger JA, Lee S, Garvey EP, Salter M, Duffy C, Burnette TC, Furfine ES. (1998) N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity. J. Med. Chem., 41 (15): 2858-71. [PMID:9667974]

2. Connolly S, Aberg A, Arvai A, Beaton HG, Cheshire DR, Cook AR, Cooper S, Cox D, Hamley P, Mallinder P et al.. (2004) 2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution. J. Med. Chem., 47 (12): 3320-3. [PMID:15163211]

3. Wang HY, Qin Y, Li H, Roman LJ, Martásek P, Poulos TL, Silverman RB. (2016) Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker. J. Med. Chem., 59 (10): 4913-25. [PMID:27050842]

4. Zhang HQ, Fast W, Marletta MA, Martasek P, Silverman RB. (1997) Potent and selective inhibition of neuronal nitric oxide synthase by N omega-propyl-L-arginine. J. Med. Chem., 40 (24): 3869-70. [PMID:9397167]

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