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4- ((2- cyclobutyl- 1H- imidazo(4,5- b)pyrazin- 1- yl)methyl)- 7,8- difluoroquinolin- 2(1H)- one

inhibits both iNOS and nNOS dimerization; structure in first source

Also Known As:

KD 7332; KD-7332; KD7332; KLYP 961; KLYP-961; KLYP961

Networked: 3 relevant articles (0 outcomes, 0 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyrazines: 150
    - 4-((2-cyclobutyl-1H-imidazo(4,5-b)pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one: 3
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinolines: 146
      - Quinolones: 2938
        Fluoroquinolones: 5348
        4-((2-cyclobutyl-1H-imidazo(4,5-b)pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one: 3

Experts

1.	Hassig, Christian A: 3 articles (02/2011 - 05/2009)
2.	Nguyen, Phan M: 3 articles (02/2011 - 05/2009)
3.	Noble, Stewart A: 3 articles (02/2011 - 05/2009)
4.	Payne, Joseph E: 3 articles (02/2011 - 05/2009)
5.	Rao, Tadimeti S: 3 articles (02/2011 - 05/2009)
6.	Rozenkrants, Natasha: 3 articles (02/2011 - 05/2009)
7.	Sablad, Marciano: 3 articles (02/2011 - 05/2009)
8.	Shiau, Andrew K: 3 articles (02/2011 - 05/2009)
9.	Smith, Nicholas D: 3 articles (02/2011 - 05/2009)
10.	Symons, Kent T: 3 articles (02/2011 - 05/2009)

Related Diseases

1.	Pain (Aches) 02/01/2011 - "In summary, KLYP961 represents an ideal tool with which to probe the physiological role of NO derived from iNOS and nNOS in human pain and inflammatory states." 05/14/2009 - "Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models." 11/11/2010 - "Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNOS dimerization inhibitors that are orally active in pain models." 02/01/2011 - "KLYP961 attenuated pain behaviors in a mouse formalin model (ED(50) 13 mg/kg p.o.), cold allodynia in the chronic constriction injury model (ED(50) 25 mg/kg p.o.), or tactile allodynia in the spinal nerve ligation model (ED(50) 30 mg/kg p.o.) with similar efficacy, but superior potency relative to gabapentin, pregabalin, or duloxetine. "
2.	Hyperalgesia 02/01/2011 - "KLYP961 also attenuated capsaicin-induced thermal allodynia in rhesus primates in a dose-related manner with a minimal effective dose (≤ 10 mg/kg p.o.) and a greater potency than gabapentin. " 02/01/2011 - "KLYP961 also attenuated carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by phenylbenzoquinone with efficacy and potency similar to those of celecoxib. " 02/01/2011 - "KLYP961 attenuated pain behaviors in a mouse formalin model (ED(50) 13 mg/kg p.o.), cold allodynia in the chronic constriction injury model (ED(50) 25 mg/kg p.o.), or tactile allodynia in the spinal nerve ligation model (ED(50) 30 mg/kg p.o.) with similar efficacy, but superior potency relative to gabapentin, pregabalin, or duloxetine. "
3.	Edema (Dropsy) 02/01/2011 - "KLYP961 also attenuated carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by phenylbenzoquinone with efficacy and potency similar to those of celecoxib. "

Related Drugs and Biologics

1.	Quinolones
2.	Nitric Oxide Synthase Type I (Neuronal Nitric Oxide Synthase)
3.	Nitric Oxide Synthase Type II (Inducible Nitric Oxide Synthase)
4.	Formaldehyde (Formol)
5.	Carrageenan
6.	Capsaicin (Zostrix)
7.	Gabapentin (Neurontin)
8.	Pregabalin (Lyrica)
9.	Duloxetine Hydrochloride (Cymbalta)
10.	Celecoxib (Celebrex)

Related Therapies and Procedures

1.	Ligation