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6- amino- 5- (2,3,5- trichlorophenyl)pyridine- 2- carboxylic acid methylamide

an Nav1.8 channel blocker; structure in first source

Also Known As:

PF-01247324

Networked: 3 relevant articles (0 outcomes, 1 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - Picolinic Acids: 1
      - 6-amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxylic acid methylamide: 3
- Heterocyclic Acids
  - Picolinic Acids: 1
    - 6-amino-5-(2,3,5-trichlorophenyl)pyridine-2-carboxylic acid methylamide: 3

Experts

1.	Butt, Richard P: 2 articles (05/2015 - 01/2015)
2.	Alles, Sascha R A: 1 article (01/2021)
3.	Smith, Peter A: 1 article (01/2021)
4.	Alexandrou, Aristos J: 1 article (05/2015)
5.	Anand, Praveen: 1 article (05/2015)
6.	Anand, Uma: 1 article (05/2015)
7.	Antonio, Brett M: 1 article (05/2015)
8.	Bagal, Sharan: 1 article (05/2015)
9.	Bannon, Anthony W: 1 article (05/2015)
10.	Brown, Adam R: 1 article (05/2015)

Related Diseases

1.	Experimental Autoimmune Encephalomyelitis (Encephalomyelitis, Autoimmune Experimental) 01/01/2015 - "In the present study, we assessed the effect of per os (p.o.) dosing of a new orally bioavailable Nav1.8-selective blocker, PF-01247324, in transgenic mice expressing Nav1.8 in Purkinje neurons, and in wildtype mice in the experimental autoimmune encephalomyelitis (EAE) model. "
2.	Cerebellar Diseases (Cerebellar Syndrome) 01/01/2015 - "These preclinical proof-of-concept data suggest that PF-01247324, its derivatives, or other Nav1.8-selective blockers merit further study for providing symptomatic therapy for cerebellar dysfunction in MS and related disorders. "
3.	T-Cell Lymphoma (Lymphoma, T Cell) 01/01/2021 - "The way forward may include (i) further structural refinement of K+ channel activators such as retigabine and ASP0819 to improve selectivity and limit toxicity; use or modification of Na+ channel blockers such as vixotrigine, PF-05089771, A803467, PF-01247324, VX-150 or arachnid toxins such as Tap1a; the use of Ca2+ channel blockers such as TTA-P2, TTA-A2, Z 944, ACT709478, and CNCB-2; (ii) improving methods for assessing "pain" as opposed to nociception in rodent models; (iii) recognizing sex differences in pain etiology; (iv) tailoring of therapeutic approaches to meet the symptoms and etiology of pain in individual patients via quantitative sensory testing and other personalized medicine approaches; (v) targeting genetic and biochemical mechanisms controlling channel expression using anti-NGF antibodies such as tanezumab or re-purposed drugs such as vorinostat, a histone methyltransferase inhibitor used in the management of T-cell lymphoma, or cercosporamide a MNK 1/2 inhibitor used in treatment of rheumatoid arthritis; (vi) combination therapy using drugs that are selective for different channel types or regulatory processes; (vii) directing preclinical validation work toward the use of human or human-derived tissue samples; and (viii) application of molecular biological approaches such as clustered regularly interspaced short palindromic repeats (CRISPR) technology."
4.	Pain (Aches) 01/01/2021 - "The way forward may include (i) further structural refinement of K+ channel activators such as retigabine and ASP0819 to improve selectivity and limit toxicity; use or modification of Na+ channel blockers such as vixotrigine, PF-05089771, A803467, PF-01247324, VX-150 or arachnid toxins such as Tap1a; the use of Ca2+ channel blockers such as TTA-P2, TTA-A2, Z 944, ACT709478, and CNCB-2; (ii) improving methods for assessing "pain" as opposed to nociception in rodent models; (iii) recognizing sex differences in pain etiology; (iv) tailoring of therapeutic approaches to meet the symptoms and etiology of pain in individual patients via quantitative sensory testing and other personalized medicine approaches; (v) targeting genetic and biochemical mechanisms controlling channel expression using anti-NGF antibodies such as tanezumab or re-purposed drugs such as vorinostat, a histone methyltransferase inhibitor used in the management of T-cell lymphoma, or cercosporamide a MNK 1/2 inhibitor used in treatment of rheumatoid arthritis; (vi) combination therapy using drugs that are selective for different channel types or regulatory processes; (vii) directing preclinical validation work toward the use of human or human-derived tissue samples; and (viii) application of molecular biological approaches such as clustered regularly interspaced short palindromic repeats (CRISPR) technology."
5.	Neuralgia (Stump Neuralgia) 05/01/2015 - "Using PF-01247324, we have confirmed a role for Nav 1.8 channels in both inflammatory and neuropathic pain. " 05/01/2015 - "The inhibition of Nav 1.8 channels by PF-01247324 was studied using in vitro patch-clamp electrophysiology and the oral bioavailability and antinociceptive effects demonstrated using in vivo rodent models of inflammatory and neuropathic pain. "

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Related Therapies and Procedures

1.	Therapeutics
2.	Precision Medicine
3.	Oral Administration