1428327-31-4 Usage
Description
N-[[4-(4-phenyl-piperazin-1-yl)tetrahydro-2H-pyran-4-yl]methyl]-2-(phenylthio)nicotinamide, also known as JNJ-47965567, is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. It is characterized by its ability to reduce calcium flux induced by the activation of P2X receptors by BzATP in various species, including human, macaque, dog, rat, and mouse. JNJ-47965567 also exhibits anticonvulsant properties and is effective in suppressing neonatal hypoxia-induced seizures in mice and reducing spontaneous seizures in epileptic mice even after treatment cessation.
Uses
1. Used in Pharmaceutical Applications:
N-[[4-(4-phenyl-piperazin-1-yl)tetrahydro-2H-pyran-4-yl]methyl]-2-(phenylthio)nicotinamide is used as a potent and selective human P2X7 antagonist for its ability to modulate the P2X7 receptor, which plays a role in various physiological and pathological processes.
2. Used in Neurological Applications:
In the field of neurology, N-[[4-(4-phenyl-piperazin-1-yl)tetrahydro-2H-pyran-4-yl]methyl]-2-(phenylthio)nicotinamide is used as an anticonvulsant agent for its effectiveness in suppressing neonatal hypoxia-induced seizures in mice and reducing spontaneous seizures in epileptic mice.
3. Used in Preclinical Research:
N-[[4-(4-phenyl-piperazin-1-yl)tetrahydro-2H-pyran-4-yl]methyl]-2-(phenylthio)nicotinamide is utilized as a research tool in preclinical studies to investigate the role of P2X7 receptors in various conditions and to develop potential therapeutic strategies targeting these receptors.
4. Used in Drug Development:
In the pharmaceutical industry, N-[[4-(4-phenyl-piperazin-1-yl)tetrahydro-2H-pyran-4-yl]methyl]-2-(phenylthio)nicotinamide serves as a lead compound for the development of new drugs targeting the P2X7 receptor, with potential applications in treating neurological disorders and other conditions related to P2X7 receptor activation.
Biochem/physiol Actions
JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped.
Check Digit Verification of cas no
The CAS Registry Mumber 1428327-31-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,2,8,3,2 and 7 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1428327-31:
(9*1)+(8*4)+(7*2)+(6*8)+(5*3)+(4*2)+(3*7)+(2*3)+(1*1)=154
154 % 10 = 4
So 1428327-31-4 is a valid CAS Registry Number.
1428327-31-4Relevant articles and documents
Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists
Letavic, Michael A.,Lord, Brian,Bischoff, Francois,Hawryluk, Natalie A.,Pieters, Serge,Rech, Jason C.,Sales, Zachary,Velter, Adriana I.,Ao, Hong,Bonaventure, Pascal,Contreras, Victor,Jiang, Xiaohui,Morton, Kirsten L.,Scott, Brian,Wang, Qi,Wickenden, Alan D.,Carruthers, Nicholas I.,Bhattacharya, Anindya
supporting information, p. 419 - 422 (2013/06/26)
The synthesis and preclinical characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to
