869802-58-4 Usage
Uses
A 841720 is a potent & non-competitive mGluR-1 antagonist.
Biological Activity
a 841720 is a novel non-competitive antagonist of metabotropic glutamate receptor 1 (mglur1), with an ic50 value of 10.7 nm to 10 μm l-glutamate-induced calcium release at human mglur1 receptors [1].glutamate as the major excitatory neurotransmitter in the central nervous system functions through two types of receptors, ionotropic glutamate receptors and metabotropic glutamate receptors (mglurs). mglurs includes group i mglurs (mglur1 and mglur5 receptors), group ii (mglur2 and mglur3 receptors) and group iii (mglur4, 6, 7, 8 receptors) [1].in cells, agonist-induced calcium release was concentration-dependently inhibited by a 841720 in a human mglur5 receptor flipr functional assay. but the ic50 value was just 343 nm. in cells expressing recombinant mglur5 receptors, a 841720 did not block agonist-induced response. in the human mglur1 receptor flipr assay, the log concentration-response curve was shifted by a 841720 at 10 nm to the right. a 841720 at increasing concentrations profoundly reduced the amplitude of l-quisqualate-evoked calcium release. a 841720 at 30 nm reduced the maximal agonist-induced response by 38%. l-quisqualate-induced response was completely abolished by a 841720 at 100 nm [1].in a water maze test, all rats gradually learned to locate the submerged platform. treatment with a 841720 significantly slowered rats to find the platform than vehicle control rats. rats treated with a 841720 at both 30 and 100 μmol/kg doses not only significantly traveled longer distance to find the hidden platform, but also significantly spent longer time to reach the platform [1].
references
[1]. el-kouhen o, lehto sg, pan jb, et al. blockade of mglur1 receptor results in analgesia and disruption of motor and cognitive performances: effects of a-841720, a novel non-competitive mglur1 receptor antagonist. british journal of pharmacology, 2006, 149(6): 761-774.
Check Digit Verification of cas no
The CAS Registry Mumber 869802-58-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,6,9,8,0 and 2 respectively; the second part has 2 digits, 5 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 869802-58:
(8*8)+(7*6)+(6*9)+(5*8)+(4*0)+(3*2)+(2*5)+(1*8)=224
224 % 10 = 4
So 869802-58-4 is a valid CAS Registry Number.
869802-58-4Relevant articles and documents
ANTAGONISTS OF THE MGLU RECEPTOR AND USES THEREOF
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Page/Page column 35-36, (2008/06/13)
The present invention discloses compounds of general formula (I) wherein X1-X4 and R1-R3 are as defined in the description. The present invention also discloses methods of treatment for pain, neurodegeneration and convulsive states in a host mammal in need thereof, and pharmaceutical compositions including those compounds.
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists
Zheng, Guo Zhu,Bhatia, Pramila,Daanen, Jerome,Kolasa, Teodozyj,Patel, Meena,Latshaw, Steven,El Kouhen, Odile F.,Chang, Renjie,Uchic, Marie E.,Miller, Loan,Nakane, Masaki,Lehto, Sonya G.,Honore, Marie P.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 7374 - 7388 (2007/10/03)
SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative alloste
