| Identification | Back Directory | [Name]
9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one | [CAS]
869802-58-4 | [Synonyms]
A 841720
3-(azepan-1-yl)-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one
3-(azepan-1-yl)-9-(dimethylamino)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one
9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one
Pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one, 9-(dimethylamino)-3-(hexahydro-1H-azepin-1-yl)- | [Molecular Formula]
C17H21N5OS | [MDL Number]
MFCD09970991 | [MOL File]
869802-58-4.mol | [Molecular Weight]
343.45 |
| Chemical Properties | Back Directory | [Boiling point ]
539.9±60.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
DMSO: soluble15mg/mL, clear | [form ]
powder | [pka]
9.90±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [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]. | [IC 50]
Human mGluR1: 10 nM (IC50); human mGluR5: 342 nM (IC50) | [storage]
Store at RT | [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. |
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