Bulk Inquiry
A 841720
- Soluble in DMSO
- MF: C17H21N5OS
- MW: 343.45
Description
A 841720 is a potent and selective non-competitive metabotropic glutamate receptor 1 (mGlu1/mGluR1) antagonist with reported IC50 of 10 nM. It shows 34-fold selectivity over mGluR5 and lacks significant activity at other tested receptors, ion channels and transporters.
mGluR1 regulates excitatory neurotransmission, synaptic plasticity and nociceptive processing. A 841720 is pharmacologically relevant for glutamate receptor studies and for evaluating mGluR1 blockade in inflammatory and neuropathic pain models.
Key Features
- Potent non-competitive mGluR1 antagonist
- Selectivity over mGluR5 and other targets
- Nanomolar functional potency
- Efficacy reported in multiple pain models
Applications
- mGluR1 receptor pharmacology
- Glutamatergic signaling studies
- Pain and nociception model research
- CNS receptor selectivity profiling
More Information
| Parent CAS No. | 869802-58-4 |
|---|---|
| Chemical Name | 9-(Dimethylamino)-3-(hexahydro-1H-azepin-1-yl)-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one |
| SMILES | C1N(N2CCCCCC2)C(=O)C2SC3=NC=CC(N(C)C)=C3C=2N=1 |
| MFCD | MFCD09970991 |
| InChi | InChI=1S/C17H21N5OS/c1-20(2)12-7-8-18-16-13(12)14-15(24-16)17(23)22(11-19-14)21-9-5-3-4-6-10-21/h7-8,11H,3-6,9-10H2,1-2H3 |
| InChiKey | GYWGXEGOXODOQU-UHFFFAOYSA-N |
| CID | 11559235 |
| Short Description | mGluR1 antagonist |
References
- GZ Zheng et al. Structure-Activity Relationship of Triazafluorenone Derivatives as Potent and Selective mGluR1 Antagonists. J. Med. Chem. 2005, 48, 7374-7388.
- O El-Kouhen 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. Br. J. Pharmacol. 2006, 149, 761-774.
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