1034442-21-1
Chemical Structure
Basimglurant sulfate
Synonym(s): RG7090 sulfate; RO4917523 sulfate
- CAS No.: 1034442-21-1
- Formula:C18H15ClFN3O4S
- Molecular Weight:423.85
IUPAC Name: 2-chloro-4-((1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-yl)ethynyl)pyridine sulfate
InChIKey: RPRPXJNEEIIWAL-UHFFFAOYSA-N
SMILES: O=S(O)(O)=O.FC1=CC=C(N2C(C)=NC(C#CC3=CC(Cl)=NC=C3)=C2C)C=C1
Biological Activity: Basimglurant (RG7090; RO4917523) sulfate is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [3H]-ABP688 (HY-110141)) and 35.6 nM (against [3H]-MPEP (HY-14609A)). Basimglurant sulfate inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant sulfate can be used in research on depression, fragile X syndrome, anxiety disorders, etc[1][2].
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Basimglurant sulfate | Basimglurant (RG7090; RO4917523) sulfate is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a Ki of 1.4 nM (against [3H]-ABP688 (HY-110141)) and 35.6 nM (against [3H]-MPEP (HY-14609A)). Basimglurant sulfate inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant sulfate can be used in research on depression, fragile X syndrome, anxiety disorders, etc. | |||||||||||||||||||||
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- [1]. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. J Med Chem. 2015;58(3):1358-1371. [Content Brief]
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[2]. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33.
[Content Brief]
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