2926782-31-0
Chemical Structure
VU6019650
- CAS No.: 2926782-31-0
- Formula:C18H22FN3O3S2
- Molecular Weight:411.51
InChIKey: MWXZKSDFCSPEBK-ZBFHGGJFSA-N
SMILES: O=S(C1=CC2=C(OCC2)C=C1)(N(CC[C@@H]3CSC4=NC=CN4C)C[C@@H]3F)=O
Biological Activity: VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA)[1][2].
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VU6019650 | 99.83% | VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA). | ||||||||||||||||||||
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- [1]. Garrison AT, et al. Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. J Med Chem. 2022 Apr 28;65(8):6273-6286. [Content Brief]
- [2]. Capstick RA, et al. Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorg Med Chem Lett. 2022 Nov 15;76:128988. [Content Brief]
Keywords
