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VU 0365114
- Soluble in DMSO and EtOH
- MF: C22H14F3NO3
- MW: 397.35
Description
VU 0365114 is a selective positive allosteric modulator (PAM) of the M5 muscarinic acetylcholine receptor (mAChR) with reported EC50 activity of 2.7 µM at M5 and weak activity at M1-M4 subtypes.
The M5 receptor is implicated in central cholinergic signaling, dopaminergic modulation and cerebrovascular regulation. VU 0365114 is useful for probing CHRM5-selective allosteric modulation without directly activating other muscarinic receptor subtypes.
Key Features
- Selective M5 muscarinic receptor PAM
- Reported EC50: 2.7 µM at M5
- Displays selectivity over M1-M4 muscarinic subtypes
- Modulates acetylcholine receptor signaling allosterically
Applications
- M5 receptor pharmacology
- Cholinergic signaling studies
- Allosteric modulator screening
- CNS receptor pathway research
More Information
| Parent CAS No. | 1208222-39-2 |
|---|---|
| Chemical Name | 1-(biphenyl-4-ylmethyl)-5-(trifluoromethoxy)indoline-2,3-dione |
| SMILES | C1(OC(F)(F)F)C=C2C(=O)C(=O)N(CC3C=CC(C4C=CC=CC=4)=CC=3)C2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C22H14F3NO3/c23-22(24,25)29-17-10-11-19-18(12-17)20(27)21(28)26(19)13-14-6-8-16(9-7-14)15-4-2-1-3-5-15/h1-12H,13H2 |
| InChiKey | SPBGRXOPAXZSER-UHFFFAOYSA-N |
| CID | 45281794 |
| Short Description | M5 PAM |
References
- TM Bridges et al. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. Bioorg. Med. Chem. Lett. 2010, 20(19), 5617.
- Structure-activity relationships for a series of M5 muscarinic receptor modulators. by Rao, Paluri Sai Shantanu, Pharm.D., The University of Toledo, Dissertations & Theses 2011, P/N 3489809.
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