Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H16ClN3OS |
| Molecular Weight | 345.846 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC2=C(C(N)=C(S2)C(=O)NCC3=CC=C(Cl)C=C3)C(C)=C1
InChI
InChIKey=FPRULFHDSFKYBV-UHFFFAOYSA-N
InChI=1S/C17H16ClN3OS/c1-9-7-10(2)21-17-13(9)14(19)15(23-17)16(22)20-8-11-3-5-12(18)6-4-11/h3-7H,8,19H2,1-2H3,(H,20,22)
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/18772318
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/18772318
VU 10010 is a selective allosteric potentiator of M4 acetylcholine receptors. VU 10010 had no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5. VU 10010 is selective for M4 relative to other mAChRs - this compound does not displace [3H]NMS binding at any (rM1, rM2, rM3 and rM5) mAChR subtype. VU10010 was not found to be centrally active. It suffers from poor physiochemical properties. Novel analogs of VU10010 are CNS penetrant following systemic administration.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Presynaptic M3 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in area CA1 of rat hippocampus. | 2015-12-10 |
|
| Functional activation of G-proteins coupled with muscarinic acetylcholine receptors in rat brain membranes. | 2014 |
|
| Synaptic muscarinic response types in hippocampal CA1 interneurons depend on different levels of presynaptic activity and different muscarinic receptor subtypes. | 2013-10 |
|
| Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. | 2008-12 |
|
| An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. | 2008-01 |
Patents
Sample Use Guides
The Ki value for ACh at the orthosteric site decreased from 540 ± 72 nM in the absence of VU 10010 to 39 ± 7 nM in the presence of 10 uM VU 10010. These data suggest that this compound binds to an allosteric site on the M4 mAChR and shifts the receptor into a conformation that has higher affinity for ACh.
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