French
DeutschVU-0152099
 | |
| Names | |
|---|---|
| IUPAC name 3-Amino-N-(1,3-benzodioxol-5-ylmethyl)-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide | |
| Identifiers | |
3D model (JSmol) | |
| ChEMBL | |
| ChemSpider | |
PubChem CID | |
| |
| |
| Properties | |
| C18H17N3O3S | |
| Molar mass | 355.41 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
VU-0152099 is a positive allosteric modulator of the M4 receptor used in scientific research.
Mechanism of action
[edit]VU-0152099 is a positive allosteric modulator acting at M4 receptors,[1] it lacks agonist activity, which means it cannot activate the receptor on its own, but can potentiate the activity of M4 receptor agonists such as acetylcholine.
Potential use
[edit]In rats, VU-0152099 is able to decrease self-administration of cocaine[2] and reverse hyperlocomotion induced by amphetamine.[1]
These tests show that VU-0152099 could potentially be developed as a treatment for addiction to stimulants.
See also
[edit]References
[edit]- ^ a b Brady, Ashley E.; Jones, Carrie K.; Bridges, Thomas M.; Kennedy, J. Phillip; Thompson, Analisa D.; Heiman, Justin U.; Breininger, Micah L.; Gentry, Patrick R.; Yin, Huiyong; Jadhav, Satyawan B.; Shirey, Jana K.; Conn, P. Jeffrey; Lindsley, Craig W. (December 2008). "Centrally Active Allosteric Potentiators of the M 4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats". Journal of Pharmacology and Experimental Therapeutics. 327 (3): 941–953. doi:10.1124/jpet.108.140350. ISSN 0022-3565. PMC 2745822. PMID 18772318.
- ^ Thomsen, Morgane; Crittenden, Jill R.; Lindsley, Craig W.; Graybiel, Ann M. (March 2022). "Effects of acute and repeated administration of the selective M4 PAM VU0152099 on cocaine versus food choice in male rats". Addiction Biology. 27 (2): e13145. doi:10.1111/adb.13145. ISSN 1369-1600. PMC 9162150. PMID 35229940.