VU-0152099 explained
VU-0152099 is a positive allosteric modulator of the M4 receptor used in scientific research.
Mechanism of action
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
In rats, VU-0152099 is able to decrease self-administration of cocaine[2] and reverse hyperlocomotion induced by amphetamine.
These tests show that VU-0152099 could potentially be developed as a treatment for addiction to stimulants.
See also
Notes and References
- 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 . en . 327 . 3 . 941–953 . 10.1124/jpet.108.140350 . 0022-3565 . 2745822 . 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 . 10.1111/adb.13145 . 1369-1600 . 9162150 . 35229940.