Chemistry:VU-0152099
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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.[1]
These tests show that VU-0152099 could potentially be developed as a treatment for addiction to stimulants.
See also
References
- ↑ 1.0 1.1 Brady, Ashley E.; Jones, Carrie K.; Bridges, Thomas M.; Kennedy, J. Phillip; Thompson, Analisa D.; Heiman, Justin U.; Breininger, Micah L.; Gentry, Patrick R. et al. (December 2008). "Centrally Active Allosteric Potentiators of the M 4 Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats" (in en). Journal of Pharmacology and Experimental Therapeutics 327 (3): 941–953. doi:10.1124/jpet.108.140350. ISSN 0022-3565. 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). doi:10.1111/adb.13145. ISSN 1369-1600. PMID 35229940.
