VU-0152099

VU-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)	Interactive image;
ChEMBL	ChEMBL4461667;
ChemSpider	1261401;
PubChem CID	1541501;
	InChI InChI=1S/C18H17N3O3S/c1-9-5-10(2)21-18-14(9)15(19)16(25-18)17(22)20-7-11-3-4-12-13(6-11)24-8-23-12/h3-6H,7-8,19H2,1-2H3,(H,20,22) Key: AZOGCTMOKNTHIU-UHFFFAOYSA-N;
	SMILES CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC4=C(C=C3)OCO4)N)C;
Properties
Chemical formula	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). Infobox references

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.

References

^ ^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.

[:0-1] Brady, Ashley E.; Jones, Carrie K.; Bridges, Thomas M.; Kennedy, J. Phillip; Thompson, Analisa D.; Heiman, Justin U.; Breininger, Micah L.; Gentry, Patrick R.; 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.

[2] 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.

[1]

[2]

Mechanism of action

Potential use

See also

References