VU-0152100

VU-0152100
Names
IUPAC name
3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard 100.209.922
EC Number
  • 684-470-8
  • InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22)
    Key: MDNWGCQSCGNTKH-UHFFFAOYSA-N
  • CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
Properties
C18H19N3O2S
Molar mass 341.43 g·mol−1
Hazards
GHS labelling:[1]
GHS06: Toxic
Danger
H301, H319
P264, P264+P265, P270, P280, P301+P316, P305+P351+P338, P321, P330, P337+P317, P405, P501
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

VU-0152100 is a positive modulator of the M4 receptor,[1] one of the muscarinic acetylcholine receptors.

Treatment of stimulant addiction

In mice, VU-0152100 is able to decrease self-administration of cocaine, this is thought to come from the M4 receptor's action on D1 containing dopaminergic neurons.[2] It is also able to almost completely inhibit the hyperactivity caused by cocaine.[3] Another study has shown that this drug is able to reverse hyperlocomotion induced by amphetamine, in an anti-psychotic-like manner.[4] This data suggests that it could potentially be developed as a treatment for stimulant abuse.

See also

References

  1. ^ "VU0152100" (PDF).
  2. ^ Dencker, Ditte; Weikop, Pia; Sørensen, Gunnar; Woldbye, David P. D.; Wörtwein, Gitta; Wess, Jürgen; Fink-Jensen, Anders (November 2012). "An allosteric enhancer of M₄ muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine". Psychopharmacology. 224 (2): 277–287. doi:10.1007/s00213-012-2751-8. ISSN 1432-2072. PMC 3914671. PMID 22648127.
  3. ^ Dall, Camilla; Weikop, Pia; Dencker, Ditte; Molander, Anna C.; Wörtwein, Gitta; Conn, P. Jeffrey; Fink-Jensen, Anders; Thomsen, Morgane (2017-07-01). "Muscarinic receptor M4 positive allosteric modulators attenuate central effects of cocaine". Drug and Alcohol Dependence. 176: 154–161. doi:10.1016/j.drugalcdep.2017.03.014. ISSN 1879-0046. PMC 6423356. PMID 28544993.
  4. ^ 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 M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats". The Journal of Pharmacology and Experimental Therapeutics. 327 (3): 941–953. doi:10.1124/jpet.108.140350. ISSN 1521-0103. PMC 2745822. PMID 18772318.


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