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VU-0152100

From Wikipedia, the free encyclopedia
Muscarinic acetylcholine receptor positive modulator selective for M4
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 InfoCard100.209.922Edit this at Wikidata
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 mass341.43 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 theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

VU-0152100 is a positive modulator of theM4 receptor,[1] one of themuscarinic acetylcholine receptors.

Treatment of stimulant addiction

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In mice, VU-0152100 is able to decrease self-administration of cocaine, this is thought to come from the M4 receptor's action onD1 containing dopaminergic neurons.[2] It is also able to almost completely inhibit thehyperactivity 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

[edit]

References

[edit]
  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.
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(andprodrugs)


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