Chemistry:VU-0152100
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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
- VU-0152099
References
- ↑ "VU0152100". https://cdn.caymanchem.com/cdn/insert/32968.pdf.
- ↑ 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. PMID 22648127.
- ↑ 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. PMID 28544993.
- ↑ 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 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. PMID 18772318.
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