VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic.
VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) reverses amphetamine-induced perlocomotion in a dose-dependent manner [1].
References:
[1]. Le U, et al. Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett. 2013 Jan 1;23(1):346-50.