VU0238429

VU0238429 is a positive allosteric modulator of M₅ muscarinic acetylcholine receptors (mAChRs; EC₅₀ = 1.16 µM in a calcium mobilization assay).¹ It is selective for M₅ mAChRs over M₁, M₂, M₃, and M₄ mAChRs in CHO cells expressing the human receptors (EC₅₀s = >30 µM for all in calcium mobilization assays). VU0238429 (10 mg/kg) reduces head-twitch behavior induced by the serotonin (5-HT) receptor subtype 5-HT_2A agonist DOI in mice.² It reverses MK-801-induced memory deficits in the novel object recognition test in mice when administered alone or in combination with the GABA_B receptor positive allosteric modulator GS-39783 (Item No. 29482).

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1. Bridges, T.M., Marlo, J.E., Niswender, C.M., et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J. Med. Chem. 52(11), 3445-3448 (2009).

2. Cieślik, P., Woźniak, M., Tokarski, K., et al. Simultaneous activation of muscarinic and GABAB receptors as a bidirectional target for novel antipsychotics. Behav. Brain Res. 359, 671-685 (2019).