VU0238429

VU0238429 is a positive allosteric modulator of M5 muscarinic acetylcholine receptors (mAChRs, EC50 = 1.16 µM in a calcium mobilization assay). 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-HT2A agonist DOI in mice. It reverses MK-801-induced memory deficits in the novel object recognition test in mice when administered alone or in combination with the GABAB receptor positive allosteric modulator GS-39783 (Cay-29482).Formal Name: 1-[(4-methoxyphenyl)methyl]-5-(trifluoromethoxy)-1H-indole-2,3-dione. CAS Number: 1160247-92-6. Synonyms: HY-12157, ML129. Molecular Formula: C17H12F3NO4. Formula Weight: 351.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: 15 mg/ml. lambdamax: 228, 245 nm. SMILES: O=C1C(N(CC2=CC=C(C=C2)OC)C3=CC=C(C=C13)OC(F)(F)F)=O. InChi Code: InChI=1S/C17H12F3NO4/c1-24-11-4-2-10(3-5-11)9-21-14-7-6-12(25-17(18,19)20)8-13(14)15(22)16(21)23/h2-8H,9H2,1H3. InChi Key: CKLGZXFOLMHCMC-UHFFFAOYSA-N.