Usmarapride

• CAT Number: I045553
• CAS Number: 1428862-33-2
• Molecular Formula: C23H31N5O6
• Molecular Weight: 473.52
• Purity: ≥95%
• Synonyms: 2-[1-(3-methoxypropyl)piperidin-4-yl]-5-(1-propan-2-ylindazol-3-yl)-1,3,4-oxadiazole;oxalic acid
• InChI: InChI=1S/C21H29N5O2.C2H2O4/c1-15(2)26-18-8-5-4-7-17(18)19(24-26)21-23-22-20(28-21)16-9-12-25(13-10-16)11-6-14-27-3;3-1(4)2(5)6/h4-5,7-8,15-16H,6,9-14H2,1-3H3;(H,3,4)(H,5,6)
• InChIKey: XHXCJKNEBFAUSE-UHFFFAOYSA-N
• SMILES: CC(C)N1C2=CC=CC=C2C(=N1)C3=NN=C(O3)C4CCN(CC4)CCCOC.C(=O)(C(=O)O)O

Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer’s disease[1].
Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) attenuates the long-term memory deficits in object recognition test (ORT)[1].
Usmarapride (1, 3, and 10 mg/kg; p.o.) significantly reverses the scopolamine-induced amnesia[1].
Usmarapride shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index[1].
Usmarapride (SUVN-D4010) shows good oral exposures, good bioavailability, and good brain exposures in rats[1].
Pharmacokinetic of Usmarapride in Rats[1]
(3.0 mg/kg for p.o. dosing; 1.0 mg/kg for i.v.)

F%
Cmax (ng/mL)
AUC (ng·hr/mL)
t1/2 (h)
Vdss (L/kg)
CL (mLg/min/kg)

34
360
709
1.7
8.0
76

Reference

[1]. Nirogi, Ramakrishna; Mohammed, Abdul Rasheed; Yarlgadda, Suresh; Ravella, Srinivasa Rao; Shinde, Anil Karbhari; Kambhampati, Ramasastri; Roayalley, Praveen Kumar; Jayarajan, Pradeep; Bhyrapuneni, Gopinadh; Patnala, Sriramachandra Murthy; et al. Preparatio