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
[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. Preparation of heteroaryl compounds as 5-HT4 receptor ligands.WO2013042135A1